NCI Drug Dictionary

656 results found for: T

T-cell membrane-anchored tumor-targeted IL-12-modified tumor infiltrating lymphocytes: A preparation of tumor infiltrating lymphocytes (TILs) engineered to express membrane-bound interleukin-12 (mbIL-12), with potential immunomodulating and antineoplastic activities. Upon infusion of the T-cell membrane-anchored tumor-targeted IL-12-modified TILs, the cells specifically recognize and kill the tumor cells. IL-12 expression activates the immune system by promoting the secretion of interferon-gamma (IFNg), activating natural killer cells (NKs), and inducing cytotoxic T-lymphocyte (CTL) responses, further killing tumor cells.
T-Guard: (Other name for: anti-CD3/CD7-ricin toxin A immunotoxin)
T-Phyl: (Other name for: theophylline)
T-regulatory cell-enriched donor cells: A preparation of donor-derived T cells that have been enriched with donor T-regulatory (Treg) cells, with potential immunomodulating activity. Upon administration of the Treg cell-enriched donor cells prior to hematopoietic stem cell transplantation (HSCT), the donor cells may induce tolerance to HSCT and may reduce risk of relapse and graft-versus-host-disease (GVHD) in hematologic malignancies.
T1E28z CAR-expressing autologous CD4-positive T lymphocytes: Autologous CD4 positive T-lymphocytes engineered to express the chimeric antigen receptor (CAR) T1E28z containing the ErbB ligand, T1E, fused to the hinge region, transmembrane domain and endodomain of CD28 and the CD3zeta endodomain, with potential immunomodulating and antineoplastic activities. T1E, a chimeric polypeptide containing the N-terminus of human transforming growth factor (TGF)-alpha fused to the C-terminus of epidermal growth factor (EGF), binds to ErbB1 homodimers and heterodimers as well as ErbB2/3 heterodimers, but not to ErbB2 or ErbB3 alone. Upon intratumoral administration, the promiscuous ErbB ligand T1E of the T1E28z CAR-expressing autologous CD4-positive T lymphocytes binds to the specific ErbB homo- and heterodimers on tumor cells. This induces selective toxicity in ErbB-expressing tumor cells resulting in tumor cell lysis. ErbB1, ErbB2 and ErbB3, members of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, are frequently overexpressed in solid tumors and play key roles in tumor cell proliferation and tumor angiogenesis.
T900607: A pentafluorophenylsulfonamide compound with potential antineoplastic activity. T900607 inhibits tubulin polymerization by binding irreversibly to colchicine binding sites, resulting in cell cycle arrest and apoptosis.
Tab-cel: (Other name for: tabelecleucel)
tabalumab: A human IgG4 monoclonal antibody against B-cell activating factor (BAFF), with potential immunomodulating and antineoplastic activities. Tabalumab binds to and inhibits the activity of both soluble and cell surface-bound BAFF. This may reduce the activity, proliferation and survival of B-cells. A dysregulated expression of BAFF, a member of the tumor necrosis factor (TNF) family of proteins, is often seen in certain autoimmune diseases and certain cancers, and may promote B lymphocyte activation, proliferation and survival.
tabelecleucel: Allogeneic cytotoxic T lymphocytes (CTLs) selective for the tumor-associated antigens (TAAs) expressed by the Epstein-Barr virus (EBV), with potential immunostimulating and antineoplastic activities. Upon administration, and after hematopoietic cell transplants (HCT) or solid organ transplants (SOT), or during certain other immunocompromised states, tabelecleucel targets and binds to EBV-associated antigens expressed on EBV-infected cells. This results in lysis of EBV-infected cells and prevents growth of EBV-associated cancer cells. EBV is associated with a variety of cancers and post-transplant lymphoproliferative disorders (EBV+ PTLD).
Tabloid: (Other name for: thioguanine)
Tabrecta: (Other name for: capmatinib hydrochloride)
TAC regimen: A regimen consisting of docetaxel, doxorubicin and cyclophosphamide that can be used in the treatment of breast cancer.
TACC3 protein-protein interaction inhibitor AO-252: An orally bioavailable protein-protein interaction (PPI) inhibitor that targets transforming acidic coiled-coil-containing protein 3 (TACC3), with potential antineoplastic activity. Upon oral administration, TACC3 PPI inhibitor AO-252 targets and inhibits the interactions of TACC3 with its protein partners, including clathrin/KIFC1, BARD1 and MBD2/HAT complexes. This may inhibit tumor cell growth. TACC3 plays an important role in the regulation of mitosis, DNA damage response and epigenetic functions via its interaction with its protein partners.
tacedinaline: An orally bioavailable substituted benzamide derivative with potential antineoplastic activity. Tacedinaline inhibits histone deacetylation, which may result in histone hyperacetylation, followed by the induction of differentiation, the inhibition of cell proliferation, and apoptosis in susceptible tumor cell populations.
TachoComb H: (Other name for: aprotinin)
TachoSil: (Other name for: absorbable fibrin sealant patch)
tacrolimus: A macrolide isolated from Streptomyces tsukubaensis. Tacrolimus binds to the FKBP-12 protein and forms a complex with calcium-dependent proteins, thereby inhibiting calcineurin phosphatase activity and resulting in decreased cytokine production. This agent exhibits potent immunosuppressive activity in vivo and prevents the activation of T lymphocytes in response to antigenic or mitogenic stimulation. Tacrolimus possesses similar immunosuppressive properties to cyclosporine, but is more potent.
tadalafil: A carboline-based compound with vasodilatory activity. Tadalafil selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase- (PDE-5)-mediated degradation of cGMP, which is found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis. Inhibition of cGMP degradation by tadalafil results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection.
TAEK-VAC-HerBy vaccine: A cancer vaccine targeting the tumor-associated antigen (TAA) HER-2/neu (ErbB-2), with potential immunomodulating and antineoplastic activities. Upon administration, TAEK-VAC-HerBy vaccine may induce a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells expressing the HER-2/neu antigen, which may result in the inhibition of proliferation in Her-2/neu-expressing tumor cells. Her-2/neu, a member of the epidermal growth factor receptor (EGFR) family of tyrosine kinases, is overexpressed in various tumor cell types.
tafamidis meglumine: A soft gelatin capsule formulation containing the meglumine salt form of tafamidis, a small molecule and pharmacological chaperone with potential disease-modifying activity. Tafamidis binds to and stabilizes wild-type and variant (V122I) transthyretin (TTR), thereby preventing tetramer dissociation into monomers; this prevents misfolding of the TTR protein and inhibits the formation of TTR amyloid fibrils and the subsequent deposition of these insoluble protein clusters in peripheral nerve tissues and organs. TTR is a 127 amino acid transport protein for thyroxine and retinol and is secreted by the liver.
tafasitamab-cxix: An Fc engineered, humanized anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD19 with potential immunostimulating and antineoplastic activities. Tafasitamab-cxix targets and binds to CD19, thereby depleting and eliminating CD19-expressing B cells. The modified Fc region of XmAb5574 increases binding affinity to Fc-gamma receptors of effector cells and thereby enhances antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cell-mediated phagocytosis (ADCP). CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.
Tafinlar: (Other name for: dabrafenib mesylate)
tafolecimab: NCIt DEF: A human immunoglobulin G2 (IgG2) monoclonal antibody directed against human proprotein convertase subtilisin/kexin type 9 (PCSK9), with potential anti-hypercholesterolemic, anti-hyperlipidemic and antineoplastic activities. Upon administration, tafolecimab targets, binds to and inhibits the activity of PCSK9. This prevents the binding of PCSK9 to low-density lipoprotein receptor (LDLR) on hepatocytes and prevents its degradation. This increases LDLR on hepatocytes and increases the liver's ability to remove LDL cholesterol (LDL-C) from the blood, thereby lowering LDL-C levels. In addition, as PCSK9 may regulate proliferation and apoptosis in certain human cancer cells, tafolecimab may be able to inhibit proliferation and induce apoptosis in susceptible cancer cells, possibly due to its cholesterol-lowering effects. Tafolecimab may also enhance the anti-tumor immune response. PCSK9 binds to LDLR on the surface of hepatocytes to promote LDLR degradation within the liver.
Tag7 gene-modified vaccine: A cell-based vaccine composed of autologus inactivated tumor cells that have been genetically modified with the gene encoding for the innate immunity protein peptidoglycan recognition protein 1 (Tag7; PGRP-S; PGLYRP1; TAG-7), with potential immunomodulating and antineoplastic activities. Upon subcutaneous administration of Tag-7 gene-modified vaccine (GMV), the Tag-7 transfected tumor cells express Tag-7 which is presented to the immune system and activates the innate immune system. This may activate the immune system to exert a T-lymphocyte-mediated immune response against Tag-7-expressing tumor cells.
Tagamet: (Other name for: cimetidine)
tagitanlimab: A humanized monoclonal antibody directed against the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, tagitanlimab specifically targets and binds to PD-L1, blocking its binding to and activation of its receptor programmed cell death 1 (PD-1; cluster of differentiation 279; CD279). This reverses T-cell inactivation caused by PD-1/PD-L1 signaling and enhances the cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune response against PD-L1-expressing tumor cells. PD-L1 is overexpressed by many human cancer cell types. PD-L1 binding to PD-1 on T cells suppresses the immune system and results in immune evasion. PD-1, a transmembrane protein belonging to the immunoglobulin superfamily (IgSF) expressed on activated T cells, is a negative regulator of the immune system that limits the expansion and survival of CD8-positive T cells.
tagmokitug: A human immunoglobulin G1 (IgG1) afucosylated monoclonal antibody against C-C-chemokine receptor 8 (CCR8), with potential immunomodulating and antineoplastic activities. Upon administration, tagmokitug targets and binds to CCR8 on CCR8-positive tumor-infiltrating regulatory T cells (Tregs) in the tumor microenvironment (TME), and depletes CCR8-positive tumor-infiltrating Tregs via antibody-dependent cellular cytotoxicity (ADCC) and antibody dependent cellular phagocytosis (ADCP). This may reactivate antitumor immune responses. CCR8 is specifically expressed by tumor-infiltrating Tregs in multiple types of cancer and plays a key role in immunosuppression.
tagraxofusp-erzs: A recombinant protein consisting of human interleukin 3 (IL3) fused to the first 388 amino acids of diphtheria toxin [DT(388)] (DT388IL3) with potential antineoplastic activity. Upon intravenous administration of tagraxofusp-erzs, the IL3 moiety binds to IL3 receptors on cells expressing the receptor. Subsequently, the DT(388) toxin moiety, which contains both translocation and catalytic domains, is transported across the cell membrane via endocytosis. Within the cytosol, the catalytic domain of the toxin both catalyzes the ADP-ribosylation of, and inactivates, translation elongation factor 2 (EF-2), which results in the inhibition of translation during protein synthesis. IL3 may be overexpressed by a variety of cancers, including blastic plasmacytoid dendritic cell neoplasm and acute myeloid leukemia (AML).
Tagrisso: (Other name for: osimertinib)
Takecab: (Other name for: vonoprazan fumarate)
talabostat mesylate: The mesylate salt of an orally active small molecule with antineoplastic and hematopoiesis- stimulating activities. By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity. This agent may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. Dipeptidyl peptidases are involved in the activation of polypeptide hormones and chemokines.
talacotuzumab: A humanized IgG1 monoclonal antibody against CD123 (Interleukin-3 receptor alpha chain or IL3RA) with potential antineoplastic activity. Upon intravenous administration, talacotuzumab binds to and neutralizes CD123. This may inhibit IL-3-dependent signaling and may inhibit proliferation and differentiation in CD123-positive tumor cells. CSL362 contains an engineered Fc region which increases its binding affinity to Fc-gamma receptors on the surface of natural killer (NK) cells thereby initiating antibody-dependent cellular cytotoxicity (ADCC). CD123 is normally expressed on committed blood progenitor cells in the bone marrow; its overexpression is associated with increased leukemic cell proliferation and aggressiveness.
talactoferrin: An orally bioavailable recombinant human lactoferrin produced in the fungus Aspergillus niger with potential antineoplastic and immunomodulating activities. Upon oral administration, talactoferrin is transported into small intestinal Peyer's patches of the gut-associated lymphoreticular tissues (GALT), where it recruits circulating immature dendritic cells (DCs) bearing tumor antigens and induces their maturation. In the GALT, DC maturation in the presence of tumor antigens and lymphoid effector cells may induce systemic innate and adaptive immune responses mediated by anti-tumor natural killer (NK) cells, cytotoxic T lymphocytes, and natural killer T (NKT) cells; activation of tumor-draining lymph nodes, cellular infiltration of distant tumors, and tumor-cell death may follow. Raising the initial immune response in the GALT, distant from the primary tumor, may counter local tumor-mediated immunosuppression.
taladegib: An orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity. Taladegib inhibits signaling that is mediated by the Hh pathway protein Smo, which may result in a suppression of the Hh signaling pathway and may lead to the inhibition of the proliferation of tumor cells in which this pathway is abnormally activated. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair; constitutive activation of this pathway is associated with uncontrolled cellular proliferation and has been observed in a variety of cancers.
talampanel: A synthetic derivative of dioxolo-benzodiazepine with anti-seizure activity. Talampanel noncompetitively binds to the AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) subtype of glutamate excitatory amino acid receptors and may inhibit the growth of gliomas by interfering with neurotransmitters involved in brain tumor growth. This agent may also protect against traumatic brain injury.
talaporfin sodium: An agent consisting of chlorin e6, derived from chlorophyll, and L-aspartic acid with photosensitizing activity. After intratumoral activation by light emitting diodes, taporfin sodium forms an extended high energy conformational state that generates singlet oxygen, resulting in free radical-mediated cell death.
talazoparib tosylate: The tosylate salt form of talazoparib, an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity. Upon administration, talazoparib selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks.
talc: Finely-powdered native hydrous magnesium silicate. When administered into the pleural space, talc initiates an inflammatory reaction, resulting in adhesion of the visceral pleura to the parietal pleura and fibrosis, thereby effectively closing the pleural space and preventing further accumulation of fluid. This agent exhibits no intrinsic antineoplastic activity.
TALEN-edited HPV16/18 E6/E7 plasmid: A transcription activator-like effector nuclease (TALEN)-edited plasmid targeting human papillomavirus (HPV) types 16 (HPV16) and 18 (HPV18) epitopes E6 and E7, with potential antineoplastic activity. Upon administration of TALEN-edited HPV16/18 E6/E7, the TALEN targets and binds to specific sites on genomic HPV16 and 18 E6 and E7, and cleaves the DNA sequences encoding E6 and E7. This causes double-strand DNA (dsDNA) breaks, which prevents the transcription and translation of E6 and E7. In addition, inhibition of HPV16/18 E6/E7 increases the expression of tumor suppressor genes, such as p53 and retinoblastoma 1 (RB1). Altogether, TALEN-based HPV editing increases apoptosis and inhibits tumor cell proliferation of HPV-driven cancer cells. HPV16/18 E6 and E7 are oncogenes vital to viral function and carcinogenesis.
taletrectinib adipate: The adiptate form of taletrectinib, an orally available inhibitor of the receptor tyrosine kinases C-ros oncogene 1 (ROS1) and the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, with potential antineoplastic activity. Upon oral administration, taletrectinib binds to and inhibits ROS1 and the NTRK family members. This inhibition leads to a disruption of ROS1- and NTRK-mediated signaling and eventually inhibits the growth of tumor cells that are overexpressing ROS1 and/or NTRKs. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells. NTRK mutations or rearrangements play a key role in cancer progression.
talimogene laherparepvec: An ICP34.5, ICP47-deleted, oncolytic herpes simplex type-1 virus (HSV-1) based on the JS1 strain, and encoding the immunostimulating factor human cytokine granulocyte-macrophage colony stimulating factor (GM-CSF) with potential immunostimulating and antineoplastic activities. Upon intratumoral injection, talimogene laherparepvec selectively infects and replicates in tumor cells, thereby inducing tumor cell lysis. In addition, GM-CSF attracts dendritic cells (DCs) and may stimulate a cytotoxic T cell response against tumor cells, which results in immune-mediated tumor cell death. Deletion of the gene encoding for ICP34.5 provides tumor selectivity and prevents replication in healthy cells. As ICP47 blocks antigen presentation in HSV-infected cells, deletion of this gene may induce a more potent antitumor immune response in the tumor cells. Additionally, deletion of ICP47 causes increased expression of the HSV US11 gene and allows US11 to be expressed as an immediate early and not a late gene. This further enhances the degree of viral replication and oncolysis of tumor cells.
Tality: (Other name for: vitamins/minerals/proteins-based synthetic meal replacement)
talmapimod: An orally bioavailable, small-molecule, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential immunomodulating, anti-inflammatory, and antineoplastic activities. Talmapimod specifically binds to and inhibits the phosphorylation of p38 MAPK, which may result in the induction of tumor cell apoptosis, the inhibition of tumor cell proliferation, and the inhibition of tumor angiogenesis. This agent may also enhance proteasome inhibitor-induced apoptosis. p38 MAPK is a serine/threonine protein kinase involved in a MAPK signaling cascade that controls cellular responses to various environmental stresses, cytokines, and endotoxins.
talotrexin ammonium: The ammonium salt of an antimetabolite analogue of aminopterin with potential antineoplastic activity. As a folate antagonist, talotrexin binds to and inhibits the function of dihydrofolate reductase, resulting in the inhibition of folate metabolism, DNA synthesis, and cell division. Hydrosoluble, talotrexin is actively transported into cells by the reduced folate carrier (RFC) and, therefore, is unlikely to be associated with P-glycoprotein-mediated multidrug resistance.
talquetamab-tgvs: A bispecific humanized monoclonal antibody against human CD3, a T-cell surface antigen, and human G-protein coupled receptor family C group 5 member D (GPRC5D), a tumor-associated antigen (TAA), with potential antineoplastic activity. Upon administration, talquetamab-tgvs binds to both CD3 on T cells and GPRC5D expressed on certain tumor cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against GPRC5D-expressing tumor cells. GPRC5D is overexpressed on certain tumors, such as multiple myeloma, while minimally expressed on normal, healthy cells, and plays a key role in tumor cell proliferation.
taltirelin hydrate: The hydrate of tatirelin, a thyrotropin releasing hormone (TRH) analogue with potential neuroprotective, analgesic and central nervous system-stimulating (CNS)/analeptic activities. Taltirelin mimics the physiological actions of TRH on the CNS while exerting a minimal effect on the release of thyrotrophin (TSH) from the anterior lobe of the pituitary. Like TRH, the mechanism of action of this agent in the CNS has not been fully elucidated mechanism, but may involve various cerebral monoamine pathways. Compared to TRH, taltirelin has a much longer half-life and duration of effects.
Talvey: (Other name for: talquetamab-tgvs)
Talzenna: (Other name for: talazoparib tosylate)
TAM/c-Met inhibitor RXDX-106: An orally available and selective inhibitor of the receptor tyrosine kinase (RTK) activity of both hepatocyte growth factor receptor (c-Met; HGFR) and receptors in the TYRO3, AXL, and MER (TAM) family, with potential immunomodulating and antineoplastic activities. Upon oral administration of TAM/c-Met inhibitor RXDX-106, this agent selectively targets and binds to TYRO3, AXL, MER and c-Met, and prevents their RTK activity. This blocks TYRO3/AXL/MER/c-Met-mediated signal transduction pathways, and inhibits the proliferation and migration of TYRO3-, AXL-, MER- and c-Met-overexpressing tumor cells. Inhibition of the TAM family in the tumor microenvironment (TME) activates the immune system in the TME, reverses TAM mediated immunosuppression and enhances the anti-tumor immune response, which lead to immune-mediated tumor cell killing. TYRO3, AXL and MER, members of the TAM family of RTKs, are overexpressed in many tumor cell types. TAMs play key roles in tumor cell proliferation, survival, invasion, angiogenesis and metastasis, and their expression is associated with drug resistance and poor prognosis. c-Met, also overexpressed in many tumor cell types, plays a critical role in tumor formation, proliferation, invasion and metastasis, and contributes to tumor resistance. In the TME, TAM expression on immune cells contributes to tumor cell evasion of immune surveillance and to the negative regulation of immune responses.
tamibarotene: An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than ATRA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to ATRA. In addition, this agent may exhibit a lower toxicity profile than ATRA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium.
Tamiflu: (Other name for: oseltamivir phosphate)
tamnorzatinib: An orally available and selective inhibitor of the receptor tyrosine kinases (RTKs) Axl (UFO) and Mer, with potential antineoplastic activity. Upon administration, tamnorzatinib targets and binds to both Axl and Mer, and prevents their activity. This blocks Axl- and Mer-mediated signal transduction pathways, and inhibits proliferation and migration of Axl- and Mer-overexpressing tumor cells. Axl and Mer, both members of the TAM (Tyro3, Axl and Mer) family of RTKs, are overexpressed by many tumor cell types. They play key roles in tumor cell proliferation, survival, invasion, angiogenesis and metastasis, and their expression is associated with drug resistance and poor prognosis.
tamoxifen citrate: The citrate salt of an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA. The result is a reduction in DNA synthesis and cellular response to estrogen. In addition, tamoxifen up-regulates the production of transforming growth factor B (TGFb), a factor that inhibits tumor cell growth, and down-regulates insulin-like growth factor 1 (IGF-1), a factor that stimulates breast cancer cell growth. Tamoxifen also down-regulates protein kinase C (PKC) expression in a dose-dependant manner, inhibiting signal transduction and producing an antiproliferative effect in tumors such as malignant glioma and other cancers that overexpress PKC.
tamsulosin hydrochloride: The hydrochloride salt of tamsulosin, a sulfonamide derivative with adrenergic antagonist activity. Tamsulosin selectivity binds to and blocks the activity of alpha1 adrenoreceptors in the human prostate and bladder neck; blockade of these adrenoceptors can cause smooth muscle in the prostate and bladder neck to relax, resulting in an improvement in urinary flow rate.
tandutinib: A piperazinyl quinazoline receptor tyrosine kinase inhibitor with antineoplastic activity. Tandutinib inhibits the autophosphorylation of FLT3 (FMS-Like Tyrosine kinase-3), c-KIT and PDGF (platelet-derived growth factor) receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis.
tanespimycin: A benzoquinone antineoplastic antibiotic derived from the antineoplastic antibiotic geldanamycin. Tanespimycin binds to and inhibits the cytosolic chaperone functions of heat shock protein 90 (HSP90). HSP90 maintains the stability and functional shape of many oncogenic signaling proteins; the inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins that may be overexpressed by tumor cells.
tanezumab: A humanized monoclonal antibody directed against nerve growth factor (NGF), a modulator of nociceptor function, with potential analgesic activity. Tanezumab binds to NGF and prevents NGF binding to its high affinity, membrane-bound, catalytic receptor tropomyosin-related kinase A (TrkA), which is present on sympathetic and sensory neurons; reduced stimulation of TrkA by NGF inhibits the pain-transmission activities of these neurons. NGF, a neurotrophin, is critical to the growth and maintenance of sympathetic and sensory neurons. In addition, NGF may induce mast cells to release inflammatory proteins and may induce the upregulation of substance P and other pain-related peptides in sympathetic and sensory neurons. Upon neurotrophin binding, TrkA phosphorylates itself and members of the MAPK pathway, mediating the multiple neuronal effects of NGF.
tangerine tomato juice: Tomato juice derived from the tangerine tomato, with potential antioxidant and chemopreventive activities. Tangerine tomato juice contains higher levels of the cis-isomer of lycopene (cis-LYC) compared to the trans-isomer (trans-LYC). Lycopene, a linear, unsaturated hydrocarbon carotenoid, is the major red pigment in certain fruits such as tomatoes, pink grapefruit, apricots, red oranges, watermelon, rosehips, and guava. As an antioxidant, lycopene scavenges free radicals, which may both inhibit cellular oxidation and prevent free radical damage to cells. cis-LYC is better absorbed than its trans form.
tanomastat: A biphenyl matrix metalloproteinase (MMP) inhibitor (MMPI) with potential antineoplastic activity. Tanomastat inhibits MMP-2, MMP-3, and MMP-9, inhibiting extracellular matrix degradation and potentially inhibiting angiogenesis, tumor growth and invasion, and metastasis. MMPs consist of at least 18 zinc-containing endo-proteinases that are capable of degrading collagen and proteoglycan.
Tapazole: (Other name for: methimazole)
tapentadol hydrochloride ER: An orally active, extended-release preparation of the hydrochloride salt of tapentadol with analgesic activity. Tapentadol is a synthetic, centrally acting analgesic with a dual mechanism of action involving mu-opioid receptor agonism and norepinephrine reuptake inhibition. This agent may be effective in the management of pain, cancer-related and other.
TaperDex: (Other name for: dexamethasone)
tapotoclax: An inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (myeloid cell leukemia-1), with potential pro-apoptotic and antineoplastic activities. Upon administration, tapotoclax binds to and inhibits the activity of MCL-1. This disrupts the formation of MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complexes and induces apoptosis in tumor cells. MCL-1, an anti-apoptotic protein belonging to the Bcl-2 family of proteins, is upregulated in cancer cells and promotes tumor cell survival.
taragarestrant: An orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, taragarestrant specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells.
Tarceva: (Other name for: erlotinib hydrochloride)
tarenflurbil: An orally active synthetic enantiomer of flurbiprofen. Tarenflurbil activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in arrest of tumor cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumor cells. Tarenflurbil does not inhibit the enzyme cyclo-oxygenase.
tarextumab: A monoclonal antibody directed against the Notch receptor with potential antineoplastic activity. Tarextumab binds to Notch on the cell surface, thereby inhibiting Notch-mediated signaling and gene transcription, which may impede tumor angiogenesis. Notch receptors are important for cell-cell communication, which involves gene regulation mechanisms that control multiple cell differentiation processes during embryonic and adult life. Dysregulated Notch signaling is implicated in many diseases including T-ALL (T-cell acute lymphoblastic leukemia), CADASIL (cerebral autosomal dominant arteriopathy with sub-cortical infarcts and leukoencephalopathy), MS (multiple sclerosis), and many other disease states.
Targocid: (Other name for: teicoplanin)
Targretin: (Other name for: bexarotene)
tariquidar: An anthranilamide derivative with multidrug resistance properties. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs. Inhibition of transmembrane transport may result in increased intracellular concentrations of an anticancer drug, thereby augmenting its cytotoxicity.
tarlatamab-dlle: A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) delta-like protein 3 (DLL3) fused to one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration, tarlatamab binds to both the CD3 antigen on cytotoxic T lymphocytes (CTLs) and the DLL3 antigen found on DLL3-expressing tumor cells. This activates and redirects CTLs to DLL3-expressing tumor cells, which results in the CTL-mediated cell death of DLL3-expressing tumor cells. DLL3, a Notch pathway protein, is overexpressed on a variety of cancer cell types. It plays a key role in embryonic development and in tumor initiation and proliferation.
TARP 27-35 peptide vaccine: A peptide-based cancer vaccine, containing amino acid residues 27 through 35 of T cell receptor gamma alternate reading frame protein (TARP), with potential immunostimulatory and antineoplastic activities. Upon administration, TARP 27-35 peptide vaccine may stimulate a host cytotoxic T-cell (CTL) response against TARP-expressing tumor cells, resulting in tumor cell cytotoxicity. The nuclear protein TARP is commonly expressed on prostate and breast cancer cells and is highly immunogenic.
TARP 29-37-9V peptide vaccine: A peptide-based cancer vaccine, consisting of amino acid residues 29 through 37 of T cell receptor gamma alternate reading frame protein (TARP) with a leucine-to-valine substitution at position 9, with potential immunostimulatory and antineoplastic activities. Upon administration, TARP 29-37-9V peptide vaccine may induce a cytotoxic T-lymphocyte (CTL) response against TARP-expressing tumor cells, which may result in decreased tumor cell proliferation. The leucine-to-valine substitution at position 9 of this peptide improves its immunogenicity. The nuclear protein TARP is commonly expressed on prostate and breast cancer cells and is highly immunogenic.
Tarvacin: (Other name for: bavituximab)
TAS-108: A synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues. In addition, TAS-108 activates the co-repressor Silencing Mediator for Retinoid and Thyroid hormone receptor (SMRT), a protein that inhibits the activities of the estrogen receptors, which may contribute to the antitumor activity of TAS-108.
tasadenoturev-infected allogeneic bone marrow-derived mesenchymal stem cells: A preparation of bone marrow-derived allogeneic mesenchymal stem cells (MSCs) infected with tasadenoturev (Ad5-DNX-2401), an adenovirus serotype 5 strain that is selectively replication competent in cells defective in the Rb/p16 tumor suppressor pathway, with potential antineoplastic activity. Upon infusion of the tasadenoturev-infected bone marrow-derived MSCs, these cells target and deliver the adenovirus to tumor cells. The oncolytic virus then selectively transfects and replicates in the tumor cells, eventually leading to tumor cell lysis and the release of virus particles and various tumor associated antigens (TAAs). This may induce a systemic immune response against tumor cells expressing these TAAs and further infection and killing of nearby tumor cells by the released viral particles. Ad5-DNX-2401 contains an integrin binding RGD-4C motif, allowing Coxsackievirus and adenovirus receptor-independent infection of tumor cells, which are often deficient for Coxsackievirus and adenovirus receptors (CARs). As integral components of the late G1 restriction point, the Rb gene product and p16 are negative regulators of the cell cycle and are often defective in certain cancer types.
taselisib: An orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity. Taselisib selectively inhibits PIK3CA and its mutant forms in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting class I PI3K alpha, this agent may be more efficacious and less toxic than pan PI3K inhibitors. Dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and causes increased tumor cell growth, survival, and resistance to both chemotherapy and radiotherapy. PIK3CA, which encodes the p110-alpha catalytic subunit of the class I PI3K, is mutated in a variety of cancer cell types and plays a key role in cancer cell growth and invasion.
Tasigna: (Other name for: nilotinib hydrochloride monohydrate)
tasisulam sodium: The sodium salt form of tasisulam, an acyl-sulfonamide compound with potential antiproliferative activity. Tasisulam activates, through an as of yet not fully elucidated mechanism, the intrinsic mitochondrial-mediated cell death pathway as manifested by decreased adenosine triphosphate (ATP), cytochrome C release, activation of caspases, loss of mitochondrial membrane potential, production of reactive oxygen species (ROS) and eventually apoptosis.
Tasmar: (Other name for: tolcapone)
tasquinimod: A quinoline-3-carboxamide linomide analogue with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.
taurolidine: A synthetic broad-spectrum antibiotic with antibacterial, anticoagulant and potential antiangiogenic activities. Taurolidine, derived from the amino acid taurine, binds to and neutralizes bacterial exotoxins and endotoxins, or lipopolysaccharides (LPS). Taurolidine binding to LPS prevents bacterial adherence to host epithelial cells, thereby preventing bacterial invasion of uninfected host cells. Although the mechanism underlying its antineoplastic activity has not been fully elucidated, it may be related to this agent's anti-adherence property. In addition, taurolidine also promotes apoptosis by inducing various apoptotic factors and suppresses the production of vascular endothelial growth factor (VEGF), a protein that plays an important role in angiogenesis.
taurultam analogue GP-2250: An oxathiazine-based structural analogue of taurultam (TRLT), which is the main derivative of the anti-infective agent taurolidine (TRD), with potential antineoplastic activity. Upon administration, GP-2250 selectively induces reactive oxygen species (ROS)-mediated apoptosis in and inhibits proliferation of susceptible tumor cells.
Tavalisse: (Other name for: fostamatinib disodium)
Tavocept: (Other name for: dimesna)
tavokinogene telseplasmid: A DNA plasmid that encodes genes for both the p35 and p40 subunits of the heterodimeric human interleukin 12 (hIL-12) protein that are separated by an internal ribosome entry site (IRES) and under the control of a single cytomegalovirus (CMV) promoter, with potential immunomodulatory and antineoplastic activities. Upon administration via intratumoral injection and electroporation, the plasmid is introduced into human cells resulting in expression and highly-localized secretion of a functional IL-12 p70 protein into the tumor microenvironment (TME). IL-12 is a pro-inflammatory cytokine that plays a significant role in priming and maintaining T-helper (Th) cells, activating natural killer (NK) cells, and regulating the reactivation and survival of memory T cells (Tm). Increased levels of IL-12 in the TME may augment host immune response against tumor cells by inhibiting regulatory T cells (Tregs), T-helper 2 (Th2) responses, and myeloid-derived suppressor cells (MDSCs).
taxol analogue SID 530: An intravenous formulation containing docetaxel, a semi-synthetic, second-generation taxane derived from a compound found in the European yew tree, Taxus baccata, with potential antineoplastic activity. Taxol analogue SID 530 binds to and stabilizes tubulin, inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death.
Taxoprexin: (Other name for: DHA-paclitaxel)
Taxotere: (Other name for: docetaxel)
tazarotene: A synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.
tazemetostat hydrobromide: The hydrobromide salt form of tazemetostat, an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation.
Tazicef: (Other name for: ceftazidime sodium)
Tazorac: (Other name for: tazarotene)
Tazverik: (Other name for: tazemetostat hydrobromide)
TBF regimen: A regimen consisting of busulfan, fludarabine and thiotepa that is used as a conditioning regimen for hematopoietic stem cell transplantation (HSCT).
TBX-4000-treated hematopoietic stem cells TBX-2400: An allogeneic cell preparation in which donor-derived hematopoietic stem cells (HSCs) are treated ex vivo with TBX-4000, a recombinant TAT-MYC fusion protein, with potential immunoreconstitutive activity. Upon administration, the TBX-4000-treated HSCs TBX-2400 may enhance the engraftment of the bone marrow upon allogeneic hematopoietic stem cells transplant (HSCT). The TBX-4000 recombinant fusion protein consists of the N-terminal 9 amino acid segment of the HIV TAT protein transduction domain (PTD) fused to the MYC protein. TBX-4000 TAT-MYC rapidly localizes to the nucleus and transiently provides signals to drive proliferation and survival of the HSCs.
TCR alpha/beta/CD19-depleted allogeneic hematopoietic progenitor cells: A preparation of hematopoietic progenitor cells (HPCs) from a haploidentical donor that have been depleted of T-cell receptor (TCR) alpha and beta (TCRa/b+) as well as CD19-positive (CD19+) cells, that can potentially be used for immune reconstitution purposes. The TCR alpha/beta/CD19-depleted HPCs contain high amounts of natural killer (NK) cells, gamma/delta T cells, CD34+ stem cells, monocytes, and dendritic cells (DCs), while devoid of alpha/beta T cells and CD19-positive B cells. The TCR alpha/beta/CD19-depleted HPCs are used for allogeneic hematopoietic cell transplantation (HCT) and may allow for rapid and sustained engraftment, rapid immune reconstitution, and may prevent or reduce graft-versus-host disease (GvHD).
TCR-engineered T cells HRYZ-T101: A preparation of genetically engineered T lymphocytes expressing a T-cell receptor (TCR) targeting a specific tumor-associated antigen (TAA) of the human papillomavirus (HPV) type 18 (HPV-18), with potential antineoplastic activity. Upon administration, HPV-18 expressing TCR T cells target and bind to tumor cells expressing the HPV-18 TAA leading to selective cytotoxicity in HPV-18 TAA-expressing tumor cells. HPV18 TAAs are overexpressed in a variety of tumor cell types.
TCR-specific, alpha fetoprotein-enhanced autologous T lymphocytes: A preparation of human autologous T lymphocytes transduced with a viral vector encoding for a T-cell receptor (TCR) specific for human alpha-fetoprotein (AFP), with potential antineoplastic activity. Following administration, the TCR-specific, alpha fetoprotein-enhanced autologous T lymphocytes recognize and bind to AFP antigen-positive cells, which results in lysis and killing of AFP-positive cancer cells. AFP is overexpressed in a variety of cancers.
TEAD Inhibitor BGC515: An orally bioavailable inhibitor of the transcription factor TEAD (TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD inhibitor BGC515 targets, binds to and inhibits TEAD, thereby disrupting the interaction between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional coactivator with PDZ-binding motif (TAZ) and TEAD. This may inhibit YAP/TAZ-TEAD-promoted transcription of multiple genes involved in tumor cell proliferation, progression and survival, and may result in enhanced apoptosis in TEAD-dependent cancers. Hippo pathway alterations, as seen in tumors with neurofibromatosis type 2 (NF2)-deficiency, large tumor suppressor 1 (LATS1) and 2 (LATS2) mutations and YAP/TAZ fusions, lead to Hippo pathway activation, hyperactivation of YAP/TAZ and activation of TEAD. It plays a key role in cancer initiation, progression, and cancer cell resistance to various therapies.
TEAD inhibitor BPI-460372: An orally bioavailable, small molecule inhibitor of the transcription factor TEAD (TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD inhibitor BPI-460372 targets and covalently binds to the cysteine residue in the TEAD palmitoylation pocket, thereby disrupting the interaction between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional coactivator with PDZ-binding motif (TAZ) and TEAD and irreversibly inhibiting TEAD auto-palmitoylation. This may inhibit YAP/TAZ-TEAD-promoted transcription of multiple genes involved in tumor cell proliferation, progression and survival, and may result in enhanced apoptosis in TEAD-dependent cancers. Hippo pathway alterations, as seen in tumors with neurofibromatosis type 2 (NF2)-deficiency, large tumor suppressor 1 (LATS1) and 2 (LATS2) mutations and YAP/TAZ fusions, lead to Hippo pathway activation, hyperactivation of YAP/TAZ and activation of TEAD.
TEAD inhibitor SW-682: An orally bioavailable inhibitor of the transcription factor TEAD (TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD inhibitor SW-682 targets and binds to the TEAD palmitoylation pocket all TEAD isoforms, thereby disrupting the interaction between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional coactivator with PDZ-binding motif (TAZ) and TEAD and inhibiting TEAD auto-palmitoylation. This may inhibit YAP/TAZ-TEAD-promoted transcription of multiple genes involved in tumor cell proliferation, progression and survival, and may result in enhanced apoptosis in TEAD-dependent cancers. Hippo pathway alterations, as seen in tumors with neurofibromatosis type 2 (NF2)-deficiency, large tumor suppressor 1 (LATS1) and 2 (LATS2) mutations and YAP/TAZ fusions, lead to Hippo pathway activation, hyperactivation of YAP/TAZ and activation of TEAD.
TEAD inhibitor VT3989: An orally bioavailable, small molecule inhibitor of the auto-palmitoylation of the transcription factor TEAD (TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD inhibitor VT3989 inhibits TEAD auto-palmitoylation, thereby disrupting the interaction between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional coactivator with PDZ-binding motif (TAZ) and TEAD. This may inhibit YAP/TAZ-TEAD promoted gene transcription involved in tumor cell proliferation and survival. The Hippo-YAP/TAZ-TEAD pathway is dysregulated in certain cancers and diseases.
Teb-cel: (Other name for: tabelecleucel)
tebentafusp-tebn: A fusion protein containing a modified form of human T-cell receptor (TCR) specific for the gp100 antigen and fused to an anti-CD3 single-chain antibody fragment, with potential antineoplastic activity. Upon direct intratumoral administration of tebentafusp into the melanoma lesion, the TCR moiety of this agent targets and binds to the tumor associated antigen (TAA) gp100 presented on the melanoma tumor cell; the anti-CD3 fragment moiety binds to CD3- expressing T lymphocytes, thereby selectively cross-linking tumor cells and T lymphocytes. This may lead to the recruitment of cytotoxic T lymphocytes (CTL) to the T lymphocyte/tumor cell aggregates and result in CTL-mediated death of gp100-expressing melanoma cancer cells.
tebotelimab: An Fc-bearing, humanized antibody-like protein that specifically recognizes the immune checkpoint molecules programmed cell death 1 (PD-1; PD1; PDCD1; CD279; Programmed Death 1) and lymphocyte activation gene-3 (LAG-3; LAG3; CD223), with potential T-lymphocyte immunomodulatory and antineoplastic activities. Upon administration, tebotelimab specifically binds to both PD-1 and LAG-3, which are both expressed on T cells. The dual blockade of the PD-1 and LAG-3 pathways enables potent activation of a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. PD-1 and LAG-3 play key roles in suppressing T-cell activation.
Tecadriol: (Other name for: D-chiro-inositol and alpha-lactalbumin supplement)
tecaginlimab: A humanized immunoglobulin (Ig) G1, Fc-silenced, bispecific, agonistic monoclonal antibody targeting both CD40 and 4-1BB (CD137; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunostimulatory and antineoplastic activity. Upon administration, tecaginlimab simultaneously binds to CD40 and 4-1BB, crosslinks CD40 and 4-1BB positive cells, induces conditional stimulation, and activates both CD40- and 4-1BB-medicated signaling. The activation of CD40-mediated signaling triggers the proliferation and activation of antigen-presenting cells (APCs) and activates T cells. This results in an enhanced cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. The activation of 4-1BB-mediated signaling induces cytokine production and promotes T-cell mediated anti-tumor immune responses. CD40, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on various immune cells, such as dendritic cells (DCs), macrophages and B-cells, and plays a key role in the activation of the immune system. 4-1BB, a surface glycoprotein of the TNFRSF, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity.
Tecartus: (Other name for: brexucabtagene autoleucel)
Tecelra: (Other name for: afamitresgene autoleucel)
Tecentriq: (Other name for: atezolizumab)
Tecentriq Hybreza: (Other name for: atezolizumab and hyaluronidase-tqjs)
Tecfidera: (Other name for: dimethyl fumarate)
TechneScan MDP: (Other name for: technetium Tc 99m methylene diphosphonate)
technetium Tc 94m sestamibi: A radioconjugate consisting of sestamibi labeled with the positron-emitting isotope Tc 94m. Sestamibi is a synthetic molecule of the isonitrile family that diffuses through cell membranes and may preferentially accumulate within mitochondria. Technetium Tc 94m sestamibi may be used in tumor-imaging studies utilizing positron emission tomography (PET).
technetium Tc 99 hydrazinonicotinamide-tricine-linked interleukin-2: A radioconjugate composed of the cytokine interleukin-2 (IL-2) conjugated to the bifunctional chelating agent succinimidyl-6-hydrazinopyridine-3-carboxylate (HYNIC-NHS) and co-ligand tricine and labeled with the radioisotope technetium Tc 99m (99mTc-HYNIC-IL2), that can potentially be used as a diagnostic agent to detect tumor inflammation. Upon intravenous administration, IL-2 selectively binds to the IL-2 receptor (IL-2R) expressed on tumor infiltrating lymphocytes (TILs); upon internalization, the Tc99m moiety can be visualized using radioimaging, which allows the quantification of TILs expressing IL-2R. This agent detects tumor enlargement due to invasion by TILs and not tumor progression.
technetium Tc 99 MIRC213: A radioconjugate composed of a nanobody directed against human epidermal growth factor receptor 2 (HER2; EGFR2; ERBB2) that is site-specifically labeled with technetium Tc 99m, with potential use as a tracer for HER2-expressing tumors using single photon emission computed tomography/computed tomography (SPECT/CT). Upon administration of technetium Tc-99m-MIRC213, the anti-HER2 nanobody moiety targets and binds to HER2-expressing tumor cells. This allows the detection of HER2-expressing tumor cells upon SPECT/CT. HER2, a receptor tyrosine kinase, is overexpressed on the cell surfaces of various tumor cell types; it plays a key role in tumor cell proliferation and tumor vascularization.
technetium Tc 99m anti-HER2 affibody HPArk2: A radioconjugate composed of an affibody targeting human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2), labeled with technetium Tc 99m, with potential imaging activity using single photon emission computed tomography (SPECT)/computed tomography (CT). Upon administration, the anti-HER2 affibody moiety of technetium Tc-99m anti-HER2 affibody HPArk2 targets and binds to HER2-expressing tumor cells. Upon SPECT/CT imaging, HER2-expressing tumor cells can be detected. HER2, a receptor tyrosine kinase, is mutated in many tumor cell types and plays a key role in tumor cell proliferation and tumor vascularization.
technetium Tc 99m demobesin-4: A radioconjugate composed of the synthetic bombesin (BB) analog demobesin-4 bound to the radioisotope technetium Tc 99m with receptor ligand and gamma-emitting radioisotope activities. Upon intravenous administration, demobesin-4 selectively binds to the gastrin-releasing peptide receptor (GRPR) expressed on the surfaces of various tumor cell types; upon internalization, tumor cells expressing GRPRs bound to technetium Tc 99m can then be visualized using scintigraphy. GRPR, a bombesin receptor subtype, is frequently overexpressed on the surface of tumor cells such as prostate and breast cancer cells. Demobesin-4 was developed for technetium Tc 99m imaging of GRPR-expressing tumor cells.
technetium Tc 99m DTPA: A radiopharmaceutical core of chelating agent DTPA (diethylenetriaminepentaacetic acid) complexed with the gamma-emitting radionuclide technetium Tc 99m with radioimaging application. Tc-99m-DTPA has been utilized as a radiotracer, when conjugated to tissue specific molecules, in a wide variety of nuclear imaging studies, including brain, lung, and renal function studies.
technetium Tc 99m epratuzumab: A radioimmunoconjugate of the humanized IgG1 monoclonal antibody (MoAb) LL2 labeled with Technetium 99m (Tc-99m). Epratuzumab (MoAb LL2) recognizes CD22, a B-lymphocyte-restricted antigen expressed as a cytoplasmic protein in progenitor B cells, and as a cell surface protein in mature B cells. Tc-99m epratuzumab delivers gamma emission Tc-99m directly to B-lymphocyte lineage cells, thereby the agent may be used for diagnostic or treatment purposes.
technetium Tc 99m ethylenedicysteine-deoxyglucose: A radiopharmaceutical consisting of ethylenedicysteine-deoxyglucose (EC-DG) labeled with the metastable radioisotope technetium Tc-99 (99mTc). Upon administration, technetium Tc 99m ethylenedicysteine-deoxyglucose accumulates in cells with increased metabolic activity such as proliferating tumor cells; tumor tissue may then be imaged using gamma scintigraphy.
technetium Tc 99m galactosyl human serum albumin: A colloid formulation of human galactosyl serum albumin (GSA) conjugated to the chelating agent diethylene-triaminepentaacetic acid (DTPA) and complexed to the gamma-emitting isotope technetium-99m (99mTc-GSA) with potential diagnostic imaging activity. Upon intravenous administration, the galactosyl moiety of 99mTc-GSA binds to asialoglycoprotein receptors (ASGPR) located on hepatic cells. Upon SPECT (Single Photon Emission Computed Tomography) imaging, liver function can be assessed. The expression of ASGPR, which are solely found on the plasma membrane of mammalian hepatocytes, is associated with hepatic function.
technetium Tc 99m glycopeptide: A technetium Tc 99m radiopharmaceutical of a glutamate-rich peptide (GP) conjugated, via carbodiimide linker, to the heparin-like polysaccharide chitosan (CH) in a 1:1 ratio, with potential tumor targeting property. Upon administration, 99m Tc-glycopeptide targets and is taken up by glutamate-specific transporters on tumor cells. Upon internalization, the Tc99m moiety can be visualized upon scanning. GP may potentially be used as a drug carrier for antineoplastic drug delivery to tumor cells.
technetium Tc 99m hydroxydiphosphonate: A radioconjugate containing hydroxydiphosphonate (HDP) labeled with the metastable radioisotope technetium Tc (99mTc), with radioimaging activity. Upon intravenous administration, skeletal uptake of technetium Tc-99m HDP occurs as a function of skeletal blood flow and osteogenic activity. HDP has a specific affinity for hydroxyapatite crystals in bone where abnormal accumulation of increased osteoid mineralization has occurred. Labeling of HDP with 99mTc allows gamma scintigraphic imaging of areas of abnormal osteogenesis associated with malignant bone lesions.
technetium Tc 99m mebrofenin: A radioconjugate composed of the iminodiacetic acid derivative mebrofenin bound to an isotope of the synthetic element technetium (Tc). Upon administration and rapid clearance form the circulation, technetium Tc 99m mebrofenin is secreted into the hepatobiliary system, emitting gamma rays that are detectable with planar scintigraphy or single photon emission computer tomography (SPECT). Mebrofenin has no pharmacological effect at the recommended dosage for diagnostic imagining.
technetium Tc 99m methylene diphosphonate: A radiopharmaceutical containing methylene diphosphonate (medronate; MDP) complexed with the gamma-emitting radionuclide technetium Tc 99m with radioisotopic activity and hydroxyapatite affinity. Upon intravenous administration, skeletal uptake of technetium Tc 99m methylene diphosphonate occurs as a function of skeletal blood flow and osteogenic activity. The MDP moiety of this agent has affinity for hydroxyapatite crystals in bone with abnormal accumulation at sites with increased osteoid mineralization; labeling of MDP with Tc 99m allows scinitgraphic imaging of areas of abnormal osteogenesis associated with malignant bone lesions.
technetium Tc 99m NTP 15-5: A radioconjugate consisting of N-(triethylammonium)-3-propyl-[15]ane-N5 (NTP 15-5), labeled with the gamma-emitting, metastable radioisotope technetium Tc-99 (99mTc), with potential imaging activity upon SPECT (single photon emission computed tomography). Upon administration of technetium Tc-99m NTP 15-5, NTP 15-5 targets and binds to proteoglycans (PGs) present in cartilage extracellular matrix (ECM). This may allow the visualization of cartilage neoplasms and/or cartilage remodeling in arthritis upon imaging.
technetium Tc 99m sulfur colloid: A gamma-emitting colloid used in scintillation scanning of the reticuloendothelial system (RES). After intravenous administration, technetium Tc 99m sulfur colloid is phagocytized by the reticuloendothelial system and concentrated in the liver, spleen, and bone marrow; detection/localization of phagocytized gamma ray-emitting colloid is performed with a gamma-ray scintillation camera. Scintillation scanning using technetium Tc 99m colloid sulfur helps determine the distribution and function of the RES and the extent to which tumor involves the RES. The RES includes cells types that can phagocytize and sequester inert particles and vital dyes; RES cell types include macrophages or macrophage precursors, specialized endothelial cells lining the sinusoids of the liver, spleen, and bone marrow, and reticular cells of lymphatic tissue and of bone marrow.
technetium Tc 99m trofolastat: A radioconjugate composed of an urea-based human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the gamma-emitting radioisotope technetium Tc 99m, with potential use as a tracer for PSMA-expressing tumors using single photon emission computed tomography/computed tomography (SPECT/CT). Upon intravenous administration of the technetium Tc 99m trofolastat, the trofolastat moiety targets and binds to PSMA-expressing tumor cells. Upon internalization, PSMA-expressing tumor cells can be detected during SPECT/CT imaging. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells.
technetium Tc 99m-3PRGD2: A radiopharmaceutical agent comprised of a pegylated arginine-glycine-aspartic acid (RGD) dimer (PRGD2) labeled with technetium Tc 99m, with potential alphaVbeta3 integrin imaging activity when used with single photon emission computed tomography (SPECT). After intravenous administration of technetium Tc 99m-3PRGD2, the RGD moiety binds to alphaVbeta3 integrin on the cell membrane via the cyclic RGD motif. Upon PET imaging, alphaVbeta3 integrin-expressing tumor cells can be visualized and expression levels can be quantified. Compared to other radiolabeled RGD-containing peptides, this agent shows an increased affinity for alphaVbeta3 integrin, enhanced tumor uptake as well as improved pharmacokinetics. AlphaVbeta3 integrin, a member of the integrin receptor family, is overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells; this receptor plays a key role in angiogenesis, tumor proliferation and survival.
technetium Tc 99m-labeled albumin microspheres: An injectable radiopharmaceutical formulation containing human serum albumin (HSA) microspheres labeled with technetium-99m (Tc-99m) with diagnostic imaging activity. Technetium Tc 99m-labeled albumin microspheres contain the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. Upon injection into the hepatic artery, the radionuclide portion allows for SPECT (single photon emission computed tomography) imaging of distribution patterns of the albumin microspheres. This may possibly predict the distribution of other agents with similar particle sizes within the liver and may give a prediction of the tumor response upon administration of such agents.
technetium Tc 99m-labeled macroaggregated albumin: An injectable radiopharmaceutical formulation containing human serum albumin (HSA) labeled with technetium-99m (Tc99m) in macroaggregates (MAA) with diagnostic imaging activity. Technetium Tc 99m-labeled macroaggregated albumin contains the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. Upon injection into the hepatic artery and upon SPECT (single photon emission computed tomography) imaging, distribution patterns and possible prediction of expected distribution of agents with similar particle sizes within the liver can be assessed and may give a prediction about the tumor response upon administration of such agents.
technetium Tc 99m-labeled tilmanocept: A radiolabeled macromolecule consisting of the chelating agent diethylenetriamine pentaacetic acid (DTPA) and mannose each attached to a dextran backbone and labeled with metastable technetiumTc-99 (Tc-99m), with mannose binding and radioisotopic activities. Upon injection, the mannose moiety of technetium Tc 99m-labeled tilmanocept binds to mannose-binding protein (MBP). As MBPs reside on the surface of dendritic cells and macrophages, this gamma-emitting macromolecule tends to accumulate in lymphatic tissue where it may be imaged using gamma scintigraphy. This agent exhibits rapid clearance from the injection site, rapid uptake and high retention within the first draining lymph node, and low uptake by the remaining lymph nodes. MBP is a C-type lectin that binds mannose or fucose carbohydrate residues, such as those found on the surfaces of many pathiogens, and once bound activates the complement system.
technetium Tc 99m-NC100692: A synthetic Arg-Gly-Asp (RGD)-containing cyclic peptide radiolabeled with technetium Tc 99m with integrin-binding and radioisotopic activities. Upon administration, technetium Tc 99m-NC100692 binds to alpha5beta3 integrin and to a lesser extent alpha5beta5; subsequently, alpha5beta3-expressing tumor cells can be visualized using scintigraphy and the degree of tumor angiogenesis can be determined. Integrins, membrane-spanning protein receptors, may be upregulated on proliferating endothelial cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells and poor prognosis.
technetium TC-99m: One of the radioactive isotopes of technetium, a gamma/beta-emitter with a half life of 6 hours.
technetium Tc-99m anti-HER2 affibody ABH2: A radioconjugate composed of an optimized affibody labeled with technetium Tc 99m, with potential use as a tracer for human epidermal growth factor receptor type 2 (HER2; ErbB2)-expressing tumors using single photon emission computed tomography (SPECT). Upon administration, the Tc 99m-labeled affibody ABH2 targets and binds to HER2-expressing tumor cells. This facilitates both detection of HER2-expressing tumor cells and assessment of responses to HER2-targeting chemotherapeutic agents using SPECT. HER2, a receptor tyrosine kinase, is mutated in many tumor cell types and plays a key role in tumor cell proliferation and tumor vascularization.
technetium Tc-99m DARPinG3: A radioconjugate composed of the scaffold protein DARPinG3, labeled with technetium Tc 99m, with potential imaging activity for human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2)-expressing tumor cells upon single photon emission computed tomography (SPECT)/computed tomography (CT). Upon administration of technetium Tc-99m DARPinG3, the DARPinG3 moiety targets and binds to HER2-expressing tumor cells. Upon SPECT/CT imaging, HER2-expressing tumor cells can be detected. HER2, a receptor tyrosine kinase, is mutated in many tumor cell types and plays a key role in tumor cell proliferation and tumor vascularization.
technetium Tc-99m human serum albumin colloid: A colloid formulation of human serum albumin (HSA) labeled with technetium-99m (Tc-99m) with diagnostic imaging properties. This HSA radioconjugate contains the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. A potential advantage of the Tc-99m-HSA suspension is its smaller colloid particle size as compared to formulations containing either sulfur or tin, thereby allowing for enhanced imaging of the lymphatic draining pattern during lymphoscintigraphic or sentinel lymph node mapping procedures.
technetium Tc-99m sestamibi: Sestamibi is a large synthetic molecule of the isonitrile family, which can be labeled with Tc99m. It passes through cells membranes passively, collecting in cells with large numbers of mitochondria. It is often used for imaging of the thyroid and parathyroid.
technetium Tc-99m tetrofosmin: A radiopharmaceutical consisting of tetrofosmin, composed of two bidentate diphosphine ligands chelating the metastable radioisotope technetium Tc-99 (99mTc), with potential imaging activity upon SPECT (single photon emission computed tomography). Upon administration, technetium Tc 99m tetrofosmin is preferentially taken up by, and accumulates in, myocardial cells. Upon imaging, myocardial cells can be visualized and changes in ischemia and/or perfusion can be detected.
technetium Tc-99m-labeled rhenium sulfide nanocolloid: A colloid formulation of rhenium sulfide that is labeled with the gamma-emitting epitope technetium Tc 99m (Tc-99m) with diagnostic imaging activity. Upon administration, the 99mTc-colloidal rhenium sulfide is taken up by the lymph nodes. This allows imaging of the lymphatic drainage pattern during sentinel lymph node mapping, also known as lymphoscintigraphy.
technetium Tc-99m-MIRC208: A radioconjugate composed of a nanobody directed against human epidermal growth factor receptor 2 (HER2; EGFR2; ERBB2) that is labeled with technetium Tc 99m, with potential use as a tracer for HER2-expressing tumors using single photon emission computed tomography/computed tomography (SPECT/CT). Upon administration of technetium Tc-99m-MIRC208, the anti-HER2 nanobody moiety targets and binds to HER2-expressing tumor cells. This facilitates both the detection of HER2-expressing tumor cells and the assessment of responses to HER2-targeting chemotherapeutic agents using SPECT/CT. HER2, a receptor tyrosine kinase, is overexpressed on the cell surfaces of various tumor cell types; it plays a key role in tumor cell proliferation and tumor vascularization.
technitium Tc 99m ADAPT6: A radioconjugate composed of the imaging probe albumin-binding domain (ABD)-derived affinity protein (ADAPT) 6, which contains the ABD of streptococcal protein G as a stable protein scaffold, targeting human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2), and labeled with technetium Tc 99m, with potential imaging activity using single photon emission computed tomography (SPECT)/computed tomography (CT). Upon administration, the anti-HER2 binding moiety of technetium Tc 99m ADAPT6 targets and binds to HER2-expressing tumor cells. Upon SPECT/CT imaging, HER2-expressing tumor cells can be detected. HER2, a receptor tyrosine kinase, is mutated in many tumor cell types and plays a key role in tumor cell proliferation and tumor vascularization.
teclistamab-cqyv: A bispecific humanized monoclonal antibody against human CD3, a T-cell surface antigen, and human B-cell maturation antigen (BCMA; TNFRSF17), a tumor-associated antigen (TAA) expressed on plasma cells, with potential antineoplastic activity. Upon administration, teclistamab-cqyv binds to both CD3 on T cells and BCMA expressed on malignant plasma cells. This results in the cross-linking of T cells and tumor cells, and induces a potent cytotoxic T-lymphocyte (CTL) response against BCMA-expressing plasma cells. BCMA, a member of the tumor necrosis factor receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.
tecogalan sodium: A sulfated polysaccharide isolated from various Arthrobacter bacterial species. Possessing potential antiangiogenic and antineoplastic properties, tecogalan binds to basic fibroblast growth factor (bFGF), thereby preventing bFGF from binding to its receptors. Disruption of this receptor binding results in the inhibition of bFGF-stimulated endothelial cell growth, proliferation, and migration.
tecovirimat: An orally available small molecule with activity against orthopoxviruses. Tecovirimat is an inhibitor of viral p37 and blocks the ability of virus particles to be released from infected cells.
Tectin: (Other name for: tetrodotoxin)
Tecvayli: (Other name for: teclistamab-cqyv)
Teflaro: (Other name for: ceftaroline fosamil)
tegafur: A congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme. Subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by inhibiting thymidylate synthase and reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate.
Tegafur-gimeracil-oteracil Potassium: An orally bioavailable fluoropyrimidine antagonist composed of tegafur combined with two modulators of 5-fluorouracil (5-FU) activity, gimeracil and potassium oxonate, in a molar ratio of 1:0.4:1. Tegafur is a prodrug of 5-fluorouracil, an antimetabolite that inhibits thymidylate synthase, DNA synthesis and cell division, and competes with uridine triphosphate, thus inhibiting RNA and protein synthesis. Gimeracil is a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the liver enzyme responsible for rapid catabolism of 5-FU into inactive metabolites. Potassium oxonate preferentially localizes in the gut and inhibits the enzyme orotate phosphoribosyl-transferase (OPRT), thereby decreasing activation of 5-FU in the gut and activated 5-FU-related gastrointestinal toxicity.
tegafur-gimeracil-oteracil potassium-leucovorin calcium oral formulation: An orally bioavailable granular formulation composed of the fluoropyrimidine antagonist tegafur combined with two modulators of 5-fluorouracil (5-FU) activity, gimeracil and oteracil potassium, and the folic acid derivative leucovorin calcium, with potential antineoplastic activity. Tegafur is a prodrug of 5-fluorouracil (5-FU), an antimetabolite that is further metabolized to 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP inhibits thymidylate synthase, DNA synthesis and cell division; FUTP competes with uridine triphosphate (UTP), thus inhibiting RNA and protein synthesis. Gimeracil is a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the liver enzyme responsible for rapid catabolism of 5-FU into inactive metabolites. Oteracil potassium preferentially localizes in the gut and inhibits the enzyme orotate phosphoribosyl-transferase (OPRT), which converts tegafur to 5-FU. This decreases the amount of 5-FU in the gut and prevents activated 5-FU-related gastrointestinal (GI) toxicity. Leucovorin calcium, an active metabolite of folic acid, counteracts the toxic effects of 5-FU, thereby 'rescuing' the patient while permitting the antitumor activity of 5-FU.
tegafur-uracil: A formulated therapeutic oral agent consisting of a combination of the 5-fluorouracil (5-FU) congener prodrug tegafur (tetrahydrofuranyl-5-fluorouracil) and uracil (1:4). The high concentration of uracil reversibly inhibits the uracil-reducing enzyme dihydropyrimidine dehydrogenase (DPD), thereby inhibiting first-pass DPD-mediated hepatic metabolism of the uracil analogue 5-FU and permitting administration of 5-FU as the orally bioavailable prodrug tegafur. Tegafur is bioactivated to 5-FU by liver microsomal cytochrome P450 enzymes. 5-FU is subsequently converted into its active metabolites 5-fluoro-deoxyuridine-monophosphate (FdUMP) and 5-fluorouridine-triphosphate (FUTP) intracellularly; these metabolites inhibit the enzyme thymidylate synthase and intercalate into RNA, resulting in decreased thymidine synthesis, reduced DNA synthesis, disrupted RNA function, and tumor cell cytotoxicity.
tegavivint: A small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity. Upon intravenous administration, tegavivint binds to transducin beta-like protein 1 (TBL1) and disrupts the binding of beta-catenin to TBL1. This promotes beta-catenin degradation, attenuates nuclear and cytoplasmic levels of beta-catenin, and reduces transcriptional activity of transcription factor 4 (TCF4) and expression of its target genes, cyclin D1, c-Myc and survivin. The Wnt/beta-catenin signaling pathway regulates cell morphology, motility, and proliferation; aberrant regulation of this pathway leads to neoplastic proliferation. Beta-catenin is frequently mutated in various tumors.
teglarinad chloride: A water-soluble prodrug of a cyanoguanidine compound with potential antineoplastic activity. In vivo, teglarinad chloride is rapidly converted into active drug through hydrolytic cleavage of a carbonate ester bond. Although the exact mechanism of action has yet to be fully elucidated, the active drug appears to antagonize nuclear factor-kappa B (NF-kB) transcription, resulting in the induction of tumor cell apoptosis.
Tegretol: (Other name for: carbamazepine)
teicoplanin: A glycopeptide antibiotic complex isolated from the bacterium Actinoplanes teichomyceticus. Teicoplanin inhibits peptidoglycan polymerization, resulting in inhibition of bacterial cell wall synthesis and cell death.
telaglenastat: An orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. Upon oral administration, telaglenastat selectively and irreversibly inhibits glutaminase, a mitochondrial enzyme that is essential for the conversion of the amino acid glutamine into glutamate. By blocking glutamine utilization, proliferation in rapidly growing cells is impaired. Glutamine-dependent tumors rely on the conversion of exogenous glutamine into glutamate and glutamate metabolites to both provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival.
telaprevir: An orally available peptidomimetic small molecule with activity against hepatitis C virus (HCV). Telaprivir is a selective protease inhibitor that targets the viral HCV NS3-4A serine protease and disrupts processing of viral proteins and formation of a viral replication complex.
telapristone acetate: The acetate form of the 21-substituted-19-nor-progestin telapristone, an orally available selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Upon oral administration, telapristone competitively binds to the progesterone receptor (PR) in progesterone-responsive tissue and inhibits PR-mediated gene expression. This interferes with progesterone activity in the reproductive system. As a result, this agent may suppress ovulation and inhibit proliferation of endometrial tissue. Also, this agent may prevent cell growth and induce apoptosis in estrogen receptor (ER) and PR-positive breast cancer cells through a reduction in progesterone levels, ER downregulation and a suppression of the expression of cyclin-dependent kinases (CDK) 2 and 4, ultimately leading to G1/S cell cycle arrest. Unlike some other SPRMs, this agent does not exert any estrogenic, androgenic, anti-estrogenic, and anti-androgenic activities.
telatinib mesylate: The orally bioavailable mesylate salt of the 17-allylaminogeldanamycin (17-AAG) small-molecule inhibitor of several receptor protein tyrosine kinases with potential antiangiogenic and antineoplastic activities. Telatinib binds to and inhibits the vascular endothelial growth factor receptors (VEGFRs) type 2 and 3, platelet-derived growth factor receptor beta (PDGFRb) and c-Kit, which may result in the inhibition of angiogenesis and cellular proliferation in tumors in which these receptors are upregulated. These telatinib-inhibited receptor protein tyrosine kinases are overexpressed or mutated in many tumor cell types and may play key roles in tumor angiogenesis and tumor cell proliferation. 17-AAG is a synthetic analogue of the benzoquinone ansamycin antibiotic geldanamycin and has also been found to inhibit the molecular chaperone Hsp90.
telavancin hydrochloride: The hydrochloride salt form of telavancin, a lipoglycopeptide and a semisynthetic derivative of vancomycin with antibacterial activity against gram-positive bacteria. Like vancomycin, telavancin binds tightly to the D-alanyl-D-alanine residue of cell wall precursors, thereby interfering with bacterial cell wall synthesis. In addition, the lipophilic moiety of telavancin may interact with the lipid bilayer in the bacterial cell membrane, thereby compromising the integrity of cell membrane and causing cell membrane depolarization. This novel mechanism of action may contribute to telavancin's rapid bactericidal activity and its improved activity over vancomycin against some antibiotic resistance gram-positive bacteria.
telbivudine: A synthetic thymidine nucleoside analogue with antiviral activity highly specific for the treatment of hepatitis B virus (HBV). Intracellularly, telbivudine is phosphorylated to its active metabolite, telbivudine triphosphate. The dideoxy telbivudine triphosphate competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). This results in the blockade of HBV DNA replication and viral propagation.
TELCYTA: (Other name for: canfosfamide hydrochloride)
Telintra: (Other name for: ezatiostat hydrochloride)
Telisotuzumab: An immunoglobulin G1 (IgG1) humanized monoclonal antibody directed against human hepatocyte growth factor receptor (HGFR or c-Met), with potential antineoplastic activity. Telisotuzumab binds to c-Met, thereby preventing both c-Met binding to its ligand, HGF and the subsequent activation of the HGF/c-Met signaling pathway. This may cause cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.
telisotuzumab adizutecan: An antibody-drug conjugate (ADC) composed of a monoclonal antibody against the tumor-associated antigen (TAA) proto-oncogene c-Met (hepatocyte growth factor receptor; HGFR) linked to an undisclosed topoisomerase inhibitor, with potential antineoplastic activity. Upon intravenous administration of anti-c-Met ADC ABBV-400, the monoclonal antibody moiety targets and binds to c-Met expressed on tumor cells. Upon binding and internalization, the topoisomerase inhibitor is released, which binds to and inhibits topoisomerase, thereby inhibiting DNA replication and killing the c-Met-expressing cancer cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis and tumor angiogenesis.
telisotuzumab vedotin: An antibody-drug conjugate (ADC) composed of telisotuzumab, a monoclonal antibody against the tumor-associated antigen (TAA) and proto-oncogene, c-Met receptor tyrosine kinase (c-Met; MET; hepatocyte growth factor receptor; HGFR) conjugated to the cytotoxic agent monomethyl auristatin E (MMAE) via a valine-citrulline (vc) peptide linker (vc-MMAE; vedotin), with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of telisotuzumab vedotin targets and binds to c-Met expressed on tumor cells. Upon binding, internalization and enzymatic cleavage, the cytotoxic agent MMAE is released into the cytosol. MMAE binds to tubulin and inhibits tubulin polymerization, which results in G2/M phase arrest and tumor cell apoptosis. This kills the c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays key roles in tumor cell proliferation, survival, invasion, metastasis and tumor angiogenesis.
telitacicept: A fusion protein composed of the extracellular domain of human tumor necrosis factor receptor superfamily member 13B (TNFRSF13B; transmembrane activator and calcium modulator and cyclophilin ligand interactor; TACI) fused to a human immunoglobulin (Ig) fragment crystallizable (Fc) domain, with potential immunomodulating activity. Upon administration, telitacicept targets both tumor necrosis factor ligand superfamily member 13B (TNFSF13B; BAFF; B lymphocyte stimulator; BLyS) and tumor necrosis factor ligand superfamily member 13 (TNFSF13; a proliferation-inducing ligand; APRIL) and inhibits their interaction with their cell membrane receptors, including TACI, tumor necrosis factor receptor superfamily member 17 (TNFRSF17; B-cell maturation antigen; BCMA) and tumor necrosis factor receptor superfamily member 13C (TNFRSF13C; BAFF receptor; BAFF-R). This inhibits B-cell proliferation and maturation, thereby inhibiting B-cell mediated autoimmune responses. APRIL and BAFF, and their interactions with their receptors TACI, BCMA and BAFF-R, play important roles in in B-cell proliferation and survival.
telmisartan: A benzimidazole derivative and a non-peptide angiotensin II receptor antagonist with antihypertensive property. Telmisartan selectively antagonizes angiotensin II binding to the AT1 subtype receptor, located in vascular smooth muscle and adrenal gland. The antagonism results in vasodilation and inhibits the angiotensin II-mediated aldosterone production, which in turn leading to a decrease in sodium and water as well as an increase in potassium excretion leading to a subsequent reduction in blood pressure.
Telomelysin: (Other name for: suratadenoturev)
telomerase: 540-548 peptide vaccine: A recombinant peptide consisting of the amino acid residues 540 to 548 of the human telomerase reverse transcriptase (hTERT). Telomerase expression has been directly linked to tumor development; its catalytic subunit is expressed in the majority of human cancer cells, but infrequently in normal cells. Vaccination with telomerase:540-548 peptide may stimulate cytotoxic T cells to recognize and kill telomerase-expressing cells.
telotristat etiprate: An orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor prodrug, with potential antiserotonergic activity. Upon administration, telotristat etiprate is converted to its active moiety, telotristat (LP-778902), which binds to and blocks the activity of TPH. This may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells.
teloxantrone hydrochoride: The hydrochloride salt of an anthrapyrazole antineoplastic antibiotic. Teloxantrone intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis.
temanogrel hydrochloride: The hydrochloride salt form of temanogrel, an orally bioavailable, selective inverse agonist of 5-hydroxytryptamine receptor 2A (5-HT2A), with potential anti-thrombotic and vasodilating activities. Upon oral administration, temanogrel targets, binds to and inhibits 5-HT2A expressed on platelet surfaces and in smooth muscle cells, thereby inhibiting 5-HT-mediated platelet aggregation and vasoconstriction. This may attenuate platelet aggregation and vasoconstriction, and improve blood flow.
Temferon: (Other name for: autologous CD34+-enriched HSPCs transduced with VSV-G encoding IFN-a2)
Temodar: (Other name for: temozolomide)
temoporfin: A synthetic light-activated chlorin with photodynamic activity. Upon systemic administration, temoporfin distributes throughout the body and is taken up by tumor cells. Upon stimulation of temoporfin by non-thermal laser light (at 652 nm), and in the presence of oxygen, this agent produces highly reactive short-lived singlet oxygen and other reactive oxygen radicals, resulting in local damage to tumor cells. This may kill tumor cells and may reduce the tumor size.
temozolomide: A triazene analog of dacarbazine with antineoplastic activity. As a cytotoxic alkylating agent, temozolomide is converted at physiologic pH to the short-lived active compound, monomethyl triazeno imidazole carboxamide (MTIC). The cytotoxicity of MTIC is due primarily to methylation of DNA at the O6 and N7 positions of guanine, resulting in inhibition of DNA replication. Unlike dacarbazine, which is metabolized to MITC only in the liver, temozolomide is metabolized to MITC at all sites. Temozolomide is administered orally and penetrates well into the central nervous system.
Tempol: (Other name for: topical piperidine nitroxide MTS-01)
tempol-containing MBM-02: An orally bioavailable gelatin capsule-based formulation containing tempol, a hydrophilic piperidine nitroxide, with potential chemo/radioprotective and antioxidant activities. Upon oral administration of MBM-02, tempol, being a free radical compound, may be able to protect cells against the damaging effects of reactive oxygen species (ROS), upon exposure to ionizing radiation and oxidative stress. MBM-02 may selectively protect normal tissue from chemotherapy- and radiation-induced toxicities. Tempol is in its protective form in oxygenated cells and is in its unprotective form in the hypoxic tumor microenvironment (TME).
Tempostatin: (Other name for: halofuginone hydrobromide)
Temsirolimus: An ester analog of rapamycin. Temsirolimus binds to and inhibits the mammalian target of rapamycin (mTOR), resulting in decreased expression of mRNAs necessary for cell cycle progression and arresting cells in the G1 phase of the cell cycle. mTOR is a serine/threonine kinase which plays a role in the PI3K/AKT pathway that is upregulated in some tumors.
tenalisib: An orally active, highly selective, small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, tenalisib inhibits the PI3K delta and gamma isoforms and prevents the activation of the PI3K/AKT-mediated signaling pathway. This may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. In addition, this agent modulates inflammatory responses through various mechanisms, including the inhibition of both the release of reactive oxygen species (ROS) from neutrophils and tumor necrosis factor (TNF)-alpha activity. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and in inflammatory and autoimmune diseases. By selectively targeting these isoforms, PI3K signaling in normal, non-neoplastic cells is minimally impacted or not affected at all, which minimizes the side effect profile for this agent.
tenifatecan: A lipophilic preparation of 7-ethyl-10-hydroxycamptothecin (SN-38) with potential antineoplastic activity. Tenifatecan is an oil-in-water emulsion of tocopherol covalently linked, via a succinate linker, to SN-38, an active metabolite of the camptothecin derivative irinotecan. After the succinate linker is hydrolyzed in vivo, the active moiety SN-38 is released and selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks and inducing lethal double-stranded DNA breaks; DNA replication is inhibited and apoptosis is triggered. This agent may provide greater delivery and exposure of SN-38 to the tumor than can be achieved with irinotecan.
teniposide: A semisynthetic derivative of podophyllotoxin with antineoplastic activity. Teniposide forms a ternary complex with the enzyme topoisomerase II and DNA, resulting in dose-dependent single- and double-stranded breaks in DNA, DNA: protein cross-links, inhibition of DNA strand religation, and cytotoxicity. This agent acts in the late S or early G phase of the cell cycle.
tenofovir: A nucleoside reverse transcriptase inhibitor analog of adenosine.
tenofovir alafenamide: A lipophilic phosphonamidate prodrug of tenofovir, a synthetic antiviral acyclic nucleotide analog of adenosine 5-monophosphate and a nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity against hepatitis B virus (HBV) and potentially against human immunodeficiency virus (HIV). Upon oral administration, tenofovir alafenamide is taken up by hepatocytes through passive diffusion and through the hepatic uptake transporters organic anion transporting polypeptides 1B1 (OATP1B1) and 1B3 (OATP1B3). Inside the hepatocytes, tenofovir alafenamide is hydrolyzed and converted to tenofovir by carboxylesterase 1 (CES1). Intracellular tenofovir is phosphorylated by cellular kinases to its pharmacologically active form, tenofovir diphosphate. Tenofovir diphosphate is incorporated into viral DNA instead of the natural substrate deoxyadenosine 5-triphosphate, and inhibits HBV reverse transcriptase, resulting in DNA chain-termination and inhibition of HBV replication. In addition, tenofovir diphosphate is incorporated into HIV DNA instead of the natural substrate deoxyadenosine 5-triphosphate, thereby inhibiting HIV-1 reverse transcriptase (RT) and resulting in DNA chain termination and impairment of HIV replication.
tenofovir disoproxil fumarate: A pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.
Tepadina: (Other name for: thiotepa)
Tepmetko: (Other name for: tepotinib hydrochloride)
tepotinib: An orally bioavailable inhibitor of MET tyrosine kinase with potential antineoplastic activity. Tepotinib selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase. The receptor tyrosine kinase MET (also known as hepatocyte growth factor receptor or HGFR), is the product of the proto-oncogene c-Met and is overexpressed or mutated in many tumor cell types; this protein plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.
tepotinib hydrochloride: The hydrochloride salt form of tepotinib, an orally bioavailable inhibitor of MET tyrosine kinase with potential antineoplastic activity. Upon oral administration, tepotinib selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase. The receptor tyrosine kinase MET (also known as hepatocyte growth factor receptor or HGFR), is the product of the proto-oncogene c-Met and is overexpressed or mutated in many tumor cell types; this protein plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.
teprotumumab: A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor-1 receptor (IGF-1R) with potential antineoplastic activity. Teprotumumab binds to membrane-bound IGF-1R, preventing the binding of the natural ligand IGF-1 and the activation of PI3K/AKT signal transduction; downregulation of the PI3K/AKT survival pathway may result in the induction of apoptosis and decreased cellular proliferation. The activation of IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been implicated in tumorigenesis and metastasis.
Tepylute: (Other name for: thiotepa)
terameprocol: A synthetic tetra-methylated derivative of nordihydroguaiaretic acid (NDGA) and transcriptional inhibitor with potential antiviral, antiangiogenic, and antineoplastic activities. Terameprocol competes with the transcription factor Sp1 for specific Sp1 DNA binding domains within gene promoter regions during DNA synthesis. In virally-infected cells, blocking of the Sp1 binding site suppresses Sp1-regulated viral promoter activity and gene expression, thereby inhibiting viral transcription and replication. In tumor cells, blockage of Sp1 binding sites by this agent interferes with the transcription of the Sp1-dependant genes cyclin-dependant kinase (Cdc2), survivin, and vascular endothelial growth factor (VEGF), which are overexpressed in a variety of cancers. By suppressing Sp1-regulated transcription of these genes, terameprocol may reduce tumor angiogenesis and tumor cell proliferation and induce tumor cell apoptosis.
terephthalamidine: A derivative of the phthalanilide compounds. Terephthalamidine belongs to a family of compounds which appear to reversibly bind to the minor groove of the DNA double helix but not intercalate DNA. This agent also has been suggested to form ionic complexes with many biological components in vitro, including nucleic acids, proteins and lipids.
terlipressin: A synthetic triglycyllysine derivative of vasopressin with vasoconstrictive, antihemorrhagic, and antidiuretic properties. Upon intravenous administration, terlipressin, an inactive prodrug, is biotransformed to its active moiety, lysine vasopressin (LVP), a nonselective vasopressin analogue with affinity for vasopressin receptors V1 (V1a), V2 and V3 (V1b). As a V1 agonist, terlipressin increases systemic vascular resistance, particularly in the splanchnic area, resulting in a decrease of portal pressure. V1 binding also promotes platelet aggregation and glycogenolysis, while V3 binding induces adrenocorticotropic hormone (ACTH) secretion. Compared to vasopressin, terlipressin has a minimal effect on V2 receptors, which are responsible for promotion of water reabsorption in the collecting ducts of the kidney via stimulation of cyclic AMP production.
teroxirone: A triazene triepoxide with antineoplastic activity. Teroxine alkylates and cross-links DNA, thereby inhibiting DNA replication.
tersolisib: An orally bioavailable, brain penetrative, selective inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (phosphoinositide 3-kinase alpha; PIK3CA; PI3K p110alpha) mutant H1047X, with potential antineoplastic activity. Upon oral administration, tersolisib selectively targets and allosterically binds to the PIK3CA mutated form PIK3CA H1047X, thereby preventing the activity of the H1047X mutant. This prevents PIK3CA H1047X-mediated activation of the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA H1047X mutant-expressing tumor cells. By specifically targeting the PIK3CA H1047X mutation, tersolisib may be more efficacious and less toxic than other PI3K-alpha inhibitors that are not mutant specific. Dysregulation of the PI3K/Akt/mTOR pathway is often found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to chemo- and radio-therapy. PIK3CA, one of the most frequently mutated oncogenes, encodes the p110-alpha catalytic subunit of the class I PI3K. Tersolisib is able to penetrate the blood-brain-barrier (BBB).
tertomotide: A synthetic peptide vaccine containing a 16-amino-acid human telomerase reverse transcriptase peptide(hTERT: 611-626) with potential antineoplastic activity. Vaccination with telomerase peptide vaccine GV1001, which binds multiple HLA class II molecules and harbors putative HLA class I epitopes, may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against telomerase-expressing tumor cells. Telomerase, a reverse transcriptase normally repressed in healthy cells, is overexpressed in most tumor cell types and plays a key role in cellular proliferation.
tesetaxel: A semi-synthetic, orally bioavailable taxane derivative with potential antineoplastic and antiangiogenic properties. Tesetaxel binds to and stabilizes tubulin, promoting microtubule assembly and thereby preventing microtubule depolymerization. This may lead to cell cycle arrest and an inhibition of cell proliferation. This agent may also inhibit pro-angiogenic factors such as vascular endothelial growth factor (VEGF). As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors.
tesevatinib: An orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Tesevatinib binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression.
tesidolumab: A human immunoglobulin G1 (IgG1) monoclonal antibody directed against the complement pathway protein C5, with complement pathway inhibitory activity and potential immunomodulating activity. Upon administration, tesidolumab targets and binds to C5, thereby preventing both C5 convertase-mediated cleavage of C5 and the formation of C5a and C5b. This inhibits C5-mediated signal transduction, the formation of the membrane attack complex (MAC) and the activation of the terminal complement pathway, and results in the prevention and/or inhibition of both complement-mediated inflammation and cell destruction. C5 plays a key role in the activation of the complement cascade.
Teslac: (Other name for: testolactone)
tesnatilimab: A recombinant human immunoglobulin G4 (IgG4) monoclonal antibody against the immune activating receptor natural-killer group 2, member D receptor protein (NKG2D or KLRK1), with potential immunomodulating and anti-inflammatory activities. Upon administration, tesnatilimab targets and binds to NKG2D expressed on human natural killer (NK) and certain T lymphocytes, and blocks the activation of NKG2D. This may inhibit both the cytotoxic activities of lymphocytes and the production of pro-inflammatory cytokines. NKG2D, a dimeric, type II transmembrane protein expressed on human NK and certain T cells, and its ligands play important roles in some inflammatory and autoimmune conditions.
Testate: (Other name for: testosterone enanthate)
Testoderm: (Other name for: therapeutic testosterone)
testolactone: A progesterone derivative with antineoplastic activity. Testolactone inhibits steroid aromatase, thereby preventing the formation of estrogen from adrenal androstenedione and reducing endogenous estrogen levels.
Testolin: (Other name for: therapeutic testosterone)
Testolone: (Other name for: vosilasarm)
testosterone cypionate: An eight-carbon ester form of testosterone. The number of ester carbon atoms correlate with the half-life of the prodrug. Testosterone inhibits gonadotropin secretion from the pituitary gland and ablates estrogen production in the ovaries, thereby decreasing endogenous estrogen levels. In addition, this agent promotes the maintenance of male sex characteristics and is indicated for testosterone replacement in hypogonadal males.
testosterone enanthate: A long-acting intramuscular form of the androgen testosterone. Testosterone inhibits gonadotropin secretion from the pituitary gland and ablates estrogen production in the ovaries, thereby decreasing endogenous estrogen levels. In addition, this agent promotes the maintenance of male sex characteristics and is indicated for testosterone replacement in hypogonadal males, delayed puberty, and metastatic mammary cancer.
testosterone gel: A topical gel preparation of synthetic testosterone. In vivo, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes, resulting in an increase in protein anabolism, a decrease in amino acid catabolism, and retention of nitrogen, potassium, and phosphorus; DHT binds with higher affinity to nuclear androgen receptors than testosterone. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Testosterone and DHT promote the development and maintenance of male sex characteristics related to the internal and external genitalia, skeletal muscle, and hair follicles; estradiol promotes epiphyseal maturation and bone mineralization.
testosterone nasal gel: A nasal gel containing the human androgen testosterone that is used as a replacement agent for low or missing endogenous testosterone caused by various conditions. Upon intranasal administration of testosterone nasal gel using a pump, testosterone is taken up systemically and is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. Testosterone and DHT promote the growth, development and maintenance of male sex organs and the maintenance of secondary sex characteristics. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue.
testosterone undecanoate: The undecanoate ester form of the androgen testosterone, with gonadotropin-secretory inhibiting and hormone replacement activity. As testosterone inhibits the secretion of gonadotropins from the pituitary gland, administration of testosterone decreases the secretion of luteinizing hormone (LH). By inhibiting LH secretion, the growth of Leydig cells, which are normally stimulated by LH to produce testosterone, may be suppressed. In addition, this agent promotes the maintenance of male sex characteristics and can be used for testosterone replacement in hypogonadal males.
testosterone vaginal cream: A topical cream containing a synthetic form of the endogenous androgenic steroid testosterone. Upon vaginal application, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. DHT binds with higher affinity to androgen receptors than testosterone, activating gene expression more efficiently. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Topical application of testosterone may improve symptoms of vaginal dryness.
Testostroval: (Other name for: therapeutic testosterone)
Testostroval-PA: (Other name for: therapeutic testosterone)
Testred: (Other name for: methyltestosterone)
Testro AQ: (Other name for: therapeutic testosterone)
tetanus peptide melanoma vaccine: A vaccine consisting of peptides derived from melanoma-associated antigens and a modified T-cell epitope derived from tetanus toxoid. Vaccination with this agent may stimulate a host cytotoxic and helper T-cell response against tumor cells expressing melanoma-associated antigens, resulting in decreased tumor growth.
tetanus toxoid: A solution of formaldehyde-deactivated toxin isolated from the bacterium Clostridium tetani. Tetanus toxoid stimulates the production of antitoxin antibodies. This agent may be used as an adjuvant in cancer vaccines.
tetanus toxoid helper peptide: Obtained by genetic engineering from the bacterial Clostridium tetani toxoid, tetanus toxoid helper peptide QYIKANSKFIGITEL (amino acids 830-844) binds to class II MHC molecules as a nonspecific vaccine helper epitope (adjuvant) and induces an increased (and long term) immune response by increasing the helper T-cell response.
tetanus-CMV fusion peptide vaccine: A vaccine containing an inactivated epitope of tetanus toxin fused to a cytomegalovirus (CMV) peptide epitope, with potential anti-viral and immunomodulating activities. Upon administration, tetanus-CMV fusion peptide may stimulate a cytotoxic T-lymphocyte (CTL) response against CMV in the CMV-infected host. Tetanus toxin contains universal T cell helper epitopes.
TetMYB vaccine: A therapeutic engineered DNA vaccine composed of DNA sequences encoding for one or more tetanus toxoid peptides and the oncoprotein MYB, with potential immunostimulatory and antineoplastic activities. Upon intradermal administration, TetMYB is taken up and processed by dendritic cells (DCs), which present the processed antigen to the immune system. This activates cytotoxic T lymphocytes (CTLs) and causes a CTL-mediated immune response against MYB-expressing tumor cells. MYB, an oncoprotein and transcription factor, is overexpressed in a variety of cancer types and is essential for tumor cell growth, inhibition of differentiation, and protection from apoptosis. Its expression is correlated with lower T-cell infiltration and poorer prognosis. As MYB is only weakly immunogenic, the tetanus toxoid peptides enhance the T-cell mediated immune responses against the MYB-expressing tumor cells.
tetracycline antibiotic: Any of a group of broad spectrum naphthacene antibiotics isolated from various species of Streptomyces or produced semisynthetically. In bacteria, tetracycline antibiotics block binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis.
tetracycline hydrochloride: The hydrochloride salt of tetracycline, a broad-spectrum naphthacene antibiotic produced semisynthetically from chlortetracycline, an antibiotic isolated from the bacterium Streptomyces aureofaciens. In bacteria, tetracycline blocks binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis and bacterial cell growth. Because naturally fluorescing tetracycline binds to newly formed bone at the bone/osteoid interface, tetracycline-labeling of bone and fluorescence microscopy may be used to perform bone histomorphometry.
Tetracyn: (Other name for: tetracycline hydrochloride)
tetradecanoylphorbol acetate: A phorbol ester with potential antineoplastic effects. Tetradecanoylphorbol acetate (TPA) induces maturation and differentiation of hematopoietic cell lines, including leukemic cells. This agent may induce gene expression and protein kinase C (PKC) activity. In addition to potential antineoplastic effects, TPA may exhibit tumor promoting activity.
tetrahydrobiopterin: A cofactor that is essential for the activity of aromatic amino acid hydroxylases. Tetrahydrobiopterin degrades phenylalanine, and facilitates the biosynthesis of several neurotransmitters and the production of nitric oxide.
tetrahydrouridine: A synthetic pyrimidine nucleoside analogue with biomodulating activity. Tetrahydrouridine increases the efficacy of the radiosensitizer cytochlor (5-chloro-2'-deoxycytidine) by inhibiting the enzyme deoxycytidine monophosphate (dCMP) deaminase and preventing the premature deamination of the cytochlor metabolite 5-chloro-2'-deoxycytidine monophosphate (CldCMP) to 5-chloro-2'-deoxyuridine monophosphate (CldUMP); in turn, this increases tumor concentrations of CldUMP which is then further anabolized and incorporated selectively into tumor DNA as CldU (5-chloro-2'-deoxyuridine).
tetraphenyl chlorin disulfonate: A meso-tetraphenylchlorin substituted by two adjacent sulfonated groups with potential photosensitizing activity. Upon administration, tetraphenyl chlorin disulfonate incorporates into the cell’s endosome and lysosome membranes. Subsequently, cytotoxic agents are administered and accumulate in endosomal and lysosomal compartments; upon local activation by light, tetraphenyl chlorin disulfonate produces reactive oxygen species (ROS), such as singlet oxygen, damaging endo/lysosomal membranes and accumulated cytotoxic agents are released into the tumor cell cytosol. This photochemical internalization (PCI) method can enhance the efficacy and selectivity of cytotoxic agents.
tetravalent RNA-lipoplex cancer vaccine BNT111: A RNA-lipoplex (RNA-LIP)-based cancer vaccine containing four naked ribonucleic acid (RNA)-drug products (DPs) RBL001.1, RBL002.2, RBL003.1, and RBL004.1 encoding the four melanoma-associated antigens (MAAs), the cancer-testis antigen NY-ESO-1, the human melanoma-associated antigen A3 (MAGE-A3), tyrosinase, and putative tyrosine-protein phosphatase (TPTE), encapsulated in liposomes, with potential antineoplastic activity. Upon intravenous administration of the tetravalent RNA-lipoplex cancer vaccine BNT111, the liposomes protect the RNA from degradation in the bloodstream, travel to the spleen and are taken up by antigen-presenting cells (APCs). The RNA is translocated to the cytoplasm and translated into the four tumor-associated proteins. The expressed proteins are processed and the human leukocyte antigen (HLA)-peptide complexes are presented to the immune system. This results in the production of various pro-inflammatory cytokines and induces antigen-specific CD8+ and CD4+ T-cell responses against the four selected MAAs NY-ESO-1, MAGE-A3, tyrosinase, and TPTE.
tetrodotoxin: A neurotoxin with potential analgesic activity. Tetrodotoxin binds to the pores of fast voltage-gated fast sodium channels in nerve cell membranes, inhibiting nerve action potentials and blocking nerve transmission. Although found in various species of fish (such as the pufferfish), newts, frogs, flatworms, and crabs, tetrodotoxin, for which there is no known antidote, is actually produced by bacteria such as Vibrio alginolyticus, Pseudoalteromonas tetraodonis, and other vibrio and pseudomonas bacterial species.
teverelix: A synthetic decapeptide and antagonist of the naturally occurring gonadotropin-releasing hormone (GnRH), with potential hormone production inhibitory and antineoplastic activities. Upon administration, teverelix directly competes with GnRH for receptor binding in the anterior pituitary gland, thereby inhibiting GnRH receptor signaling. This inhibits the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. In females, this prevents the production of estrogen by the ovaries and may relieve symptoms from sex-hormone dependent diseases.
Tevimbra: (Other name for: tislelizumab-jsgr)
tezacitabine: A synthetic purine nucleoside analogue with potential antineoplastic activity. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types.
TGF-beta receptor 1 inhibitor GFH018: An orally bioavailable inhibitor of transforming growth factor-beta receptor 1 (TGFbR1), with potential antineoplastic activity. Upon oral administration, TGFbR1 inhibitor GFH018 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFbR1-dependent proliferation of cancer cells. The TGFb signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME.
TGF-beta receptor 1 kinase inhibitor SH3051: An orally bioavailable, small molecule inhibitor of the serine/threonine kinase transforming growth factor-beta (TGF-beta) receptor 1 (TGFbR1; activin receptor-like kinase 5; ALK5), with potential antineoplastic and immunomodulating activities. Upon administration, TGFbR1 inhibitor SH3051 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFbR1-dependent proliferation of tumor cells. The TGF-beta signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME and cancer cell progression.
TGF-beta receptor 1 kinase inhibitor YL-13027: An orally bioavailable inhibitor of the serine/threonine kinase transforming growth factor-beta receptor 1 (TGFbR1; activin receptor-like kinase 5; ALK5), with potential antineoplastic and immunomodulating activities. Upon administration, TGF-betaR1 inhibitor YL-13027 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFbR1-dependent proliferation of cancer cells. The TGFb signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME and cancer cell progression.
TGF-beta-15 peptide vaccine: A vaccine composed of the transforming growth factor-beta (TGF-beta; TGFb)-derived peptide TGF-beta-15 combined with the immunoadjuvant montanide ISA-51, with potential immunomodulating and antineoplastic activities. Upon administration, TGF-beta-15 peptide vaccine may activate TGF-beta-specific CD4+ and CD8+ T cells and stimulate the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against TGF-beta-expressing immunosuppressive cells in the tumor microenvironment (TME), including tumor-associated macrophages (TAMs), myeloid-derived suppressor cells (MDSCs), tolerogenic dendritic cells (DCs), regulatory T cells (Tregs), and cancer-associated fibroblasts (CAFs). This may restore the anti-tumor immune response. TGF-beta, dysregulated in many types of cancer, plays a key role in immunosuppression in the TME, enhances tumor cell proliferation, and promotes cancer progression.
TGF-beta-resistant LMP-specific cytotoxic T-lymphocytes: A preparation of transforming growth factor-beta (TGF-beta)-resistant cytotoxic T-lymphocytes (CTL) reactive to Epstein-Barr virus (EBV) latent membrane proteins 1 and 2 (LMP 1 and 2) with potential antineoplastic activity. T lymphocytes are transduced with a retroviral vector expressing the dominant-negative mutant type II TGF-beta receptor, which blocks signaling by all three TGF-beta isoforms. These TGF-beta-resistant T-lymphocytes are exposed ex-vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP; subsequent exposure to LMP1- or LMP2-expressing lymphoblastoid cell lines is used to expand the CTL. Administered to patients with EBV-positive tumors, TGF-beta-resistant LMP-specific CTL target LMP-positive cells, which may result in a specific CTL response, followed by cell lysis and inhibition of tumor cell proliferation. Tumor-expressed TGF-beta inhibits T lymphocyte activation and expansion.
TGF-beta2 antisense oligonucleotide TASO-001: A transforming growth factor (TGF)-beta2 specific antisense oligodeoxynucleotide (ASO), with potential antineoplastic activity. Upon administration, TGF-beta2 ASO TASO-001 binds to TGF-beta2 mRNA causing inhibition of protein translation. This decreases TGF-beta2 levels, which may result in the inhibition of tumor cell growth and migration, and tumor angiogenesis. TGF-beta2, a cytokine overexpressed in various malignancies, plays an important role in promoting the growth, progression, and migration of tumor cells.
TGFa-PE38 immunotoxin: A recombinant, chimeric toxin composed of human transforming growth factor alpha (TGF-alpha) fused to a fragment of Pseudomonas exotoxin (PE38) without its cell-binding domain. The TGF-alpha moiety of the agent attaches to tumor cells expressing the epithelial growth factor receptor (EGFR); the exotoxin induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis.
TGFbDNRII-transduced autologous tumor-infiltrating lymphocytes: A preparation of tumor infiltrating lymphocytes (TILs) that are transduced with a retroviral vector encoding a gene for a dominant-negative form of the transforming growth factor beta (TGFb) receptor, TGFbDNRII, with potential immunomodulating activity. Upon administration, the TGFbDNRII-transduced autologous TILs recognize and kill tumor cells. The expression of TGFbDNRII allows for the TILs to be resistant to TGF-b-mediated inhibition of T cell proliferation and activation, which allows optimal TIL activity. The immunosuppressant TGF-b is produced by tumor cells and plays a key role in the repression of the immune system.
TGFbeta inhibitor LY3200882: An orally bioavailable agent that targets transforming growth factor-beta (TGFb), with potential antineoplastic activity. Upon administration, LY3200882 specifically targets and binds to TGFb, which prevents both the binding of TGFb to its receptor TGFbR and TGFb-mediated signal transduction. This may lead to a reduction in TGFb-dependent proliferation of cancer cells. The TGFb signaling pathway is often deregulated in tumors, and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, angiogenesis, and various immune responses.
TGFbeta receptor ectodomain-IgG Fc fusion protein BMS-986416: A fusion protein composed of the ectodomain of the transforming growth factor (TGF) beta (TGF-beta; TGFb) receptor fused to the human immunoglobulin G (IgG) Fc domain, with potential antineoplastic, immunomodulating and anti-fibrotic activities. Upon administration of the TGFb receptor ectodomain-IgG Fc fusion protein BMS-986416, the fusion protein specifically and selectively targets, binds to and neutralizes the TGF ligands TGF-beta isoform 1 (TGFb1) and 3 (TGFb3). This prevents TGF ligands from binding to TGF receptors and prevents TGFb-mediated signaling. This abrogates TGFb1/3-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFb-dependent proliferation of cancer cells. By preventing TGFb1/3-mediated signaling, BMS-986416 also prevents bone marrow fibrosis and promotes the proliferation of normal hematopoietic progenitors. TGFb, overproduced in myelodysplastic syndrome (MDS) and in many other types of cancer, plays a key role in immunosuppression in the TME, enhances tumor cell proliferation, and promotes cancer progression. The TGFb1 and TGFb3 isoforms are negative regulators of hematopoiesis that play key roles in the pathogenesis and progression of fibrotic diseases. By selectively targeting only specific isoforms of TGFb with minimal activity against TGFb2, BMS-986416 minimizes the potential for cardiotoxicity and promotion of metastasis. The TGFb2 isoform promotes hematopoiesis and plays a key role in normal cardiac function while the inhibition of the TGFb2 isoform promotes metastasis.
thalicarpine: A natural aporphine benzylisoquinoline vinca alkaloid with antineoplastic activity. Thalicarpine binds to and inhibits p-glycoprotein, the multidrug resistance efflux pump. Thalicarpine also induces single-strand breaks in DNA and arrests cancer cells at the G2/M and G1 phase of the cell cycle.
Thalidomide: A synthetic derivative of glutamic acid (alpha-phthalimido-glutarimide) with teratogenic, immunomodulatory, anti-inflammatory and anti-angiogenic properties. Thalidomide acts primarily by inhibiting both the production of tumor necrosis factor alpha (TNF-alpha) in stimulated peripheral monocytes and the activities of interleukins and interferons. This agent also inhibits polymorphonuclear chemotaxis and monocyte phagocytosis. In addition, thalidomide inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and basic fibroblast growth factor (bFGF), thereby inhibiting angiogenesis.
Thalomid: (Other name for: Thalidomide)
Theo-24: (Other name for: theophylline)
Theobid Duracap: (Other name for: theophylline)
Theochron: (Other name for: theophylline)
theophylline: A natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm.
Therapav: (Other name for: papaverine hydrochloride)
therapeutic allogeneic cytotoxic T lymphocytes: A population of cytotoxic T-lymphocytes (CTLs) that are therapeutically administered to a recipient individual who is genetically distinct from a donor of the same species.
therapeutic allogeneic lymphocytes: A population of lymphocytes therapeutically administered to a recipient individual who is genetically distinct from a donor of the same species.
therapeutic angiotensin-(1-7): A synthetic heptapeptide identical to endogenous angiotensin-(1-7) with vasodilator and antiproliferative activities. Therapeutic angiotensin 1-7 may inhibit cyclooxygenase 2 (COX-2) and the production of proinflammatory prostaglandins and may activate the angiotensin-(1-7) receptor Mas, resulting in diminished tumor cell proliferation. Activation of the angiotensin-(1-7) receptor Mas, a G-protein coupled, seven transmembrane protein, may down-regulate the phophorylation and activation of Erk1 and Erk2 in the Erk1/Erk2 Mapk signaling pathway. In the renin-angiotensin system, the vasodlilating activity of angiotensin- (1-7), hydrolysed from angiotensin II by the type I transmembrane metallopeptidase and carboxypeptidase angiotensin converting enzyme 2 (ACE2) in vivo, counteracts the vasoconstricting activity of angiotensin II.
therapeutic autologous dendritic cells: A population of a type of antigen-presenting cell (APC), the dendritic cell (DC), harvested from a patient and grown in vitro in the presence of tumor-associated antigens (TAAs) derived from the patient's tumor (a technique known as 'pulsing') and then injected back into the patient; autologous DCs so manipulated may stimulate a specific cell-mediated antitumoral cytotoxicity. DCs derived from a patient may also be fused with the patient's tumor cells in vitro to combine sustained tumor antigen expression with the antigen-presenting and immunostimulatory capacities of DCs; when injected back into the patient, these autologous DC-tumor cell hybrids (fusion cells) may stimulate an active antitumoral immune response.
therapeutic autologous lymphocytes: A population of lymphocytes isolated from an individual, altered in vitro, and returned to the same individual for therapeutic purposes.
therapeutic bacterial strain CJRB-101: A live bacterial strain, with potential immunostimulating and antineoplastic activities. Upon administration of the therapeutic bacterial strain CJRB-101, the bacteria activates M1 macrophage and induces repolarization of M2 macrophages. This increases C-X-C motif chemokine 9 (CXCL9) and 10 (CXCL10)-expressing M1 macrophages and induces a shift from M2 to M1 macrophage dominance in the tumor microenvironment (TME). This stimulates the recruitment of other immune cells, increases the population of antigen-presenting specialized dendritic cells (DCs) and activates cytotoxic CD8+ T cells in the TME. This may enhance anti-tumor immune responses, specifically a cytotoxic T-lymphocyte (CTL)-mediated killing of tumor cells, and may eradicate tumor cells.
therapeutic breast/ovarian/prostate cancer vaccine DPX-0907: A lipid-based multi-peptide cancer vaccine targeted against multiple cancers with immunopotentiating activity. Therapeutic breast/ovarian/prostate peptide cancer vaccine DPX-0907 is a lyophilized liposomal proprietary preparation comprised of 7 tumor-specific HLA-A2-restricted epitopes (TAAs): topoisomerase II alpha, B-cell receptor-associated protein 31 (CDM protein), TNF-alpha-converting enzyme (TACE/ADAM17), Abelson homolog 2 (Abl2), gamma catenin (Junction plakoglobin), epithelial discoidin domain receptor 1 (EDDR1) and integrin beta 8 subunit. Upon vaccination, the lyophilized antigen/adjuvant/liposome complex is re-suspended in Montanide 1SA51 VG to create a depot effect, thereby presenting the TAAs to the immune system for a prolonged period of time. This may stimulate a potent cytotoxic T-lymphocyte (CTL) immune response against cancer cells that express these 7 TAAs and share epitopes with the vaccine epitope peptides, resulting in tumor cell lysis. The 7 TAAs are overexpressed on the surface of breast/ovarian and prostate cancer cells and play an important role in tumor cell growth and survival.
therapeutic cancer vaccine ATP128: A self-adjuvanted chimeric recombinant protein vaccine, based on the self-adjuvanting KISIMA immunization platform, composed of three components: the 42 residue fragment Z12, a cell penetrating peptide (CPP) derived from the ZEBRA protein transduction domain, a toll-like receptor (TLR) peptide agonist as an adjuvant and a chimeric cargo, a multiple antigenic domain (MAD; MultiE), that contains an as of yet not disclosed amount of major histocompatibility class (MHC)-restricted peptides derived from as of yet undisclosed tumor-associated antigens (TAAs) that are specific for colorectal cancer (CRC) patients, with potential immunomodulating and antineoplastic activities. Upon administration of ATP128, the Z12 moiety targets, binds to and penetrates antigen-presenting cells (APCs), specifically dendritic cells (DCs) and promotes the loading of the epitopes into the DCs and transports antigenic cargoes into both endosomal and cytosolic compartments. Upon processing and antigen presentation by MHC II and I, the immune system is stimulated and activates specific CD4+ and CD8+ T-cells, respectively, against the multi-epitopes specific for the CRC cells, thereby killing the CRC cells.
therapeutic cancer vaccine ATP150: A self-adjuvanted chimeric recombinant protein priming vaccine, based on the self-adjuvanting KISIMA immunization platform, composed of three components: the 42 residue fragment Z12, a cell penetrating peptide (CPP) derived from the ZEBRA protein transduction domain, a toll-like receptor (TLR) peptide agonist as an adjuvant and a chimeric cargo, a multiple antigenic domain (MAD; MultiE), that contains an as of yet not disclosed amount of major histocompatibility class (MHC)-restricted peptides derived from as of yet undisclosed tumor-associated antigens (TAAs) that are specific for pancreatic cancer patients, with potential immunomodulating and antineoplastic activities. Upon administration of ATP150, the Z12 moiety targets, binds to and penetrates antigen-presenting cells (APCs), specifically dendritic cells (DCs) and promotes the loading of the epitopes into the DCs and transports antigenic cargoes into both endosomal and cytosolic compartments. Upon processing and antigen presentation by MHC II and I, the immune system is stimulated and activates specific CD4+ and CD8+ T cells, respectively, against the multi-epitopes specific for pancreatic adenocarcinoma cells, thereby killing the tumor cells.
therapeutic cancer vaccine ATP152: A self-adjuvanted chimeric recombinant protein priming vaccine, based on the self-adjuvanting KISIMA immunization platform, composed of three components: the 42 residue fragment Z12, a cell penetrating peptide (CPP) derived from the ZEBRA protein transduction domain, a toll-like receptor (TLR) peptide agonist as an adjuvant and a chimeric cargo, a multiple antigenic domain (MAD; MultiE), that contains an as of yet not disclosed amount of major histocompatibility class (MHC)-restricted peptides derived from as of yet undisclosed tumor-associated antigens (TAAs) that are specific for pancreatic cancer patients, with potential immunomodulating and antineoplastic activities. Upon administration of ATP152, the Z12 moiety targets, binds to and penetrates antigen-presenting cells (APCs), specifically dendritic cells (DCs) and promotes the loading of the epitopes into the DCs and transports antigenic cargoes into both endosomal and cytosolic compartments. Upon processing and antigen presentation by MHC II and I, the immune system is stimulated and activates specific CD4+ and CD8+ T cells, respectively, against the multi-epitopes specific for pancreatic adenocarcinoma cells, thereby killing the tumor cells.
therapeutic dendritic cells/cytokine-induced killer cells: A preparation of autologous dendritic cells (DC) mixed with cytokine-induced killer (CIK) cells (DC-CIK), with potential immunopotentiating and antineoplastic activities. DCs were obtained ex vivo by incubation of peripheral blood lymphocytes (PBLs) with granulocyte-macrophage colony-stimulating factor stimulating factor (GM-CSF or CSF2), tumor necrosis factor (TNF), and interleukin (IL)-24 and were sensitized with tumor-associated antigens (TAAs). Cytokine-induced killer (CIK) cells are immune effector cells with both T-cell and natural killer (NK) cell like phenotype. CIKs are non-major histocompatibility complex (MHC)-restricted, NK-like T-lymphocytes, which express both CD3, a T-cell surface marker, and CD56, a natural killer cell surface marker, and have been generated ex vivo by incubation of peripheral blood lymphocytes (PBLs) with anti-CD3 monoclonal antibody, IL-2, IL-1 alpha, and interferon gamma (IFN-gamma) and then expanded. Upon co-culture of DCs and CIKs, and administration of DC-CIK cells into the patient, the DCs are able to stimulate the immune response to exert a specific anti-tumor immune response, while the CIK cells exert direct oncolytic activity.
therapeutic effector T lymphocytes: A preparation of autologous or donor-derived T lymphocytes that is able to mount an antigen-specific immune response.
therapeutic epinephrine: The synthetic form of the naturally occurring sympathomimetic amine with vasoconstricting, intraocular pressure-reducing, and bronchodilating activities. By stimulating vascular alpha-adrenergic receptors, epinephrine causes vasoconstriction, thereby increasing vascular resistance and blood pressure. When administered in the conjunctiva, this agent binds to alpha-adrenergic receptors in the iris sphincter muscle, resulting in vasoconstriction, a decrease in the production of aqueous humor, and a lowering of intraocular pressure. Through its beta1 receptor-stimulating actions, epinephrine increases the force and rate of myocardial contraction and relaxes bronchial smooth muscle, resulting in bronchodilation.
therapeutic estetrol: A synthetic steroid similar or identical to endogenous estetrol, a short-acting estrogen with both agonistic and antagonistic estrogen receptor activity. Administered orally, therapeutic estetrol binds to the estrogen receptor and as a selective estrogen receptor modulator (SERM) exhibits estrogen agonism in certain tissues and estrogen antagonism in others. Displaying weak estrogen activity in the uterus, estetrol acts as an estrogen antagonist in breast tissue. Produced solely by the human fetal liver, endogenous estetrol is the primary estrogen metabolite of estrogen biosynthesis in the human fetal liver.
therapeutic estradiol: A synthetic form of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females, that may be used as hormone replacement therapy. Typically esterified, estradiol derivatives are formulated for oral, intravaginal, transdermal, or parenteral administration. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. Estradiol exhibits mild anabolic and metabolic properties, and increases blood coagulability. It may play a role in immune and inflammatory processes.
therapeutic ex vivo-expanded allogeneic gamma delta T cells: An off-the-shelf preparation of a subset of therapeutic, ex vivo-expanded, allogeneic T lymphocytes that express only gamma chain and delta chain T-cell receptors (TCRs), with potential immunomodulating and antineoplastic activities. Upon administration of the therapeutic ex vivo-expanded allogeneic gamma delta T cells, these cells secrete interferon-gamma (IFN-g) and exert direct killing of tumor cells. In addition, these cells activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against tumor cells. Gamma delta T lymphocytes play a key role in the activation of the immune system and do not require major histocompatibility complex (MHC)-mediated antigen presentation to exert their cytotoxic effect.
therapeutic ex-vivo-treated autologous central memory T cells: A preparation of autologous ex-vivo treated central memory T (Tcm) cells with potential immunostimulatory activity. Upon isolation and ex-vivo treatment through as an of yet not elucidated method, the therapeutic ex-vivo-treated autologous Tcm cells, upon reintroduction into the patient, can activate an antitumor immune response which may eradicate tumor cells.
therapeutic gamma delta T lymphocytes: A subset of therapeutic autologous T-lymphocytes that express a T-cell receptor (TCR) composed of one gamma chain and one delta chain, with potential immunomodulating and antineoplastic activities. Upon administration of the therapeutic gamma delta T-lymphocytes, these cells secrete interferon-gamma (IFN-g), and exert direct killing of tumor cells. In addition, these cells activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against tumor cells. Gamma delta T-lymphocytes play a key role in the activation of the immune system and do not require major histocompatibility complex (MHC)-mediated antigen presentation to exert their cytotoxic effect.
therapeutic hemin: A sterile, lyophilized powder of hemin, the Fe3+ oxidation product of heme (Fe2+), derived from processed red blood cells. Therapeutic hemin appears to inhibit delta-aminolevulinic acid (ALA) synthetase, a rate-limiting enzyme in the porphyrin/heme biosynthetic pathway, resulting in inhibition of the hepatic and/or marrow synthesis of porphyrin precursors. The mechanism by which therapeutic hematin produces symptomatic improvement in patients with acute episodes of the hepatic porphyrias has not been determined.
therapeutic human antithrombin-III: A form of the human glycoprotein antithrombin-III (AT-III), which is produced recombinantly or isolated from human plasma, with anticoagulant activity. Upon administration, antithrombin-III binds to and blocks thrombin activity, and prevents thrombus formation.
therapeutic hydrocortisone: A synthetic or semisynthetic analog of natural hydrocortisone hormone produced by the adrenal glands with primary glucocorticoid and minor mineralocorticoid effects. As a glucocorticoid receptor agonist, hydrocortisone promotes protein catabolism, gluconeogenesis, capillary wall stability, renal excretion of calcium, and suppresses immune and inflammatory responses.
therapeutic immune globulin: A preparation of plasma proteins derived from the pooled plasma of adult donors. Largely comprised of IgG antibodies, therapeutic immune globulin provides passive immunization by increasing the recipient's serum levels of circulating antibodies. IgG antibodies have multiple functions, including binding to and neutralizing bacterial toxins; opsonization of pathogens; activation of complement; and suppression of pathogenic cytokines and phagocytes through binding to CD5, interleukin-1a (IL-1a), interleukin 6 (IL-6), tumor necrosis factor-alpha (TNF-alpha), and T-cell receptors. Therapeutic immune globulin may diminish pathogenic mechanisms in some autoimmune diseases by binding to and inhibiting the activity of autoantibodies.
therapeutic insulin: A synthetic or animal-derived form of insulin used in the treatment of diabetes mellitus. Therapeutic insulin is formulated to be short-, intermediate- and long-acting in order to individualize an insulin regimen according to individual differences in glucose and insulin metabolism. Therapeutic insulin may be derived from porcine, bovine or recombinant sources. Endogenous human insulin, a pancreatic hormone composed of two polypeptide chains, is important for the normal metabolism of carbohydrates, proteins and fats and has anabolic effects on many types of tissues.
therapeutic invariant natural killer T cells: A preparation of natural killer T cells (NKTs) expressing an invariant (alpha, beta) T-cell receptor (iNKTs), with potential immunomodulating and antineoplastic activities. Upon infusion of the therapeutic iNKTs, these cells recognize CD1d-restricted lipid ligands, which are expressed on certain tumor cells, and secrete large amounts of various cytokines. This may activate the immune system against tumor cells. Additionally, iNKTs directly target and lyse tumor cells.
therapeutic liver cancer peptide vaccine IMA970A: An off-the-shelf hepatocellular cancer (HCC) multi-peptide-based therapeutic vaccine composed of sixteen peptides derived from tumor-associated antigens (TAAs) expressed by hepatic tumor cells, of which seven are restricted to human leukocyte antigen (HLA)-A2 (HLA-A*02), five to HLA-A*24 and four to HLA class II, with potential immunomodulating and antineoplastic activities. Upon intradermal administration of the therapeutic liver cancer peptide vaccine IMA970A, the liver-specific peptides in the vaccine activate the immune system to exert both CD4+ T-helper and CD8+ cytotoxic T-lymphocyte (CTL)-mediated immune responses against liver cancer cells.
therapeutic lotion: A moisturizing skincare formulation used for various skin conditions including dry skin conditions associated with eczema, psoriasis, chapped or chafed skin.
therapeutic melatonin: A therapeutic chemically synthesized form of the pineal indole melatonin with antioxidant properties. The pineal synthesis and secretion of melatonin, a serotonin-derived neurohormone, is dependent on beta-adrenergic receptor function. Melatonin is involved in numerous biological functions including circadian rhythm, sleep, the stress response, aging, and immunity.
therapeutic progesterone: The therapeutic form of the naturally occurring hormone progesterone. Progesterone binds to the progesterone receptor, resulting in dissociation of heat shock proteins, receptor phosphorylation, and transcription activation through direct or indirect interaction with transcription factors. This agent exerts inhibitory effects on estrogens by decreasing the number of estrogen receptors and increasing its metabolism to inactive metabolites. Progesterone induces secretory changes in the endometrium, decreases uterine contractility during pregnancy, and maintains pregnancy.
therapeutic prostate cancer peptide vaccine TENDU: A peptide cancer vaccine, based on the tetanus-epitope targeting (TET)-platform, composed of as of yet undisclosed tumor-associated antigens (TAAs) that are specific for prostate cancer and a tetanus-based vaccine adjuvant in the same molecule, with potential immunomodulating and antineoplastic activities. Upon administration, therapeutic prostate cancer peptide vaccine TENDU may stimulate a potent cytotoxic T-lymphocyte (CTL) immune response against prostate cancer cells that express these TAAs, resulting in tumor cell lysis. The tetanus peptide may enhance the anti-tumor immune response.
therapeutic testosterone: A synthetic form of the endogenous androgenic steroid testosterone. In vivo, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. DHT binds with higher affinity to androgen receptors than testosterone, activating gene expression more efficiently. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Testosterone and DHT promote the development and maintenance of male sex characteristics related to the internal and external genitalia, skeletal muscle, and hair follicles; estradiol promotes epiphyseal maturation and bone mineralization. Due to rapid metabolism by the liver, therapeutic testosterone is generally administered as an ester derivative.
therapeutic triiodothyronine: A therapeutic formulation of the primary physiologically active form of endogenous thyroid hormone. In vivo, triiodothyronine enters the nucleus and binds to nuclear thyroid hormone receptors that subsequently bind to thyroid response elements (TREs) located in target genes. Receptor binding by triiodothyronine in combination with recruited coactivators results in maximal transcriptional activation after binding to TREs; in general, binding of thyroid hormone receptor alone to TREs leads to repression of gene transcription.
therapeutic tumor infiltrating lymphocytes: A preparation of cells, consisting of autologous tumor infiltrating lymphocytes, that are manipulated in vitro and, upon administration in vivo, re-infiltrate the tumor to initiate tumor cell lysis. In vitro, therapeutic tumor-infiltrating lymphocytes (TILs) are isolated from tumor tissue and cultured with lymphokines such as interleukin-2; the therapeutic TILs are then infused into the patient, where, after re-infiltration of the tumor, they may induce lysis of tumor cells and tumor regression. The use of therapeutic TILs is considered a form of adoptive immunotherapy.
TheraSphere: (Other name for: yttrium Y 90 glass microspheres)
Thermazene: (Other name for: silver sulfadiazine)
ThermoDox: (Other name for: lyso-thermosensitive liposomal doxorubicin)
thermogenic regulator RZL-012: A synthetic small molecule thermogenic regulator, that may potentially be used for the treatment of Dercum's Disease lipomas. Although the exact mechanisms(s) through which this agent exerts its effects have yet to be fully elucidated, upon subcutaneous injection into lipomas, thermogenic regulator RZL-012 activates thermogenesis in subcutaneous fat, turning fat into heat. This may lead to fat cell death and the shrinkage of fat tissue.
thiabendazole: A benzimidazole derivative with anthelminthic property. Although the mechanism of action has not been fully elucidated, thiabendazole inhibits the helminth-specific mitochondrial enzyme fumarate reductase, thereby inhibiting the citric acid cycle, mitochondrial respiration and subsequent production of ATP, ultimately leading to helminth's death. In addition, it has been suggested that thiabendazole may lead to inhibition of microtubule polymerization by binding to beta-tubulin and has an overt ovicidal effect with regard to some trichostrongylids.
thiamine: A heat-labile and water-soluble essential vitamin, belonging to the vitamin B family, with antioxidant, erythropoietic, mood modulating, and glucose-regulating activities. Thiamine reacts with adenosine triphosphate (ATP) to form an active coenzyme, thiamine pyrophosphate. Thiamine pyrophosphate is necessary for the actions of pyruvate dehydrogenase and alpha-ketoglutarate in carbohydrate metabolism and for the actions of transketolase, an enzyme that plays an important role in the pentose phosphate pathway. Thiamine plays a key role in intracellular glucose metabolism and may inhibit the action of glucose and insulin on arterial smooth muscle cell proliferation. Thiamine may also protect against lead toxicity by inhibiting lead-induced lipid peroxidation.
thiarabine: A analog of antimetabolite cytarabine (ara-C), with potential antineoplastic activity. Upon administration, thiarabine (T-araC) is phosphorylated to the triphosphate form T-araCTP and competes with cytidine for incorporation into DNA. This results in an inhibition of DNA replication and RNA synthesis, chain termination and may eventually decrease tumor cell proliferation. Compared to ara-C, T-araC appears to have a longer half-life and has a higher efficacy.
Thibenzole: (Other name for: thiabendazole)
thioguanine: A synthetic guanosine analogue antimetabolite. Phosphorylated by hypoxanthine-guanine phosphoribosyltransferase, thioguanine incorporates into DNA and RNA, resulting in inhibition of DNA and RNA syntheses and cell death. This agent also inhibits glutamine-5-phosphoribosylpyrophosphate amidotransferase, thereby inhibiting purine synthesis.
thioredoxin-1 inhibitor PX-12: An orally bioavailable small molecule with potential antineoplastic activity. Thioredoxin-1 inhibitor PX-12 irreversibly binds to thioredoxin-1 (Trx-1) and inhibits its activity, which may result in growth inhibition and the induction of apoptosis. Overexpressed in many cancer cell types, the low molecular weight redox protein Trx-1 regulates transcription factor activity and inhibits apoptosis, promoting cell growth and survival; it also interacts with growth factors extracellularly to stimulate cell growth.
thioridazine hydrochloride: The hydrochloride salt form of thioridazine, a piperidine phenothiazine derivative and a dopamine antagonist with antipsychotic property. Thioridazine hydrochloride binds to mesolimbic postsynaptic dopamine receptor D2, thereby decreasing dopamine activity leading to decreased psychotic effects, such as hallucinations and delusions. In addition, this agent binds to serotonin 5-HT2 receptors, resulting in decreased serotonin activity.
thiostrepton: A naturally-occurring, sulfur-rich, cyclic oligopeptide antibiotic of the thiopeptide class, and an irreversible inhibitor of the mitochondrial thioredoxin-dependent peroxide reductase (peroxiredoxin-3; PRX3; antioxidant protein 1; AOP-1), with potential antineoplastic activity. Upon intrapleural administration, thiostrepton irreversibly binds to and inhibits the activity of PRX3. This inhibits the peroxidase activity of the thioredoxin reductase 2 (TXNRD2)-thioredoxin-2 (TRX2)-PRX3 antioxidant signaling network within the mitochondria, which may result in the accumulation of hydrogen peroxide and lead to tumor cell death. PRX3 is upregulated in cancer cells and plays an important role in the regulation of the oxidative stress pathways.
thiotepa: A polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity. Upon administration, thiotepa is converted into highly reactive ethylenimine groups, which covalently bind to nucleophilic groups in DNA and demonstrate a preference for the N7 position of guanine bases. This induces crosslinking of alkylated guanine bases in double-stranded DNA, interferes with both DNA replication and cell division, and results in both the induction of apoptosis and the inhibition of cell growth.
thioureidobutyronitrile: A water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity. Upon intravenous administration, thioureidobutyronitrile activates p53 which in turn induces the expressions of p21 and PUMA (p53 up-regulated modulator of apoptosis), thereby inhibiting cancer cell growth and causing tumor cell apoptosis. Thioureidobutyronitrile may be effective in drug-resistant cancers with mutated p53. p53 tumor suppressor, a transcription factor regulating the expression of many stress response genes and mediating various anti-proliferative processes, is often mutated in cancer cells.
THL-P: A proprietary, oral Chinese medicinal herb preparation with potential antioxidant, immunomodulating, and antineoplastic activities. THL-P (Tien-Hsien Liquid-P) contains fourteen Chinese medicinal herbs including: Cordyceps sinensis, Oldenlandia diffusa, Indigo pulverata levis, Polyporus umbellatus, Radix astragali, Panax ginseng, Solanum nigrum L., Pogostemon cablin, Atractylodis macrocephalae rhizoma, Trichosanthes radix, Clematis radix, Margarite, Ligustrum lucidum Ait and Glycyrrhiza radix. Administered as an oral liquid, THL-P may modulate the activity of natural killer (NK) cells, cytotoxic T-lymphocytes (CTLs), macrophages and polymorphonuclear leukocytes, and enhance the secretion of interleukins (ILs) and interferon-gamma (IFN-gamma). This agent may also induce G2/M cell cycle arrest and downregulate several important oncogenic signaling pathways.
Thorazine: (Other name for: chlorpromazine)
Thorazine: (Other name for: chlorpromazine)
thorium Th 227 anetumab corixetan: A radioimmunoconjugate consisting of anetumab, a human immunoglobulin G1 (IgG1) monoclonal antibody directed against the cell surface glycoprotein mesothelin, conjugated to the chelating agent corixetan, and labeled with the alpha-emitting radioisotope thorium Th 227, with potential antineoplastic activity. Upon administration of thorium Th 227 anetumab corixetan, the anetumab moiety binds to the tumor-associated antigen (TAA) mesothelin, delivering a cytotoxic dose of alpha radiation to cells expressing mesothelin.
thorium Th 227 anti-HER2 monoclonal antibody BAY2701439: A radioimmunoconjugate consisting of a monoclonal antibody targeting the tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2) and labeled with the alpha-emitting radioisotope thorium Th 227, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of BAY2701439 targets and specifically binds to HER2 on tumor cells, delivering a cytotoxic dose of alpha radiation to cells expressing HER2. HER2 is overexpressed in a variety of cancer cell types and is associated with increased tumor cell proliferation.
thorium Th 227 anti-PSMA monoclonal antibody BAY 2315497: A radioimmunoconjugate consisting of a monoclonal antibody targeting the tumor-associated antigen (TAA) human prostate-specific membrane antigen (PSMA) and labeled, via a 3-hydroxypyridin-2-one (3,2-HOPO) chelator, with the alpha-emitting radioisotope thorium Th 227, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of BAY 2315497 targets and specifically binds to PSMA on tumor cells, delivering a cytotoxic dose of alpha radiation to cells expressing PSMA. PSMA is overexpressed on the surface of metastatic and hormone-refractory prostate cancer cells.
threonine tyrosine kinase inhibitor CFI-402257: An orally bioavailable, selective inhibitor of the dual specificity protein kinase TTK (monopolar spindle 1 kinase, Mps1), with potential antineoplastic activity. Upon administration, luvixasertib selectively binds to and inhibits the activity of Mps1. This inactivates the spindle assembly checkpoint (SAC) and accelerates mitosis, which results in chromosomal misalignment and missegregation, and mitotic checkpoint complex destabilization. This induces cell death in Mps1-overexpressing cancer cells. Mps1, a tyrosine and serine/threonine kinase expressed in proliferating normal tissues, is essential for proper SAC functioning and chromosome alignment. Overexpressed in various human tumors, Mps1 plays a key role in uncontrolled tumor cell growth.
Thrombi-Gel: (Other name for: topical thrombin gel)
thrombomodulin alfa: A recombinant, soluble form of the human protein thrombomodulin, with potential anticoagulant activity. Upon administration, thrombomodulin binds to thrombin, which stimulates the activation of protein C. Activated protein C (APC) degrades factor Va and Factor VIIa in the presence of the cofactor protein S, inhibits thrombin formation, and prevents both thrombin-mediated coagulation and further clot formation.
thymalfasin: A synthetic analogue of thymosin-alpha-1, a 28-amino acid protein derived from the precursor protein prothymosin-alpha. Exhibiting a variety of immunoregulating properties, thymosin-alpha-1 induces differentiation of murine T-cell precursors and human thymocytes and the terminal differentiation of functionally immature cord blood lymphocytes and induces production of IL-2, high affinity IL-2 receptors, and B-cell growth factors by peripheral blood mononuclear cells. T-helper and cytotoxic/suppressor T cell populations are targets of thymosin activity. Thymosin-alpha-1 has been shown to increase the efficiency of antigen presentation by macrophages and to be an endogenous modulator of alpha-thrombin activity.
thyme and honey-based oral spray: An oral spray containing thyme and honey, with potential anti-inflammatory and anti-mucositis activities. Upon administration, the ingredients in this agent may prevent or decrease inflammation and bacterial infections of the oral mucosal membranes and may prevent or decrease radiation-induced oral mucositis. In addition, honey may have a protective and healing effect on the oral mucosa.
Thymectacin: (Other name for: brivudine phosphoramidate)
thymidine: A pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix.
thymidylate synthase inhibitor CX1106: A thymidylate synthase (TS) inhibitor with potential antineoplastic activity. Upon administration, TS inhibitor CX1106 binds to and inhibits TS. This reduces thymine nucleotide synthesis, inhibits DNA synthesis and cell division, causes DNA damage and leads to tumor cell apoptosis. TS catalyzes the conversion of deoxyuridine monophosphate (dUMP) to deoxythymidine monophosphate (dTMP), an essential precursor for DNA synthesis, and plays a key role in cell growth and division.
thymidylate synthase inhibitor DFP-11207: An orally available thymidylate synthase (TS) inhibitor with potential antineoplastic activity. Upon oral administration, DFP-11207 binds to and inhibits TS. This reduces thymine nucleotide synthesis, inhibits DNA synthesis and cell division, causes DNA damage and leads to tumor cell apoptosis. TS catalyzes the conversion of deoxyuridine monophosphate (dUMP) to deoxythymidine monophosphate (dTMP).
Thymitaq: (Other name for: nolatrexed dihydrochloride)
Thymoglobulin: (Other name for: anti-thymocyte globulin)
thymopentin: A synthetic pentapeptide which is the active site of the naturally occurring hormone thymopoietin with immunomodulating properties. Thymopentin enhances the production of thymic T cells and may help restore immunocompetence in immunosuppressed subjects. This agent also augments the effects of ionizing radiation by arresting cancer cells in the G2/M phase of the cell cycle.
Thyrogen: (Other name for: recombinant thyrotropin alfa)
thyrointegrin alphaVbeta3 antagonist fb-PMT: A fluorobenzyl polyethylene glycol (PEG) conjugated to tetraiodothyroacetic acid that targets the thyrointegrin alphaVbeta3, with potential antineoplastic activity. Upon administration, the thyrointegrin alphaVbeta3 antagonist fb-PMT targets and binds to alphaVbeta3 integrin. This results in the inhibition of angiogenesis and metastasis. The mechanism of actions (MOAs) through which fb-PMT exerts its actions may be more complex and may be through multiple signaling pathways. AlphaVbeta3 integrin, a cell adhesion and signaling receptor, is overexpressed on the surface of tumor vessel endothelial cells, some tumor cells, and a number of other cell types.
thyroxine: A hormone synthesized and secreted by the thyroid gland containing four iodine atoms and is converted to triiodothyronine (T3) in the body, influencing metabolism and organ function.
Thytropar: (Other name for: recombinant thyroid-stimulating hormone)
tiazofurin: A synthetic nucleoside analogue with antineoplastic activity. Tiazofurin (TR) is anabolized intracellularly to an analogue of NAD, tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH); IMPDH is the rate-limiting enzyme for de novo purine synthesis. Inhibition of IMPDH results in reduced levels of guanylates, resulting in the inhibition tumor cell growth in vitro and in vivo.
Tibetree: (Other name for: camphor/herbal formulation-based topical plaster)
tibolone: A synthetic anabolic steroid with estrogenic, androgenic and progestagenic activities. The 3alpha- and 3beta-hydroxy metabolites of tibilone activate estrogenic receptors (ERs) in bone and vaginal tissue leading to a decrease in bone turnover, and decreased vaginal dryness, respectively; derived from the 3beta-hydroxy metabolite, its delta4-isomer activates androgenic receptors (ARs) in the brain and liver and progestogenic receptors (PRs) in endometrial tissue, affecting sexual function, lipid metabolism, and endometrial function, respectively. In breast and endometrial tissue, tibolone metabolites inhibit sulfatase, preventing the conversion of circulating estrone sulfate and estradiol sulfate to estrone and estradiol, respectively; estrogen-mediated effects in the breast and uterus are thus reduced.
Tibsovo: (Other name for: ivosidenib)
TICE BCG: (Other name for: BCG vaccine)
TICE BCG solution: (Other name for: BCG solution)
tifcemalimab: A recombinant humanized immunoglobulin G4 kappa (IgG4k) monoclonal antibody directed against B- and T-lymphocyte attenuator (BTLA), with potential immunomodulating and antineoplastic activities. Upon intravenous infusion administration, tifcemalimab targets and binds to BTLA. This prevents BTLA-mediated inhibition of T-cell activation leading to antigen specific T-cell proliferation and activation of a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. BTLA, an immunoglobulin (Ig) receptor family member expressed on activated T and B lymphocytes, subsets of dendritic cells (DCs), macrophages, and nature killer (NK) cells, is an immune checkpoint involved in suppressing immune responses. It mediates inhibition of human tumor-specific CTLs upon engagement by tumor expressed herpesvirus-entry mediator (HVEM).
tigapotide: A synthetic 15-mer peptide corresponding to amino acids 31-45 of the 94-amino acid isoform of human prostate secretory protein (PSP-94) with potential anti-metastasis and anti-angiogenesis activities. Tigapotide may inhibit the secretion of the metastasis-related protein matrix metalloproteinase-9 (MMP-9) and its potential binding to its cell surface receptor CD44; may interfere with the vascular endothelial growth factor (VEGF) signaling pathway, resulting in an anti-angiogenesis effect; and may reduce the levels of parathyroid hormone-related protein (PTHrP), decreasing plasma calcium levels. PSP-94, one of three predominant proteins found in seminal fluid, may be down-regulated in prostate cancer, representing a potential survival mechanism for prostate cancer cells. MMP-9 is implicated in the invasion and metastasis of cancer. PTHrP may be expressed by various tumor cell types, resulting in the hypercalcemia of malignancy.
tigatuzumab: A humanized agonistic monoclonal antibody directed against human tumor necrosis factor-related apoptosis-inducing ligand receptor 2 (TRAIL-R2) with potential antitumor activity. Mimicking the natural receptor ligand TRAIL, tigatuzumab binds to TRAIL-R2, activating signal transduction pathways that may result in tumor cell apoptosis and a reduction in tumor growth. A member of the tumor necrosis factor (TNF) receptor family, TRAIL-R2, also known as DR5 (death receptor 5), is expressed on the surfaces of many types of malignant cells.
tigecycline: A broad-spectrum glycylcycline antibiotic derived from tetracycline. Tigecycline binds to the 30S ribosomal subunit, thereby interfering with the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This prevents the incorporation of amino acid residues into the elongating peptide chain, inhibiting protein synthesis and eventually bacterial cell growth.
tigilanol tiglate: A short-chain diterpene ester isolated from the seed of Fontainea picrosperma, with potential antineoplastic activity. Upon intratumoral administration, tigilanol tiglate disrupts mitochondrial functioning and induces mitochondrial swelling, which leads to oncolysis of tumor cells that are in direct contact of the agent. In addition, tigilanol tiglate activates protein kinase C (PKC) signaling cascade, which leads to an acute inflammatory response. This results in hypoxia and activates innate immune cells including neutrophils and macrophages, thereby further killing tumor cells. The activation of the beta-II isoform of PKC (PKC beta II) also increases tumor vasculature permeability, which leads to the destruction of tumor vasculature.
TIGIT/PDL1 inhibitor AUR-106: An orally bioavailable small molecule inhibitor of the co-inhibitory molecule and immune checkpoint inhibitor T-cell immunoreceptor with immunoglobulin (Ig) and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT) and the immunosuppressive ligand programmed cell death-1 ligand 1 (PD-L1; PDL1; cluster of differentiation 274; CD274), with potential immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, TIGIT/PD-L1 inhibitor AUR-106 simultaneously targets, binds to and inhibits TIGIT and PD-L1, thereby inhibiting their downstream signaling pathways. Inhibition of TIGIT, which is expressed on various immune cells and particularly on tumor-infiltrating lymphocytes (TILs), prevents the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PRR2; PVRL2) and CD155 (poliovirus receptor; PVR; nectin-like protein 5; NECL-5). This enhances the interaction of CD112 and CD155 with the costimulatory receptor CD226 (DNAX Accessory molecule-1; DNAM-1), which is expressed on immune cells, such as natural killer (NK) cells and CD8+ T cells. This leads to CD226 dimerization and CD226-mediated signaling and activates the immune system to exert a T-cell-mediated immune response against cancer cells. Inhibition of PD-L1 prevents its binding to and activation of its receptor, programmed cell death 1 (PD-1; PDCD1; CD279; programmed death-1). This abrogates T-cell inhibition, activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which may lead to a reduction in tumor growth. TIGIT, a member of the Ig super family (IgSF) and an immune inhibitory receptor, plays a key role in the suppression of T-cell proliferation and activation; it is involved in tumor cell immune evasion. PD-L1 binding to PD-1 on activated T-cells inhibits the expansion and survival of CD8-positive T cells, suppresses the immune system and results in immune evasion.
TIL 1383I T cell receptor-transduced autologous T cells: Autologous peripheral blood lymphocytes-derived T cells transduced with a retroviral encoding TIL 1383I, a T cell receptor (TCR) specific for melanoma antigen tyrosinase, with potential immunostimulating and antineoplastic activity. After transduction, expansion in culture, and reintroduction into the patient, TIL 1383I TCR-transduced autologous T cells bind to tumor cells expressing tyrosinase, which may induce cytokine expression, activation and proliferation of T-cells, and a specific cytotoxic T-lymphocyte (CTL) response against tyrosinase-expressing tumor cells. TIL 1383I TCR originated from a melanoma patient’s CD4+ tumor-infiltrating lymphocytes and is reactive against a class I MHC (HLA-A2)-restricted epitope (368-376) of tyrosinase.
tilarginine: A pan-nitric oxide synthase (NOS) inhibitor, with potential immunomodulating and antineoplastic activities. Upon administration, tilarginine binds to and inhibits NOS, a free radical signaling molecule that promotes angiogenesis, metastasis, and immunosuppression in the tumor microenvironment (TME). Reduction in NOS activity may abrogate the immunosuppressive TME, enhance tumor antigen-specific immune response and inhibit tumor cell proliferation.
tildacerfont: An orally bioavailable, selective nonsteroidal antagonist of the corticotropin-releasing factor type-1 (CRF1; CRF-1) receptor, that can potentially be used to prevent excess androgen production in congenital adrenal hyperplasia (CAH). Upon oral administration, tildacerfon targets, binds to and inhibits the CRF1 receptor located in the pituitary gland. This reduces adrenocorticotropic hormone (ACTH) secretion and reduces the overproduction of adrenal androgens. CRF is a key regulator of the hypothalamic-pituitary-adrenal (HPA) axis and stimulates ACTH release from the anterior pituitary. CAH comprises a set of enzymatic defects in the cortisol synthetic pathway. A decrease in adrenal cortisol production impairs negative feedback on the HPA axis, which increases production of CRF and ACTH, the primary stimulus for cortisol and 19-carbon steroid production in the adrenal cortex.
tildrakizumab: A humanized monoclonal antibody directed against the p19 protein subunit of interleukin-23 (IL-23), with immunomodulating activity. Upon subcutaneous administration, tildrakizumab targets and binds to the p19 subunit of IL-23, thereby neutralizing IL-23 and preventing the binding of IL-23 to its receptor. This inhibits IL-23-mediated signaling and inhibits differentiation of CD4 positive T cells into Th1 and Th17 cells. This prevents Th1- and Th17-mediated responses and cytokine production. This may prevent or reduce symptoms and severity of graft versus host disease (GVHD). IL-23, a pro-inflammatory cytokine that play a key role in the regulation of the immune system, is upregulated in immune-mediated inflammatory disorders. Both Th1 and Th17 cells play a crucial role in GVHD.
tilsotolimod sodium: A proprietary synthetic oligonucleotide-based agonist of toll-like receptor 9 (TLR9), with potential immunostimulating activity. Upon administration, tilsotolimod sodium binds to and activates TLR9 expressed by plasmacytoid dendritic cells (pDCs) and B cells. This initiates immune signaling pathways, activates B cells and pDCs, and induces a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
tilvestamab: A humanized immunoglobulin (Ig) G1 monoclonal antibody directed against AXL receptor tyrosine kinase (AXL; UFO), with potential immunomodulating and antineoplastic activities. Upon administration, tilvestamab targets, binds to and inhibits the activity of AXL, which is expressed on the surfaces of a variety of cancer cell types. This prevents AXL-mediated signaling, and may inhibit tumor cell proliferation, migration and invasion. AXL, a member of the TAM (TYRO3, AXL and MER) family of receptor tyrosine kinases, is overexpressed by many tumor cell types, and plays a key role in tumor cell proliferation, survival, invasion and metastasis; its expression is associated with drug resistance, tumor immune evasion and poor prognosis.
timolol maleate: The maleate salt form of timolol, a propanolamine derivative and a non-selective beta-adrenergic antagonist with antihypertensive property. Timolol competitively binds to beta-1-adrenergic receptors in the heart and vascular smooth muscle and beta-2-receptors in the bronchial and vascular smooth muscle, resulting in a decrease in beta-adrenergic stimulation. Beta-1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta-2-blockade results in an increase in peripheral vascular resistance. The ultimate results include vasodilation, and negative chronotropic and inotropic effects. In addition, timolol reduces intra-ocular pressure possibly by decreasing aqueous humor production by reduction of blood flow to the ciliary processes and cAMP synthesis.
timolol maleate gel forming solution: A gel forming solution containing the maleate salt of timolol, a propanolamine derivative and a non-selective beta-adrenergic antagonist, with intraocular pressure-reducing activity. Although the precise mechanism of action of timolol's ocular hypotensive action is not clearly established at this time, studies suggest that it may be the result of decreased aqueous humor production (possibly by reduction of blood flow to the ciliary processes and cAMP synthesis) as well as a slight increase in outflow facility. Timolol gel-forming solution can potentially be used topically as well, in the prevention of the neoangiogenesis that may occur following pulsed dye laser treatment of port wine stains.
timonacic: A cyclic sulfur amino acid derivative with potential antineoplastic and antioxidant activities. Acting on cellular membranes of malignant cells through an unknown mechanism, timonacic may induce malignant cells to revert back to an untransformed state. This agent may also restore contact inhibition, a phenomenon characterized by the paracrine inhibition of mitosis following the formation of a critical cell mass, presumably the result of cell-to-cell signal transfer. Timonacic may also produce antioxidant effects secondary to its release of cysteine and restoration of glutathione concentrations.
Timoptic-XE: (Other name for: timolol maleate gel forming solution)
tin Sn 117m DTPA: A radioconjugate composed of the chelating agent and bone seeking agent diethylenetriaminepentaacetic acid (DTPA) complexed to the radionuclide tin (Sn) 117m (stannic, 4+), with potential use as a palliative agent for bone pain from bony metastases. Upon administration of Sn-117m-DTPA, the DTPA localizes to bones, thereby leading to the accumulation of the radioactive agent in bone. The radiation may destroy tumor cells in bone metastasis and may alleviate the pain.
Tindamax: (Other name for: tinidazole)
tinengotinib: An orally available small molecule inhibitor of Aurora kinases (AKs) A and B, Janus kinases (JAKs), fibroblast growth factor receptors (FGFRs) and vascular endothelial growth factor receptors (VEGFRs), with potential antineoplastic and immunomodulatory activities. Upon oral administration, tinengotinib selectively binds to and inhibits AKs A and B, which inhibit cell division in tumor cells that overexpress AKs. Tinengotinib also targets JAKs that are involved in cytokine signaling and inflammation, and FGFRs and VEGFRs, which are overexpressed in the microenvironment (TME) and contribute to neovascularization, tumor growth and metastasis. These kinases are overexpressed by a wide variety of cancer cell types and drive tumor cell proliferation.
tinidazole: A 5-nitroimidazole derivative with antiprotozoal property. Although the mechanism of action has not been fully elucidated, it has been suggested that tinidazole is metabolized and yields nitrite anions and metronidazole. Metronidazole's nitro group in turn is reduced via the parasite ferredoxin, thereby generating a series of free nitro radicals including nitro anions. Toxicity is achieved via depletion of sulfhydryl groups and DNA strand breaks with multiple hits having an additive effect and ultimately leading to cell death.
tinodasertib: A selective mitogen-activated protein kinase (MAPK)-interacting protein kinase (MNK) types 1/2 inhibitor with potential antineoplastic activity. Upon administration, tinodasertib may inhibit MNK1/2-dependent phosphorylation of eukaryotic initiation factor 4E (eIF4E) and interfere with its role in mRNA translation. eIF4E is an oncoprotein that must be phosphorylated before it can promote the proliferation and progression of tumor cells. MNKs are a family of serine/threonine kinases that have been implicated in oncogenic transformation and tumor progression.
tinostamustine: An alkylating histone-deacetylase inhibitor (HDACi) fusion molecule composed of the alkylating agent bendamustine fused to the pan-HDACi vorinostat, with potential bi-functional antineoplastic activity. Upon administration of tinostamustine, the vorinostat moiety targets and binds to HDACs. This leads to an accumulation of highly acetylated histones, which results in an induction of chromatin remodeling, a modulation of gene expression, an inhibition of tumor cell division and the induction of tumor cell apoptosis. The bendamustine moiety binds to, alkylates and crosslinks macromolecules, inhibiting DNA, RNA and protein synthesis, which also results in tumor cell apoptosis. Thus, tinostamustine shows superior efficacy compared to the activity of either agent alone. In addition, the inhibition of HDAC6 activity by tinostamustine induces the activation of inositol-requiring enzyme 1 (IRE-1), the key regulatory protein for the unfolded protein response (UPR). Induction of the UPR increases the sensitivity of certain cancer cell types to certain chemotherapeutic agents, such as proteasome inhibitors. Therefore, tinostamustine may work synergistically with proteasome inhibitors. HDACs, enzymes that deacetylate chromatin histone proteins, are overexpressed in various cancers and play a key role in proliferation and resistance of tumor cells.
tinurilimab: A humanized monoclonal antibody directed against the immune checkpoint regulator carcinoembryonic antigen-related cell adhesion molecule 6 (CEACAM6; CEACAM-6; CD66c), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, tinurilimab targets, binds to and blocks the activity of CEACAM6 expressed on various tumor and immune cells, including T cells. Blocking CEACAM6 signaling abrogates effector T-cell inhibition, activates antigen-specific T ymphocytes, increases secretion of T-cell cytokines and effector molecules, and enhances cytotoxic T-cell-mediated tumor cell lysis, which results in a reduction in tumor cell proliferation. CEACAM6, an immune checkpoint receptor, is associated with tumor-mediated immune suppression. Elevated CEACAM6 expression is associated with advanced tumor stages and poor prognosis.
tinzaparin sodium: The sodium salt of a low molecular weight heparin (LMWH), obtained by controlled enzymatic depolymerization of heparin from porcine intestinal mucosa, with antithrombotic properties. Tinzaparin is a potent inhibitor of several activated coagulation factors, especially Factors Xa and IIa (thrombin); its primary activity is mediated through the plasma protease inhibitor antithrombin. In addition, this agent may inhibit angiogenesis through: 1) competitive binding of the heparin-binding sites on endothelial cells for the proangiogenic cytokines vascular endothelial growth factor (VEGF) and beta-fibroblast growth factor (beta-FGF) and 2) increasing the release of tissue factor pathway inhibitor (TFPI), a negative regulator of angiogenesis.
tiomolibdate choline: An orally active second generation tetrathiomolybdate analog with anti-angiogenic and antineoplastic activities. Tiomolibdate choline selectively chelates the copper ion in superoxide dismutase 1 (SOD1) in endothelial cells, thereby depleting SOD1 of copper and inhibiting its activity. Inhibition of SOD1 interferes with the activation of several signal transduction pathways required for cellular proliferation and angiogenesis, including those mediated by ERK1/2 and FAK and Src kinases. This results in an inhibition of cell proliferation and angiogenesis as well as induction of apoptosis.
tiomolibdate diammonium: An ammonium salt with potential antiangiogenic and antitumor activities. ammonium Tiomolibdate diammonium has been found to deplete systemic copper reserves through an unknown mechanism. This agent has been shown to inhibit the activities of cuproenzymes, including superoxide dismutase 1 (SOD1) and cytochrome c oxidase (COX), which may contribute to its antiangiogenic and antitumor effects.
tiotropium bromide monohydrate: The monohydrate bromide salt form of tiotropium, a quaternary ammonium derivative of atropine and a long-acting muscarinic receptor antagonist, with bronchodilating activity. Upon inhalation, tiotropium binds to and blocks mainly muscarinic M3 receptors located on smooth muscle cells, thereby preventing smooth muscle contraction
tipifarnib: A nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.
tirabrutinib: An orally available formulation containing an inhibitor of Bruton agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, tirabrutinib covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
tiragolumab: A human monoclonal antibody targeting the co-inhibitory molecule and immune checkpoint inhibitor T-cell immunoreceptor with immunoglobulin (Ig) and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT), with potential immune checkpoint inhibitory activity. Upon administration, tiragolumab binds to TIGIT expressed on various immune cells, particularly on tumor-infiltrating T lymphocytes (TILs), thereby preventing the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PVRL2) and CD155 (poliovirus receptor; PVR; nectin-like 5; NECL-5). This enhances the interaction of CD112 and CD155 with the costimulatory receptor CD226 (DNAX Accessory molecule-1; DNAM-1), which is expressed on immune cells, such as natural killer (NK) cells and CD8+ T cells, and leads to CD226 dimerization and CD226-mediated signaling. This activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family and immune inhibitory receptor, plays a key role in the suppression of T-cell proliferation and activation; it is involved in tumor cell immune evasion, and the inhibition of antiviral immune responses.
tirapazamine: A benzotriazine di-N-oxide with potential antineoplastic activity. Tirapazamine is selectively activated by multiple reductases to form free radicals in hypoxic cells, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. This agent also sensitizes hypoxic cells to ionizing radiation and inhibits the repair of radiation-induced DNA strand breaks via inhibition of topoisomerase II.
Tirazone: (Other name for: tirapazamine)
tirbanibulin: An orally bioavailable small molecule Src kinase inhibitor with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, tirbanibulin specifically binds to the peptide substrate binding site of Src kinase; inhibition of kinase activity may result in the inhibition of primary tumor growth and the suppression of metastasis. Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis.
tisagenlecleucel: Autologous T lymphocytes transduced with a modified lentiviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), coupled to the signaling domain of 4-1BB (CD137), with potential immunomodulating and antineoplastic activities. Upon transfusion, tisagenlecleucel direct the T lymphocytes to CD19-expressing tumor cells, thereby inducing a selective toxicity in CD19-expressing tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19 and the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3-zeta (or CD247) is a transmembrane signaling adaptor polypeptide that regulates the assembly of complete TCR complexes and their expression on the cell surface.
tislelizumab-jsgr: A monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (PD-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, tislelizumab-jsgr binds to PD-1 and inhibits the binding of PD-1 to the PD-1 ligands programmed cell death-1 ligand 1 (PD-L1), and PD-1 ligand 2 (PD-L2). This prevents the activation of PD-1 and its downstream signaling pathways. This may restore immune function through the activation of both T cells and T-cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the immunoglobulin (Ig) superfamily expressed on activated T cells, negatively regulates T-cell activation and effector function when activated by its ligands; it plays an important role in tumor evasion from host immunity.
tisotumab vedotin-tftv: An antibody-drug conjugate (ADC) comprised of tisotumab, a monoclonal antibody against human tissue factor (TF) covalently coupled, via a protease-cleavable peptide linker, to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antiangiogenic, anticoagulant and antineoplastic activities. Upon administration of tisotumab vedotin, the tisotumab moiety binds to cell surface TF and is internalized. Tisotumab binds to factor VIIa (FVIIa), which interferes with the activation of factor X (FX) into FXa. This may prevent thrombin formation and cancer-associated venous thromboembolism, and may inhibit angiogenesis and tumor cell proliferation. After internalization of the agent, the MMAE moiety is released by proteolytic cleavage. It then binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. TF, a transmembrane protein and initiator of the coagulation cascade, is overexpressed in many tumor cells and tumor-resident endothelial cells. Expression of TF is correlated with metastasis, angiogenesis, tumor cell growth and tumor-associated thrombosis.
TISSEEL VH: (Other name for: fibrin sealant)
titanium dioxide/zinc oxide sunscreen cream SPF 60: A sunscreen formulated with titanium dioxide and zinc oxide with broad UV spectrum-blocking properties. Upon topical application, titanium dioxide and zinc oxide reflect and block both UVA and UVB ultraviolet light rays, protecting the skin against UVA and UVB radiation that causes sunburn, premature aging of the skin and skin cancer.SPF30 and SPF60 contain 5% titanium dioxide and zinc oxide, and 7.5% titanium dioxide and zinc, oxide respectively.
tivantinib: An orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity. Tivantinib binds to the c-Met protein and disrupts c-Met signal transduction pathways, which may induce cell death in tumor cells overexpressing c-Met protein or expressing consitutively activated c-Met protein. c-Met protein, the product of the proto-oncogene c-Met, is a receptor tyrosine kinase also known as hepatocyte growth factor receptor (HGFR); this protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis.
Tivdak: (Other name for: tisotumab vedotin-tftv)
Tivicay: (Other name for: dolutegravir)
tivozanib hydrochloride: The hydrochloride salt of tivozanib, an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGFR tyrosine kinases, frequently overexpressed by a variety of tumor cell types, play a key role in angiogenesis.
tivumecirnon: An orally available, small molecule antagonist of C-C chemokine receptor type 4 (CCR4) with potential immunomodulatory and antineoplastic activities. Upon oral administration, tivumecirnon inhibits the binding of CCR4 to its signaling molecules, thereby blocking the recruitment of regulatory T cells (Tregs) to the tumor microenvironment (TME). This may abrogate the immunosuppressive effects of Tregs and promote an effective anti-tumor immune response. CCR4, a chemokine receptor normally expressed on circulating and tissue-resident T cells, is highly expressed on circulating Tregs and is associated with poor prognosis in certain cancers.
tixestobart: A monospecific hexamer-forming antibody, based on the HexaBody technology platform, directed against the cell surface antigen CD27, with potential immunostimulatory and antineoplastic activities. Upon administration, tixestobart targets and binds to CD27 expressed on a variety of immune cell types, including most T lymphocytes, and forming a hexamer upon binding. This induces CD27-mediated signaling, and enhances CD27-mediated responses, including the expansion of antigen-activated T cells and natural killer (NK) cells. This restores immune function and leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. CD27, a co-stimulatory molecule and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T lymphocytes, memory B cells and NK cells. It plays an important role in NK cell-mediated cytolytic activity and T- and B-lymphocyte proliferation and activation.
tizanidine hydrochloride: The hydrochloride salt form of tizanidine, an imidazoline derivative structurally similar to clonidine and an adrenergic agonist with muscle relaxant property. Tizanidine stimulates alpha-2 adrenergic receptors in the central nervous system, thereby inhibiting presynaptic release of norepinephrine and increasing the inhibitory effect on alpha motor neurons and motor reflexes. Tizanidine exerts some activity at the postsynaptic excitatory amino acid receptors and imidazoline receptors which may contribute to the overall reduction in facilitation of spinal motor neurons. Overall, tizanidine hydrochloride causes muscle relaxation, reduces spasticity and antinociceptive effects.
tizetatug rezetecan: An antibody-drug conjugate (ADC) composed of an immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) conjugated, via a cleavable linker, to the exatecan derivative and topoisomerase-1 inhibitor rezetecan, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of tizetatug rezetecan targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and linker cleavage, rezetecan is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing TROP-2. TROP-2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.
TLR 2/6/9 agonist PUL-042: A solution consisting of a combination of two toll-like receptor (TLR) ligands: Pam2CSK4 acetate (Pam2), a synthetic diacylated lipopeptide (LP) that is an agonist of TLR2 and TLR6 (TLR2/6) and the TLR9 agonist oligodeoxynucleotide (ODN) M362, which contains unmethylated CpG-based dinucleotides, with potential immunostimulating activity. Upon administration via inhalation of the PUL-042 solution, the components in PUL-042 bind to and activate TLRs on lung epithelial cells. This induces the epithelial cells to produce peptides and reactive oxygen species (ROS) against pathogens, including bacteria, fungi and viruses, that are present in the lungs. M362, through binding of the CpG motifs to TLR9 and subsequent TLR9-mediated signaling, initiates the innate immune system and activates macrophages, natural killer (NK) cells, B cells, and plasmacytoid dendritic cells (pDCs), stimulates interferon-alpha (IFN-a) production and induces a T-helper 1 cells (Th1)-mediated immune response. Pam2CSK4, through TLR2/6, activates the production of T-helper 2 cells (Th2), leading to the production of Th2-specific cytokines. Altogether, this protects against and kills the pathogens present in the lungs and prevents pulmonary infection. TLRs play fundamental roles in both pathogen recognition and the activation of innate immunity.
TLR agonist BSG-001: A toll-like receptor (TLR) agonist with potential immunomodulating and antineoplastic activities. Upon inhalation, TLR agonist BSG-001 activates one or more not yet disclosed TLRs, which may result in macrophage and plasmacytoid dendritic cell (pDC) stimulation, secretion of interferon alpha (IFNa), production of proinflammatory cytokines, upregulation of co-stimulatory molecules, enhanced T- and B-cell stimulatory responses, T-cell proliferation and a T-helper 1 (Th1) immune response. TLRs are transmembrane receptors that recognize structurally conserved microbial molecules such as bacterial cell-surface lipopolysaccharides (LPS), lipoproteins, lipopeptides, lipoarabinomannan and flagellin, among others. Immune responses stimulated by TLR activation may result in immune-mediated tumor cell killing.
TLR agonist Decoy20: A multi-targeted toll-like receptor (TLR) agonist, with potential immunomodulating and antineoplastic activities. Upon administration, TLR agonist Decoy20 activates one or more not yet disclosed TLRs expressed on various immune cells, such as macrophages and plasmacytoid dendritic cells (pDCs), which results in their stimulation, the production of certain pro-inflammatory cytokines, and the upregulation of co-stimulatory molecules. This may lead to enhanced T- and B-cell stimulatory responses, cytotoxic T-cell proliferation, a T-helper 1 (Th1) immune response, and immune-mediated tumor cell killing. TLRs are transmembrane receptors that recognize structurally conserved microbial molecules such as bacterial cell-surface lipopolysaccharides (LPS), lipoproteins, lipopeptides, lipoarabinomannan and flagellin, among others. Immune responses stimulated by TLR activation may result in innate and adaptive immune-mediated tumor cell killing.
TLR-directed cationic lipid-DNA complex JVRS-100: A cationic lipid DNA complex (CLDC) consisting of DOTIM/cholesterol liposomes and plasmid DNA, containing immunostimulatory CpG and non-CpG motifs, with potential immunostimulating and antineoplastic activities. Upon systemic administration, TLR-directed cationic lipid-DNA complex JVRS-100 enters dendritic cells (DCs) and macrophages; immunostimulatory DNA binds to and activates Toll-like receptors (TLRs), which may result in the generation of anti-tumor natural killer (NK) cell and T-cell responses by the innate immune system. In addition, as a vaccine adjuvant, this agent may induce a strong cytotoxic T-lymphocyte (CTL) response to co-administered antigen.
TLR1/2 agonist Pam3Cys-GDPKHPKSF: A vaccine adjuvant and synthetic Toll-like receptor (TLR) type 1 and 2 ligand composed of a lipopeptide containing a water-soluble derivative of Pam3-Cys, the biologically active component of the mycobacterial 19 kDa lipoprotein of mycobacteria, that is covalently linked to a synthetic peptide (GDPKHPKSF), with potential immunostimulating activity. Upon administration, TLR1/2 agonist Pam3Cys-GDPKHPKSF targets, binds to and activates TLR1/2, which induces CD8- and T-helper 1 CD4-positive T-cell responses. This may enhance T-cell-mediated immune responses when administered together with peptide vaccine.
TLR4 agonist G100: A synthetic lipid A derivative and selective toll-like receptor 4 (TLR4) agonist composed of glucopyranosyl lipid-A (GLA) in a stable, oil-in-water emulsion (GLA-SE), with potential immunostimulating and antineoplastic activities. Upon intratumoral administration into the immunosuppressed tumor microenvironment (TME), TLR4 agonist G100 binds to and activates TLR4 on various immune cells, thereby stimulating dendritic cells (DCs), monocytes and macrophages. This activation results in the production of pro-inflammatory cytokines and chemokines. This induces a T helper cell-1 (Th1) immune response and activates a cytotoxic T-lymphocyte (CTL) response against tumor-associated antigens (TAAs) that were released in the TME by tumor cells lysed during cytotoxic treatments, such as radiotherapy. TLR4, a member of the TLR family, plays a key role in the activation of innate immunity.
TLR4 agonist GSK1795091: A toll-like receptor 4 (TLR4) agonist, with potential immunoadjuvant activity. Upon administration, GSK1795091 binds to and activates TLR4, thereby stimulating dendritic cells (DCs), monocytes and macrophages. This activation results in the production of pro-inflammatory cytokines, including interferon gamma (IFN-g), tumor necrosis factor-alpha (TNF-a) and the interleukins (IL), IL-1 beta, -6 and -12. This may induce a T helper cell-1 (Th1) immune response and, upon co-administration of a vaccine containing tumor-associated antigens (TAAs), activates a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing those TAAs. TLR4, a member of the TLR family, plays a key role in the activation of innate immunity.
TLR7 agonist ANA773 tosylate: The tosylate salt form of ANA773, a Toll-like Receptor 7 (TLR7) agonist prodrug with potential immunostimulating activity. Upon oral administration, ANA773 is metabolized into its active form that binds to and activates TLR7, thereby stimulating dendritic cells (DCs) and enhancing natural killer cell (NK) cytotoxicity. This activation results in the production of proinflammatory cytokines, including interferon alpha, and enhanced antibody-dependent cellular cytotoxicity (ADCC). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR7 agonist APR003: An orally bioavailable, small molecule Toll-Like Receptor 7 (TLR7) agonist, with potential immunostimulating activity. Upon oral administration, TLR7 agonist APR003 targets, binds to and activates TLR7, thereby stimulating dendritic cells (DCs) and enhancing natural killer cell (NK) cytotoxicity. This activation results in the production of proinflammatory cytokines, including interferon alpha, and enhanced antibody-dependent cellular cytotoxicity (ADCC). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity. APR003 is localized in the gastrointestinal (GI) tract and liver, which may promote local immune responses and local tumor eradication and prevent systemic adverse effects.
TLR7 agonist BNT411: A Toll-like receptor (TLR) 7 agonist with potential immunostimulating and antitumor activities. Upon administration, TLR7 agonist BNT411 binds to and activates TLR7. This may trigger, in addition to other possible responses, the activation of cluster of differentiation (CD) 8+ T cells, B cells, and innate immune cells including natural killer (NK) cells and macrophages. TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR7 agonist CAN1012: A Toll-like receptor type 7 (TLR 7) agonist, with potential immunostimulating and antineoplastic activities. Upon intratumoral (IT) administration, TLR7 agonist CAN1012 targets, binds to and activates TLR7, thereby activating TLR7-mediated pathways. This stimulates the maturation and activation of antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs results in the production of pro-inflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL)- and B-lymphocyte-mediated immune responses. This may lead to tumor cell lysis. TLR7, a member of the TLR family, plays a fundamental role in the activation of the innate immune system, myeloid cell responses and tumor antigen presentation.
TLR7 agonist JNJ-64794964: An orally bioavailable Toll-like receptor (TLR) 7 agonist, with potential immunostimulating, antiviral and antitumor activities. Upon oral administration, TLR7 agonist JNJ-64794964 specifically targets, binds to and activates TLR7. This triggers anti-viral and anti-tumor activities through the activation of cluster of differentiation (CD) 8-positive T cells, B cells, and innate immune cells including natural killer (NK) cells and macrophages, secretion of interferon alpha (IFNa), and the production of various pro-inflammatory and anti-inflammatory cytokines. TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR7 agonist LHC165: A benzonapthyridine Toll-like receptor (TLR) 7 agonist that is adsorbed to aluminum hydroxide with immunostimulating and potential antitumor activities. Upon intratumoral administration of TLR7 agonist LHC165, the agent is slowly released and targets, binds to and activates TLR7. This may trigger, in addition to other possible responses, the activation of cluster of differentiation (CD) 8+ T cells and natural killer (NK) cells, the blockage of the suppressive function of regulatory T cells (Tregs), and the production of interferon alpha (IFNa). TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR7 agonist RO7119929: An orally bioavailable Toll-like receptor (TLR) 7 agonist, with potential immunostimulating and antitumor activities. Upon oral administration, TLR7 agonist RO7119929 targets, binds to and activates TLR7. This may trigger the activation of cluster of differentiation (CD) 8-positive T cells, B cells, and innate immune cells including natural killer (NK) cells and macrophages, and may induce the production of cytokines including interferon alpha (IFNa), leading to antitumor activity. TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR7 agonist SHR2150: A Toll-like receptor (TLR) 7 agonist with potential immunostimulating and antineoplastic activities. Upon administration, TLR7 agonist SHR2150 targets, binds to and activates TLR7. This may trigger, in addition to other possible responses, the activation of dendritic cells (DCs), macrophages and B cells, and activate cluster of differentiation (CD) 8+ T cells. This may induce anti-tumor immune responses. TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR7/8 agonist BM201: An extended-release (ER) microparticle formulation of toll-like receptor type 7 and 8 (TLR 7/8) agonist, with potential immunostimulating and antitumor activities. Upon administration, TLR7/8 agonist BM201 targets, binds to and activates TLR7 and 8, thereby activating TLR7/8-mediated pathways. This stimulates the maturation and activation of antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs results in the production of pro-inflammatory cytokines and the activation of cytotoxic T-lymphocyte (CTL)- and B-lymphocyte-mediated immune responses. This may lead to tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the innate immune system, myeloid cell responses and tumor antigen presentation.
TLR7/8 agonist MEDI9197: A toll-like receptor type 7 and 8 (TLR7/8) agonist with potential immunostimulating and antitumor activities. Upon intratumoral administration, TLR7/8 agonist MEDI9197 binds to and activates TLR7 and 8, thereby stimulating antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs results in the production of proinflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL) and B-lymphocyte immune responses. This may cause tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the immune system.
TLR8 agonist DN1508052: A small molecule Toll-like receptor 8 (TLR8; CD288) agonist with potential immunostimulating and antineoplastic activities. Upon subcutaneous administration, TLR8 agonist DN1508052 binds to TLR8, which is expressed in myeloid dendritic cells (mDCs), monocytes, and natural killer (NK) cells. This may lead to the activation of nuclear factor NF-kappa-B, the release of proinflammatory cytokines and a Th1-weighted anti-tumor immune response. Additionally, activation of TLR8 signaling in tumor cells may block the induction and reverse the suppression of senescent naive and tumor-specific T cells, resulting in enhanced anti-tumor immunity. TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in innate and adaptive immunity.
TLR9 agonist DUK-CPG-001: A synthetic CpG-rich oligonucleotide with potential immunopotentiating activity. TLR9 agonist DUK-CPG-001 binds to and activates intracellular toll-like receptor 9 (TLR9) in monocytes/macrophages, plasmacytoid dendritic cells (DCs), natural killer (NK) cells and B cells. This initiates immune signaling pathways, activates DCs, NK cells and B cells, and induces both the production of T-helper 1 cells (Th1) and a Th1-mediated immune response. TLR9 is a member of the TLR family, which plays a key role in both pathogen recognition and the activation of innate immunity.
TLR9 agonist EMD 1201081: A synthetic oligonucleotide containing phosphorothioate oligodeoxynucleotide with potential immunopotentiating activity. TLR9 agonist EMD 1201081 binds to and activates the intracellular Toll-like receptor (TLR) 9 in monocytes/macrophages, plasmacytoid dendritic cells (DCs) and B cells, initiating immune signaling pathways, activating B cells and inducing T-helper cell cytokine production. TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR9 agonist IMO-2055: A synthetic oligonucleotide containing unmethylated CpG dinucleotides with potential immunopotentiating activity. Mimicking unmethylated CpG sequences in bacterial DNA, TLR9 agonist IMO-2055 binds to and activates intracellular Toll-like receptors (TLR) 9 in monocytes/macrophages, plasmacytoid dendritic cells (DCs) and B cells, initiating immune signaling pathways and activating B cells and DCs and inducing T-helper cell cytokine production. TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR9 agonist MGN1703: A synthetic oligonucleotide based on a proprietary double stem-loop immunomodulator design with potential immunostimulating activity. TLR9 agonist MGN1703 binds to and activates intracellular Toll-like receptor 9 (TLR9) in monocytes/macrophages, plasmacytoidal and myeloid dendritic cells (DCs), and natural killer (NK) cells, initiating immune signaling pathways and inducing T-helper 1 cell (Th1) production leading to the production of memory T cells and a Th1-mediated immune response. By activating the immune system, MGN1703 may attack tumor associated antigen (TAAs). TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
TLR9 agonist SD-101: A proprietary oligonucleotide with immunostimulatory activity. Immunostimulatory phosphorothiolate oligodeoxyribonucleotide SD-101 targets Toll-Like Receptor 9 (TLR9) found on a specialized subset of dendritic cells. The interaction of TLR9 with SD-101, in conjunction with an allergen or antigen, induces activation of memory T helper cells 1 (Th1) against a specific pathogen or allergen, thereby leading to long-lasting therapeutic effects. Furthermore, this agent does not cause a generalized activation of the immune system.
TM4SF1-CAR/EpCAM-CAR-expressing autologous T cells: A mixed preparation of allogeneic T lymphocytes that have been genetically modified to express either a chimeric antigen receptor (CAR) specific for the antigen transmembrane 4 L six family member 1 (TM4SF1) (CART-TM4SF1) or a CAR specific for epithelial cell adhesion molecule (EpCAM) (CART-EpCAM), with potential immunostimulating and antineoplastic activities. Upon administration of the TM4SF1-CAR/EpCAM-CAR-expressing autologous T cells, the TM4SF1-CAR-expressing autologous T cells specifically recognize and bind to TM4SF1-expressing tumor cells and the EpCAM-CAR-expressing autologous T cells specifically recognize and bind to EpCAM-expressing tumor cells, resulting in tumor cell lysis. TM4SF1 and EpCAM are expressed by a variety of tumor cells.
TMPRSS6 RNAi SLN124: An RNA interference (RNAi) therapeutic composed of the liver-targeted ligand N-acetylgalactosamine (GalNAc) conjugated to small-interfering RNAs (siRNAs) directed against the serine protease TMPRSS6, that may potentially be used in the treatment of iron overload associated with certain disorders such as beta thalassemia and myelodysplastic syndromes. Upon administration of TMPRSS6 RNAi SLN124, the GalNAc moiety targets and binds with high affinity to asialoglycoprotein receptors (ASGPRs) expressed on hepatocytes. Once inside the cell, the siRNAs bind to and silence TMPRSS6 mRNA and inhibit both the translation and expression of the TMPRSS6 protein. This prevents TMPRSS6-mediated suppression of the bone morphogenetic protein (BMP)‐SMAD signaling pathway and leads to an increase in hepcidin levels. Hepcidin decreases the uptake of dietary iron and the release of iron from cellular storage, which may normalize iron levels. Hepcidin plays a key role in the homeostasis of systemic iron; low levels of hepcidin are associated with iron overload in certain disorders.
TNFalpha/IL-2-encoding oncolytic adenovirus TILT-123: A genetically-engineered, replication competent, oncolytic serotype 5/3 capsid-modified adenovirus and encoding for the T-cell immunostimulatory cytokines tumor nerosis factor-alpha (TNF-alpha) and interleukin-2 (IL-2), with potential oncolytic and immunostimulating activities. Upon administration of TNFalpha/IL-2-encoding oncolytic adenovirus TILT-123, the oncolytic adenovirus binds to specific Ad3 receptors that are highly expressed on certain tumor cells and selectively infect and replicate in tumor cells, and express TNF-alpha and IL-2. The oncolytic virus itself induces a viral-mediated tumor cell lysis which may result in the activation of a systemic immune response against tumor-associated antigens. The expressed proteins may further stimulate the immune system to modify the immunosuppressive tumor microenvironment (TME) and induce a cytotoxic T-lymphocyte (CTL) response against the tumor cells. TILT-123 is designed to replicate only in cells with defects in the p16/Rb/E2F pathway, attributed to a mutation common in many solid tumors. Replacement of the Ad5 capsid protein knob with a knob domain from serotype 3 causes higher transduction in cancer cells as compared to normal cells.
TNFerade: (Other name for: golnerminogene pradenovec)
TNP-470: A synthetic analog of fumagillin, an antibiotic isolated from the fungus Aspergillus fumigatus fresenius with antineoplastic activity. TNP-470 binds to and irreversibly inactivates methionine animopeptidase-2 (MetAP2), resulting in endothelial cell cycle arrest late in the G1 phase and inhibition of tumor angiogenesis. This agent may also induce the p53 pathway, thereby stimulating the production of cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis.
tobemstomig: A bispecific antibody directed against the human negative immunoregulatory checkpoint receptors programmed cell death protein 1 (PD-1; PD1; PDCD1; CD279; Programmed Death 1) and lymphocyte activation gene 3 protein (LAG-3; LAG3; CD223), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, tobemstomig targets and binds to both PD-1 and LAG-3 expressed on T cells and inhibits the PD-1- and LAG-3-mediated downregulation of T-cell activation and proliferation. This may lead to cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. PD-1 and LAG-3 play key roles in suppressing T-cell activation and proliferation.
tobramycin sulfate: The sulfate salt of tobramycin, an aminoglycoside antibiotic derived from the bacterium Streptomyces tenebrarius with bactericidal activity. Following active transport into the cell, tobramycin binds irreversibly to a specific aminoglycoside receptor on the bacterial 30S ribosomal subunit and fixes the 30 S-50 S ribosomal complex at the start codon (AUG), interfering with the initiation of protein synthesis. In addition, this agent induces misreading of the mRNA template, which results in 1) detachment of the ribosomal complex and inhibition of protein elongation or 2) incorporation of the incorrect amino acids into the growing polypeptide chain and the production of abnormal or nonfunctional proteins. Altogether, cell permeability is altered and cell death ensues.
Tobrex: (Other name for: tobramycin sulfate)
Toca FC: (Other name for: extended-release flucytosine)
tocilizumab: A recombinant, humanized IgG1 monoclonal antibody directed against the interleukin-6 receptor (IL-6R) with immunosuppressant activity. Tocilizumab targets and binds to both the soluble form of IL-6R (sIL-6R) and the membrane-bound form (mIL-6R), thereby blocking the binding of IL-6 to its receptor. This prevents IL-6-mediated signaling. IL-6, a pro-inflammatory cytokine that plays an important role in the regulation of the immune response, is overproduced in autoimmune disorders, certain types of cancers and possibly various other inflammatory conditions.
tocladesine: An antimetabolite and a chlorine derivative of the intracellular secondary messenger, cyclic adenosine 3,5-monophosphate (cAMP), with potential antineoplastic activity. Tocladesine appears to be converted to 8-chloro-adenosine by phosphodiesterases and subsequently phosphorylated to 8-chloro-ATP, which functions as a purine analogue and competes with ATP in transcription. In addition, generation of 8-chloro-ATP depletes the endogenous ATP pool that is essential for many biological reactions in intracellular energy transfer. As a result, this agent causes RNA synthesis inhibition, blocks cellular proliferation, and induces apoptosis.
tocophersolan: A water-soluble amphipathic formulation of d-alpha-tocopherol succinate coupled, through a succinate linker, to polyethylene glycol (PEG) 1000. Due to its amphipathic property in which it forms its own micelles, tocophersolan is easily taken up into enterocytes, even in the absence of bile salts; fat soluble d-alpha-tocopherol is then released after hydrolysis. This formulation enhances the absorption of d-alpha-tocopherol compared to the administration of free d-alpha-tocopherol. In addition, tocophersolan may enhance the absorption of water-insoluble agents and other fat-soluble vitamins.
Tocosol Paclitaxel: (Other name for: paclitaxel vitamin E-based emulsion formulation)
tocotrienol: Any of the four forms, alpha, beta, gamma and delta, of a member of the vitamin E family, with potential hypocholesterolemic, antithrombotic, antioxidant, immunomodulating and antineoplastic activities. Tocotrienol inhibits the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, thereby lowering cholesterol levels. In addition, tocotrienol acts through multiple signal transduction pathways to induce cell cycle arrest and caspase-mediated apoptosis, and to decrease tumor cell proliferation. In addition, this agent may inhibit angiogenesis through the blockage of vascular endothelial growth factor receptor (VEGFR) and the subsequent inhibition of tumor cell-induced vessel formation. Also, this agent prevents free radical formation and inhibits lipid peroxidation, thereby preventing DNA cell damage. Tocotrienol farnesyl isoprenoid side chains contain 3 double bonds, which are absent in tocopherols, likely contribute to its anti-cancer activities.
tocotrienol-rich fraction: An orally available nutritional supplement containing high amounts of the vitamin E family member tocotrienol with antioxidant, hypolipidemic and potential immunomodulating and antiproliferative activity. Upon oral administration, tocotrienol-rich fraction (TRF) accumulates in tumor cells and induces cell cycle arrest, programmed cell death, and inhibits tumor cell proliferation. In addition, this agent suppresses 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase activity and inhibits angiogenesis. Rice bran oil, palm oil and annatto seed oil are common sources of TRF.
tofacitinib: An orally available inhibitor of Janus kinases (JAK), with immunomodulatory and anti-inflammatory activities. Upon administration, tofacitinib binds to JAK and prevents the activation of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This may decrease the production of pro-inflammatory cytokines, such as interleukin (IL)-6, -7, -15, -21, interferon-alpha and -beta, and may prevent both an inflammatory response and the inflammation-induced damage caused by certain immunological diseases. JAK kinases are intracellular enzymes involved in signaling pathways affecting hematopoiesis, immunity and inflammation.
tofacitinib topical cream: A topical cream formulation containing the Janus kinase (JAK) inhibitor tofacitinib, with potential immunomodulatory and anti-inflammatory activities. Upon topical administration, tofacitinib binds to JAK and prevents the activation of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This may decrease the production of pro-inflammatory cytokines, such as interleukin (IL)-6, -7, -15, -21, interferon-alpha (IFN-a) and -beta (IFN-b), and may prevent both an inflammatory response and the inflammation-induced damage caused by certain diseases. JAK are intracellular enzymes involved in signaling pathways affecting hematopoiesis, immunity and inflammation.
Tolak: (Other name for: topical fluorouracil)
tolazamide: An intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Tolazamide is converted into five major metabolites that are excreted into the urine. Tolazamide is more potent than tolbutamide and similar in potency to chlorpropamide on a milligram basis. This agent may cause cholestatic jaundice.
tolbutamide: A first-generation sulfonylurea with hypoglycemic activity. Tolbutamide binds to and blocks adenosine triphosphate (ATP)-sensitive potassium channels on the beta cell membrane of the pancreatic islet tissues. This leads to potassium efflux, which results in depolarization, calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis. In addition, tolbutamide may increase the number and affinity of cell surface insulin receptors, thereby enhancing the peripheral response to insulin. Tolbutamide is a CYP2C9 substrate.
tolcapone: A benzophenone derivative and a catechol-O-methyltransferase (COMT) inhibitor. Tolcapone selectively and reversibly inhibits COMT, an enzyme that catalyzes the metabolism of biologically active catechols and their hydroxylated metabolites by transferring the methyl group of S-adenosyl-L-methionine to the phenolic group of catechol-containing substrates. When given in conjunction with a peripheral dopa decarboxylase inhibitor and levodopa, tolcapone may prevent the metabolism of levodopa to 3-methoxy-4-hydroxy- L-phenylalanine (3-OMD) in the brain and peripheral tissues leading to increased bioavailability and enhancement of delivery to the central nervous system (CNS) of levodopa.
tolebrutinib: An orally bioavailable, brain-penetrant, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK), with potential immunomodulatory and anti-inflammatory activities. Upon oral administration, tolebrutinib is able to cross the blood-brain barrier and inhibits the activity of BTK both peripherally and in the central nervous system (CNS). This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway, and the resulting immune activation and inflammation. The inhibition of BTK activity also prevents microglial inflammatory signaling in the CNS, and the resulting immune activation, neuroinflammation and neurodegeneration. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. In addition to B cells, BTK is also expressed in innate immune cells, including macrophages and microglia, and plays an important role in the regulation of microglial inflammatory signaling.
tolfenamic acid: An orally available, benzoic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, analgesic and potential anti-neoplastic activities. Tolfenamic acid inhibits the activity of the enzymes cyclooxygenase (COX) I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The decrease in prostaglandin synthesis results in the therapeutic effects of this agent. Tolfenamic acid also inhibits thromboxane A2 synthesis, by thromboxane synthase, which decreases platelet aggregation. In addition, this agent exerts anti-tumor effects through COX-dependent and independent pathways. Specifically, this agent induces the production of reactive oxygen species, causes DNA damage, increases nuclear factor-kappa B (NF-kB) activation and the expression of activating transcription factor 3 (ATF3) and NSAID-activated gene-1 (NAG1), and inhibits the expression of specificity proteins (Sp), which reduces the expression of Sp-dependent anti-apoptotic and growth-promoting proteins. Altogether, this enhances tumor cell apoptosis, and reduces tumor cell growth and angiogenesis.
tolinapant: An orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptotic activities. Upon administration, tolinapant selectively binds to and inhibits the activity of XIAP and cIAP1. This restores and promotes the induction of apoptotic signaling pathways in cancer cells, and inactivates the nuclear factor-kappa B (NF-kB)-mediated survival pathway. XIAP and cIAP1 are overexpressed by many cancer cell types and suppress apoptosis by inhibiting the activity of certain caspases; they promote both cancer cell survival and chemotherapy resistance.
Tolinase: (Other name for: tolazamide)
toll-like receptor 7 agonist DSP-0509: A synthetic, small molecule, toll-like receptor (TLR) 7 agonist, with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, TLR7 agonist DSP-0509 activates TLR7, thereby inducing type I interferon secretion and activation of cytotoxic T-lymphocyte (CTL)-mediated anti-tumor immune responses, thereby reducing tumor cell growth. TLR7 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.
toll-like receptor 7/8 agonist BDB018: A toll-like receptor type 7 and 8 (TLR 7/8) agonist, with potential immunostimulating and antitumor activities. Upon administration, TLR 7/8 agonist BDB018 binds to and activates TLR7 and 8, thereby activating TLR7/8-mediated pathways. This stimulates the maturation and activation of antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs results in the production of pro-inflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL)- and B-lymphocyte-mediated immune responses. This may lead to tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the innate immune system, myeloid cell responses and tumor antigen presentation.
tomato-soy juice: A juice containing tomato extract and soy protein with potential chemopreventive and antiproliferative activities. Tomato-soy juice contains phytochemicals, including flavonoids, such as the soy isoflavone genistein, and carotenoids, including lycopene. These phytochemicals may exhibit antioxidative activity, antitumor activity by modulating certain tumor-associated signal transduction pathways, and apoptosis-inducing activity.
tomivosertib: An orally bioavailable inhibitor of mitogen-activated protein kinase (MAPK)-interacting serine/threonine-protein kinase 1 (MNK1) and 2 (MNK2), with potential antineoplastic activity. Upon oral administration, tomivosertib binds to and inhibits the activity of MNK1 and 2. This prevents MNK1/2-mediated signaling, and inhibits the phosphorylation of certain regulatory proteins, including eukaryotic translation initiation factor 4E (eIF4E), that regulate the translation of messenger RNAs (mRNAs) involved in tumor cell proliferation, angiogenesis, survival and immune signaling. This inhibits tumor cell proliferation in MNK1/2-overexpressing tumor cells. MNK1/2 are overexpressed in a variety of tumor cell types and promote phosphorylation of eIF4E; eIF4E is overexpressed in many tumor cell types and contributes to tumor development, maintenance and resistance.
tomuzotuximab: A glycoengineered second-generation antibody of cetuximab with potential antineoplastic activities. Upon intravenous administration, tomuzotuximab selectively binds to the extracellular domain of the epidermal growth factor receptor (EGFR), thereby preventing the activation and subsequent dimerization of the receptor. This may prevent EGFR-mediated signaling and inhibit EGFR-dependent tumor cell proliferation. Further, tomuzotuximab has a fully human glycosylation pattern and is glyco-optimized at its Fc domain to promote antibody-dependent cell-mediated cytotoxicity (ADCC). EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of certain tumor types.
Topamax: (Other name for: topiramate)
topical AKT inhibitor SM-020: A topical gel formulation of an inhibitor of the serine/threonine protein kinase AKT (protein kinase B), with potential antineoplastic activity. Upon application, the topical AKT inhibitor SM-020 binds to and inhibits the activity of AKT, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. The AKT signaling pathway is associated with tumor cell proliferation, survival and migration.
topical ammonia-oxidizing bacteria-based probiotic solution: A probiotic spray containing a live-cultured strain of ammonia-oxidizing bacteria (AOB), with potential skin restorative activity. Upon topical application of the AOB-based probiotic solution, the AOBs within the solution oxidize ammonia, thereby converting ammonia on your skin into nitric oxide and nitrite. AOB may potentially protect and restore the skin by preventing ammonia-mediated skin damage. AOB are a naturally-occurring bacteria found in ammonia-rich soil and water.
topical betulinic acid: A topical formulation of a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) with antiinflammatory, anti-HIV and antineoplastic activities. Betulinic acid induces apoptosis through induction of changes in mitochondrial membrane potential, production of reactive oxygen species, and opening of mitochondrial permeability transition pores, resulting in the release of mitochondrial factors involved in apoptosis, activation of caspases, and DNA fragmentation. Although originally thought to exhibit specific cytotoxicity against melanoma cells, this agent has been found to be cytotoxic against non-melanoma tumor cell types including neuroectodermal and brain tumor cells.
topical calcitriol: A topical formulation containing the hormonally active form of vitamin D3, with potential protective activity against chemotherapy-induced alopecia (CIA). Upon topical application to the scalp, calcitriol may prevent keratinocyte apoptosis in anagen hair follicles. Therefore, this agent may protect against the damaging effects of certain chemotherapeutics to the hair follicles.
topical cantharidine solution: A topical, diluted solution composed of the terpenoid cantharidin, which is a natural toxin extracted from blister beetles, that is dissolved in a film-forming vehicle, that can be used for its vesicant and keratolytic activities. Upon application of the topical cantharidine solution to the surface of the wart, the film dries and cantharidin is absorbed by the epidermal cells, thereby releasing serine proteases, and inducing acantholysis, thereby causing the disintegration and detachment of the desmosomes from the tonofilaments. This results in the formation of a small blister under the wart, which eventually falls off with the blistered skin.
topical celecoxib: A topical cream formulation containing celecoxib, a nonsteroidal anti-inflammatory drug (NSAID), with anti-inflammatory and potential keratolytic, chemopreventive and antineoplastic activities. Upon topical application to the affected area, celecoxib selectively binds to and inhibits cyclooxygenase-2 activity (COX-2), which may result in localized keratinocyte apoptosis. The breakdown of keratinocytes prevents their proliferation locally and may reduce tumor cell proliferation.
topical cocaine hydrochloride: A topical formulation of the hydrochloride salt of the tropane alkaloid cocaine, with local anesthetic activity. Upon topical application of the cocaine hydrochloride solution to nasal mucous membranes, cocaine reversibly binds to and blocks the voltage-gated sodium channels in the neuronal cell membranes. By stabilizing neuronal membranes, cocaine inhibits the initiation and conduction of nerve impulses and produces a reversible loss of sensation.
topical fibrinogen-depleted human standardized platelet lysate CAM-101: A topical ophthalmic drop formulation containing fibrinogen-depleted, standardized human platelet lysate which is derived from pooled human platelet lysates (phPL) collected from healthy human donors, that can potentially be used to treat dry eye disease (DED). Upon ophthalmic administration of the topical fibrinogen-depleted human platelet lysate CAM-101, CAM-101 serves as artificial tears to relieve ocular dryness. In addition, as CAM-101 is rich in various growth factors and contains numerous nutritive, anti-inflammatory and pro-regenerative components, the components in CAM-101 may abrogate the underlying processes, such as inflammation, that contribute to DED. Compared to autologous serum drops that are used as artificial tears, CAM-101 is a more shelf-stable, convenient and standardized formulation.
topical fluorouracil: A topical formulation containing the antimetabolite 5-fluorouracil (5-FU), with antineoplastic activity. Upon topical administration, 5-FU is converted into the active metabolite 5-fluoroxyuridine monophosphate (F-UMP), which competes with uracil during RNA synthesis and inhibits RNA processing. Conversion of 5-FU into another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase; this results in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in DNA synthesis, and thus inhibits DNA synthesis. Altogether, this prevents the proliferation of tumor cells locally.
topical gel HT-001: A topical gel formulation, with potential immunomodulatory activity that can potentially be used for treatment of epidermal growth factor receptor (EGFR) inhibitor (EGFRI)-induced skin toxicity. Upon application of the topical gel HT-001 to the affected area(s) of the skin, scalp and nails, HT-001 is able to inhibit the recruitment and activation of immune cells and inhibit the expression of inflammatory mediators that are induced by EGFR signaling blockade resulting from EGFRI cancer therapy. This may prevent or reduce inflammation, reduce substance P and reduce neutrophil activity, thereby preventing and/or clearing the rash and the associated itching and/or hair loss induced by EGFRI therapy. EGFR signaling is critical to maintain normal, healthy skin homeostasis. EGFR inhibition results in high influx of inflammatory cells and production of pro-inflammatory cytokines in the skin. EGFR signaling blockade increases C-C motif chemokine ligand 2 (CCL2) and 5 (CCL5) expression.
topical gemcitabine hydrochloride: A topical preparation of gemcitabine hydrochloride with antineoplastic activity. Gemcitabine, an analogue of the antimetabolite nucleoside deoxycytidine, is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.
topical keratin: A topical formulation containing the naturally-derived biomaterial keratin that has wound repair-promoting, hemostatic, moisturizing and potential radioprotective activities. Upon topical application to an injured site, keratin adheres to the injured tissue, and forms an extracellular matrix that mimics the structure and function of the native tissue. This exogenous extracellular matrix is able to absorb fluid, accelerate thrombus formation through beta1 integrin-mediated platelet adhesion and forms a physical seal on the wound. This facilitates tissue regeneration by promoting cellular proliferation and migration, reducing pro-inflammatory cytokine and chemokine expression and altering the expression of extracellular matrix components and adhesion molecules. Altogether, this promotes wound healing and provides protection from damage due to thermal or radiation exposure. Keratin is an essential component in nails, hair and skin.
topical menthol: A topical cream containing menthol that both causes a localized cooling sensation and has analgesic activities. Upon topical application, menthol acts on the cold-sensitive transient receptor potential cation channel subfamily M member 8 (TMPR8), which provides a cooling sensation. This treatment also provides an analgesic effect through the activation of the inhibitory group II/III metabotropic glutamate receptors (mGluRs). This may decrease neuropathic pain from chemotherapy. In addition, the topical application of menthol causes vasodilation.
topical myristyl nicotinate cream: A topical cream containing the ester prodrug myristyl nicotinate (MN), a lipophilic nicotinic acid derivative with potential chemopreventive activity. Upon topical application, myristyl nicotinate penetrates into the epidermis where the agent is cleaved and is converted into nicotinic acid (niacin); nicotinic acid then diffuses into cells where it is converted to nicotinamide adenine dinucleotide (NAD). NAD may stimulate poly(ADP-ribose) polymerase-1 (PARP-1); enhance skin cell turnover and epidermal differentiation; and strengthen skin barrier function. NAD is a coenzyme that plays a crucial role in many redox reactions; PARP-1 is an enzyme that plays an important role in DNA repair.
topical naloxone hydrochloride: A topical lotion formulation of the dehydrated, hydrochloride salt form of naloxone, an opiate antagonist, with potential anti-pruritic activity. Upon topical application of the naloxone lotion, naloxone binds to and blocks epidermal mu-opiate receptors. This may suppress or diminish pruritus.
topical Nigella sativa seed oil: A topical preparation containing the oil extracted from the seeds of Nigella sativa, also known as black seed or black cumin, with potential antioxidant, anti-inflammatory and immunomodulatory activities. Upon topical administration of Nigella sativa seed oil, the main constituent thymoquinone may stimulate various cytoprotective antioxidant enzymes. Thymoquinone may also exert anti-inflammatory activity by decreasing the production of inflammation mediators, such as tumor necrosis factor (TNF)-alpha, interleukin (IL) 1-beta and IL-6, and inhibiting pro-inflammatory enzymes, including cyclooxygenase (COX). In addition, thymoquinone may modulate the activity of various immune cells such as T-cells, B-cells, macrophages, neutrophils, natural killer (NK) cells, and dendritic cells (DCs). This may decrease the wound healing process time and may reduce radiation dermatitis upon radiation therapy.
topical phenylephrine solution: A topical solution containing phenylephrine, a sympathomimetic amine with vasoconstricting activity. Upon topical application to the oral mucosa, phenylephrine may activate alpha-adrenergic receptors in the mucosa thereby causing vasoconstriction. As a result, this agent may reduce swelling of the mucosal membranes and decrease radiotherapy-induced mucositis.
topical Piper crocatum extract: A topical preparation containing an ethanol extract of Piper crocatum (red betel leaves), with potential anti-inflammatory and anti-oxidant activities. Red betel leaf contains flavonoids, alkaloids, polyphenolates, tannins, and essential oils. Upon topical application of P. crocatum extract, the active ingredients may exert anti-inflammatory and anti-oxidant effects on the skin, and may treat anogenital warts through as of yet not elucidated mechanisms of action.
topical piperidine nitroxide MTS-01: A topical gel containing a cell permeable hydrophilic piperidine nitroxide with potential radioprotective and antioxidant activity. As a stable, free radical compound, MTS-01 may be able to protect cells against the damaging effects of reactive oxygen species (ROS), upon exposure to ionizing radiation and oxidative stress. The topically applied MTS-01 may protect normal tissue from radiation-induced toxicity, such as radiation dermatitis, during radiation therapy.
topical potassium dobesilate: A topical formulation composed of an inhibitor of fibroblast growth factor (FGF), with potential antineoplastic activity. Upon topical administration potassium dobesilate selectively binds to and blocks the activity of FGF, interferes with the binding of FGF to FGFR and prevents FGFR-mediated signaling. This inhibits angiogenesis and tumor cell proliferation, and induces cell death in FGFR-overexpressing tumor cells. FGF plays a key role in angiogenesis, tumor cell proliferation, survival and invasiveness, and is upregulated in many tumor cell types.
topical sirolimus: A topical formulation containing the macrolide sirolimus (rapamycin), which is produced by the organism Streptomyces hygroscopicus, with potential anti-proliferative activity. Upon application of topical sirolimus, this agent migrates into the skin and is internalized by the affected cells. In turn, sirolimus binds to the immunophilin FK binding protein-12 (FKBP-12) and forms a sirolimus:FKBP-12 complex. This complex binds to and inhibits the activity of the serine/threonine kinase mammalian target of rapamycin (mTOR). It also decreases the production of vascular endothelial growth factor (VEGF) and results in the suppression of cellular proliferation.
topical thrombin gel: A topical porous, pliable, purified porcine skin gelatin-based pad containing bovine-derived thrombin, with coagulant and hemostatic activities. Upon topical application of the thrombin gel at the site of tissue injury and bleeding, blood is taken up by the pad/sponge and thrombin cleaves fibrinogen into fibrin, causing platelet aggregation and thrombus formation at the site of injury.
topical tirbanibulin: An ointment containing an inhibitor for both Src tyrosine kinase and tubulin polymerization, with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, tirbanibulin binds to the peptide substrate binding site of Src kinase, upon topical application. This inhibits both downstream signaling and the proliferation of tumor cells overexpressing Src. Src tyrosine kinase, a non-receptor tyrosine kinase upregulated in many tumor cell types, plays an important role in tumor cell proliferation, motility, invasiveness and survival. Tirbanibulin also binds to tubulin heterodimers and inhibits microtubule polymerization, which disrupts microtubule formation and mitosis, leading to further inhibition of cell proliferation. In addition, Tirbanibulin inhibits T-cell migration.
topical trichloroacetic acid: A topical solution containing the caustic agent trichloroacetic acid (TCA), with potential keratolytic, anti-viral and antineoplastic activities. Upon topical application to the affected area, TCA causes tissue necrosis through coagulation of proteins, leads to the destruction of human papilloma virus (HPV)-associated warts and inhibits HPV-driven proliferation of cancer cells.
topical VBP-926 solution: A topical solution with potential anti-inflammatory activity. Upon topical application to the affected area, VBP-926 may help reduce paronychia. Iatrogenic paronychia is associated with chemotherapy treatment.
topical vitamin E: A topical preparation of the fat-soluble vitamin E with potential antioxidant and cytoprotective activities. As a potent antioxidant and radical scavenger, vitamin E ameliorates free-radical damage to cell membranes, thereby protecting cells from reactive oxygen species and maintaining the integrity of cellular macromolecules. In addition, vitamin E noncompetitively inhibits cyclooxygenase (COX) activity in many tissues, which may decrease inflammation. Vitamin E is a generic name for a group of compounds known as tocopherols and tocotrienols (tocols).
topical wound spray HP802-247: A cell-based combination product consisting of a fibrinogen solution and a cell preparation containing allogeneic non-proliferating, living human skin-derived keratinocytes and fibroblasts, suspended in thrombin, with potential topical wound healing enhancing and topical anti-ulcer activity. Upon sequential spray of the two components of HP802-247 topically, a thin fibrin matrix is formed on the wound surface and the cellular components are capable of secreting wound healing cytokines and growth factors, such as vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), granulocyte-macrophage colony-stimulating growth factor (GM-CSF) and keratinocyte growth factor. Cell concentration and keratinocyte-to-fibroblast ratio in HP802-247 are essential for optimal growth factor production and thus the efficacy of this agent.
Topidex: (Other name for: dexamethasone sodium phosphate)
topiramate: A sulfamate-substituted monosaccharide with anticonvulsant activity. Although the mechanism of action has not been fully elucidated, topiramate appears to antagonize kainate/AMPA subtype glutamate receptors, which results in stabilization of hyper-excited neural membranes, inhibition of repetitive neuronal firing, and a decrease in propagation of synaptic impulses, thus impeding seizure activity. In addition, this agent enhances chloride channels activated by the inhibitory neurotransmitter GABA. Kainate/AMPA subtype glutamate receptors are ligand-activated cation channels that mediate the fast component of excitatory postsynaptic currents in neurons of the central nervous system.
topoisomerase I inhibitor Genz-644282: A non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
topoisomerase I inhibitor LMP400: An indenoisoquinoline and non-camptothecin inhibitor of topoisomerase I (Top I) with potential antineoplastic activity. Topoisomerase I inhibitor LMP400 binds to the topoisomerase I-DNA covalent cleavage complexes, and inhibits repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. Compared to camptothecins, indenoisoquinolines are chemically stable, produce stable Top I-DNA cleavage complexes, induce unique DNA cleavage sites and appear more resistant to multidrug efflux pumps.
topoisomerase I inhibitor LMP776: An indenoisoquinoline and non-camptothecin inhibitor of topoisomerase I (Top I) with potential antineoplastic activity. Topoisomerase I inhibitor LMP776 binds to the topoisomerase I-DNA covalent cleavage complexes, and inhibits repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. Compared to camptothecins, indenoisoquinolines are chemically stable, produce stable Top I-DNA cleavage complexes, induce unique DNA cleavage sites and appear more resistant to multidrug efflux pumps.
topoisomerase I/II inhibitor NEV-801: A multi-targeted agent with potential antineoplastic activity. Upon administration, NEV-801 appears to selectively inhibit topoisomerase (Topo) I and II, and activates hypoxia-inducible factor 1 (HIF-1) transcription and the expression of vascular endothelial growth factor (VEGF) mRNA. NEV-801 is also able to overcome multidrug resistance (MDR) 1-mediated resistance.
Topoisomerase-1 Inhibitor LMP744: An indenoisoquinoline derivative and topoisomerase 1 (Top1) inhibitor, with potential antineoplastic activity. Upon administration, LMP744 binds to and stabilizes cleaved DNA-Top1 complexes, which prevents DNA re-ligation, induces stable, irreversible DNA strand breaks, prevents DNA repair, and leads to cell cycle arrest and apoptosis. As tumor cells proliferate at a much higher rate than normal cells, LMP744 specifically targets cancer cells. Top1, a DNA modifying enzyme essential for transcription, replication, and repair of double-strand DNA breaks, is overexpressed in tumor cells.
topotecan hydrochloride: The hydrochloride salt of a semisynthetic derivative of camptothecin with antineoplastic activity. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Camptothecin is a cytotoxic quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata.
topotecan sustained-release episcleral plaque: An episcleral plaque containing sustained-release (SR) topotecan, a semisynthetic derivative of camptothecin and a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminate, with potential antineoplastic activity. Upon local application of the topotecan SR episcleral plaque to the eye, topotecan is released in a sustained manner and inhibits topoisomerase I activity by stabilizing the topoisomerase I-DNA covalent complexes during S phase of cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. The episcleral plaque allows for local delivery of topotecan for the potential treatment of retinoblastoma.
Toprol XL: (Other name for: metoprolol succinate)
topsalysin: A targeted prodrug consisting of a recombinant modified form of the Aeromonas protoxin proaerolysin (PA), bearing a prostate-specific protease cleavage site, with potential antineoplastic activity. When injected directly into the prostate, topsalysin is hydrolyzed to the active toxin aerolysin by the serine protease prostate specific antigen (PSA), a protein overexpressed by prostate cancers and prostate cells in hyperplastic prostatic tissue. Aaerolysin molecules then oligomerize to form ring-like heptamers that are incorporated into the lipid bilayers of cell membranes, forming large membrane channels and resulting in the leakage of cellular contents and lysis of PSA-expressing prostate cells.
Toradol: (Other name for: ketorolac tromethamine)
Toraymyxin: (Other name for: polymyxin-B immobilized fiber PMX-20R)
TORC1/2 kinase inhibitor DS-3078a: An orally bioavailable inhibitor of raptor-mTOR protein complex (TORC1) and rictor-mTOR protein complex (TORC2) with potential antineoplastic activity. TORC1/2 inhibitor DS-3078a binds to and inhibits both TORC1 and TORC2 , which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. TORC1 and 2 are upregulated in some tumors and play an important role in the PI3K/Akt/mTOR signaling pathway, which is frequently dysregulated in human cancers.
toremifene citrate: The citrate salt of a nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which is manifested depending on the tissue or species.
toripalimab-tpzi: A humanized immunoglobulin (Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed cell death 1 (programmed death-1; PD-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, toripalimab binds to PD-1 and inhibits the binding of PD-1 to its ligands, programmed cell death-1 ligand 1 (PD-L1) and PD-1 ligand 2 (PD-L2). This prevents the activation of PD-1 and its downstream signaling pathways. This may restore immune function through the activation of both T cells and T-cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein in the Ig superfamily that is expressed on activated T cells, negatively regulates T-cell activation and effector function when activated by its ligands; it plays an important role in tumor evasion from host immunity.
Torisel: (Other name for: Temsirolimus)
torvutatug samrotecan: An antibody-drug conjugate (ADC) composed of torvutatug, a human monoclonal antibody targeting folate receptor alpha (FRa; FolRa; FOLR1) conjugated to samrotecan, a linker conjugated to exatecan, with potential antineoplastic activity. Upon administration of torvutatug samrotecan, the antibody moiety targets and binds to FRa expressed on tumor cells. Upon binding, cellular uptake and linker cleavage, exatecan is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and generating DNA single- and double-strand breaks, and leading to cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of FRa-expressing tumor cells. FRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues.
tosedostat: A proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death. Noxa is a member of the BH3 (Bcl-2 homology 3)-only subgroup of the proapoptotic Bcl-2 (B-cell CLL/lymphoma 2) protein family.
tositumomab: A murine IgG2 monoclonal antibody directed against the CD20 antigen, found on the surface of B cells. Tositumomab binds to the CD20 surface membrane antigen, resulting in apoptosis, and may stimulate antitumoral cell-mediated and/or antibody-dependent cytotoxicity.
tositumomab and iodine I 131 tositumomab: A murine IgG2a lambda monoclonal antibody, both unradiolabeled and radiolabeled with iodine I 131, directed against the human B cell-specific surface antigen CD20. Tositumomab binds to CD20, resulting in complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), and apoptosis in B cells expressing CD20; in addition to the antibody-mediated cytotoxicity, iodine I 131 tositumomab delivers cytotoxic ionizing radiation specifically to CD20-expressing B cells. In a two-step therapeutic regimen, a predose of unradiolabeled tositumomab is administered first followed by the administration of a dosimetric dose of iodine I 131 tositumomab; 7-14 days later, a therapeutic dose of iodine I 131 tositumomab is administered. The predose of unradiolabeled tositumomab binds to nontumor B cells, increasing the terminal half-life of radiolabeled antibody while protecting nontumor B cells from radiolabeled antibody-mediated radiocytotoxicity.
tosposertib: An orally bioavailable inhibitor of transforming growth factor-beta (TGFb), with potential antineoplastic and anti-fibrotic activities. Upon oral administration, tosposertib specifically targets, binds to and inhibits TGFb, which prevents both the binding of TGFb to its receptor TGFbR and TGFb-mediated signal transduction. This abrogates TGFb-mediated fibrosis and immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFb-dependent proliferation of cancer cells. The TGFb signaling pathway is often upregulated and activated in fibrotic diseases and deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME.
total tumor mRNA-pulsed tumor-specific ex vivo-expanded autologous lymphocyte transfer cells: A preparation of ex vivo expanded, autologous lymphocyte transfer cells (xALTs) that are loaded with total tumor RNA (TTRNA) derived from autologous tumor cells, with potential immunostimulatory and antineoplastic activities. Upon re-infusion of the TTRNA-loaded ALTs into the patient, these ALTs may elicit a highly specific cytotoxic T-lymphocyte (CTL) response against the tumor-associated antigens (TAAs) encoded by the TTRNA.
total tumor RNA-loaded dendritic cell vaccine: A cancer vaccine containing autologous dendritic cells (DCs) that are loaded with total tumor RNA (TTRNA) from a specific tumor, with potential immunostimulatory and antineoplastic activities. Upon administration, TTRNA-loaded DC vaccine may elicit a highly specific cytotoxic T-cell (CTL) response against the tumor-associated antigens (TAAs) encoded by the TTRNA.
Totect: (Other name for: dexrazoxane hydrochloride)
totrombopag: An orally available small molecule agonist of the platelet thrombopoietin (TPO) receptor (TPOR; MPL), with potential megakaryopoiesis stimulating activity. Upon administration, totrombopag mimics TPO and binds to TPOR. This stimulates TPOR and leads to the proliferation and differentiation of megakaryocytes in the bone marrow. This increases the production of blood platelets and decreases bleeding in thrombocytopenic patients. TPOR is a cytokine receptor and member of the hematopoietin receptor superfamily.
Toviaz: (Other name for: fesoterodine fumarate)
tovorafenib: An orally available inhibitor of wild-type and certain mutant forms of A-Raf, B-Raf and C-Raf protein kinases, with potential antineoplastic activity. Upon administration, tovorafenib inhibits Raf-mediated signal transduction pathways, which may lead to an inhibition of tumor cell growth. Raf protein kinases play a key role in the RAF/MEK/ERK signaling pathway, which is often deregulated in human cancers and plays a key role in tumor cell proliferation and survival.
tozasertib lactate: The lactate salt of tozasertib, a synthetic, small-molecule Aurora kinase inhibitor with potential antitumor activity. Tozasertib binds to and inhibits Aurora kinases (AKs), thereby inducing apoptosis in tumor cells in which AKs are overexpressed. AKs, a family of serine-threonine kinases, are essential for mitotic progression, spindle formation, centrosome maturation, chromosomal segregation, and cytokinesis.
tozinameran: A formulation consisting of lipid nanoparticle (LNP) encapsulating a nucleoside modified messenger RNA (modRNA) encoding an optimized form of the full-length severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) spike glycoprotein (SP), with potential immunizing and anti-COVID-19 activities. Upon injection of tozinameran, the LNPs bind to the plasma membrane of nearby cells and release SARS-CoV-2 SP mRNA into the cell. The mRNA is then translated by the cellular protein translation machinery to produce SARS-CoV-2 SP. This may stimulate the immune system to induce an antibody and T-cell-mediated immune response. This may provide active immunization against SARS-CoV-2 infection. SP, usually found on the surface of SARS-CoV-2, plays an essential role in the infection pathway of the SARS-CoV-2 virus.
tozuleristide: A tumor targeting imaging agent composed of the tumor-specific peptide chlorotoxin (CTX), a 36-amino acid neurotoxin found in the venom of the Leiurus quinquestriatus scorpion, linked to the fluorescent dye indocyanine green (ICG), with potential tumor imaging activity using a near-infrared (NIR) imaging system. Upon intravenous administration of BLZ-100, the CTX moiety of BLZ-100 specifically binds to and is internalized by cancer cells of neuroectodermal origin. Using a NIR imaging system, the ICG, which emits light in the NIR range, permits the intraoperative visualization of tumor cells. This leads to the clear distinction of healthy tissues from tumor cells, and facilitates the surgical removal of tumor tissue while sparing normal, healthy cells.
TPF regimen: A regimen consisting of docetaxel, cisplatin and fluorouracil used for the treatment of squamous cell head and neck cancer and gastric cancer.
TPI 287: A synthetic, third generation taxane with potential antineoplastic activity. TPI 287 binds to tubulin and stabilizes microtubules, resulting in inhibition of microtubule assembly/disassembly dynamics, cell cycle arrest at the G2/M phase, and apoptosis.
TPO receptor agonist ONO-7746: An orally available small molecule and platelet thrombopoietin (TPO) receptor (TPOR; MPL) agonist with potential megakaryopoiesis stimulating activity. Upon administration, TPOR agonist ONO-7746 binds to and stimulates TPOR, which may lead to the proliferation and differentiation of megakaryocytes. In turn, this may increase the production of blood platelets and may prevent chemotherapy induced thrombocytopenia (CIT). TPOR is a cytokine receptor and member of the hematopoietin receptor superfamily.
trabectedin: A tetrahydroisoquinoline alkaloid isolated from the marine tunicate Ecteinascidia turbinate with potential antineoplastic activity. Binding to the minor groove of DNA, trabectedin inteferes with the transcription-coupled nucleotide excision repair machinery to induce lethal DNA strand breaks.and blocks the cell cycle in the G2 phase.
trabedersen: A transforming growth factor (TGF)-beta2 specific phosphorothioate antisense oligodeoxynucleotide with the sequence 5'-CGGCATGTCTATTTTGTA-3', with potential antineoplastic activity. Trebedersen binds to TGF-beta2 mRNA causing inhibition of protein translation, thereby decreasing TGF-beta2 protein levels; decreasing intratumoral TGF-beta2 levels may result in the inhibition of tumor cell growth and migration, and tumor angiogenesis. TGF-beta2, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells.
TRAC locus integrated anti-CD19 19(T2)28z1xx CAR-T cells: A preparation of T lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) targeting the tumor-associated antigen (TAA) CD19, linked to the co-stimulatory intracellular signaling domains of CD28 and the zeta chain of the TCR/CD3 complex (CD3-zeta) (CD28zeta; CD28z), and inserted into the T-cell receptor alpha constant (TRAC) locus, with potential immunostimulating and antineoplastic activities. Upon administration, the TRAC locus integrated anti-CD19 19(T2)28z1xx CAR-T cells specifically recognize and bind to CD19-expressing tumor cells, resulting in specific T-cell-mediated tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen overexpressed in B-cell lineage malignancies. CD28 and CD3zeta provide co-stimulatory activity and may enhance the cytotoxic effect and anti-tumor activity of the CAR T cells. The 19(T2)28z1xx CAR includes a 1928zeta mutant, 1xx, which contains one instead of all three immunoreceptor tyrosine-based activation motifs (iTAMs). This may help prevent counterproductive T-cell differentiation and exhaustion. Integrating the anti-CD19 CAR to the TRAC locus may enhance both T-cell potency and the re-expression of the CAR following exposure to antigen.
TraceIT: (Other name for: iodinated polyethylene glycol-based hydrogel tissue marker)
TraceIT Hydrogel: (Other name for: iodinated polyethylene glycol-based hydrogel tissue marker)
TraceIT Tissue Marker: (Other name for: iodinated polyethylene glycol-based hydrogel tissue marker)
Tracleer: (Other name for: bosentan)
Tradjenta: (Other name for: linagliptin)
trained immunity natural killer cells IBR900: A preparation of trained immunity natural killer (tiNK) cells, with potential cytolytic and antineoplastic activities. Upon administration, tiNK cells IBR900 recognize and lyse cancer cells. These cells also secrete pro-inflammatory cytokines, which further stimulate an anti-tumor immune response.
tramadol hydrochloride: A synthetic codeine analogue, tramadol hydrochloride has central analgesic properties with effects similar to opioids, such as morphine and codeine, acting on specific opioid receptors. The hydrochloride salt of tramadol and used as a narcotic analgesic for severe pain, it can be addictive and weakly inhibits norepinephrine and serotonin reuptake.
trametinib dimethyl sulfoxide: A dimethyl sulfoxide (DMSO) solvated form of trametinib, an orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MAP2K; MAPK/ERK kinase; MEK) 1 and 2, with potential antineoplastic activity. Upon oral administration, trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity serine/threonine and tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth.
tranexamic acid: A synthetic derivative of the amino acid lysine with antifibrinolytic activity. With strong affinity for the five lysine-binding sites of plasminogen, tranexamic acid competitively inhibits the activation of plasminogen to plasmin, resulting in inhibition of fibrinolysis; at higher concentrations, this agent noncompetitively inhibits plasmin. This agent has a longer half-life, is approximately ten times more potent, and is less toxic than aminocaproic acid, which possesses similar mechanisms of action.
trans sodium crocetinate: The sodium salt of the trans-isomer of the carotenoid crocetin with potential antihypoxic and radiosensitizing activities. Trans sodium crocetinate (TSC) increases the diffusion rate of oxygen in aqueous solutions such as from plasma to body tissue. The agent has been shown to increase available oxygen during hypoxic and ischemic conditions that may occur in hemorrhage, vascular and neurological disorders, and in the tumor microenvionment.
TransCon IL-2 beta/gamma: A hydrogel carrier-based, sustained-release (SR) formulation containing a variant of the endogenous cytokine interleukin-2 (IL-2), with potential immunostimulating and antineoplastic activities. Upon intravenous administration of TransCon IL-2 beta/gamma (IL-2b/g), the IL-2b/g variant is slowly released over an extended period of time and selectively binds to the IL-2 receptor b/g subunit (IL2Rb/g). The binding of IL-2b/g variant to IL2Rb/g activates IL2Rb/g-mediated signaling, which activates cytotoxic T lymphocytes (CTLs) and natural killer (NK) cells, and induces expression of certain cytotoxic cytokines, such as interferon-gamma (IFNg) and transforming growth factor-beta (TGFb). The activation of the immune responses against tumor cells causes tumor cell destruction. IL2Rb/g plays a key role in the proliferation and activation of effector T cells. IL-2b/g minimally binds to the IL2Ralpha subunit (IL2Ra). Signaling through IL2Ra activates CD4-positive regulatory, immunosuppressive T cells (Tregs), which would suppress tumor cell killing.
transcription factor protein SON-DP: A transcription factor (TF) protein, with potential antineoplastic activity. Upon administration, TF protein SON-DP induces pluripotent reprogramming in cancer cells and generates transient induced pluripotent stem cells (tiPSCs). The in situ generated tiPSCs quickly re-differentiate into normal tissue cells. The tiPSCs also secrete exosomes, which provides embryonic stem cells (ESC)-like microenvironments. This may result in malignant phenotype reversion in the surrounding cancer cells. In addition, the tiPSCs may revert distant metastatic cancer cells into normal cells through tropism effect.
transdermal 17beta-estradiol gel BHR-200: A proprietary, transdermal, hydroalcoholic gel formulation containing 17beta-estradiol, with potential antineoplastic activity. Upon topical administration, 17beta-estradiol exerts its antineoplastic effect(s) through as of yet not fully elucidated mechanism(s) of action(s). This formulation may induce feedback inhibition via the hypothalamic–pituitary–gonadal axis feedback loop, block the secretion of luteinizing hormone (LH) and prevent the release of testosterone from Leydig cells in the testes, thus suppressing testosterone secretion. In addition, 17beta-estradiol inhibits enzymes involved in steroidogenesis, thereby further inhibiting androgen production. Since testosterone is required to sustain prostate tumor growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. In addition, 17beta-estradiol prevents bone loss, and suppresses andropause symptoms, such as hot flashes, which appear during androgen-deprivation therapy (ADT) where the standard of care is the use of gonadotropin releasing hormone (GnRH) analogs. Compared to oral estrogens, the topical gel formulation lowers the risk of cardiovascular side effects.
transdermal 4-hydroxytestosterone: A transdermal formulation containing 4-hydroxytestosterone (4-OHT), a steroidal aromatase inhibitor (AI) and androgen receptor (AR) antagonist, with potential antineoplastic activity. 4-OHT is largely converted into 4-hydroxyandrostenedione (4-OHA) and irreversibly binds to and inhibits aromatase, thereby blocking the conversion of androstenedione to estrone, and testosterone to estradiol. This may inhibit tumor cell proliferation in estrogen-dependent tumor cells. In addition, 4-OHT binds to the AR and may inhibit AR-mediated tumor cell growth. Aromatase, a cytochrome P-450 enzyme, is overexpressed in a variety of cancer cells; it plays a key role in estrogen biosynthesis. Compared to oral 4-OHT, the transdermal formulation allows for continuous release of 4-OHT into the bloodstream and prevents first pass metabolism by the liver.
transdermal estrogen: A transdermal formulation containing the synthetic form of estradiol, the most potent, endogenously produced estrogen. Upon topical administration, estradiol diffuses through the cell membrane and binds to and activates specific intracellular estrogen receptors located on estrogen-responsive tissues, including the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated ligand-receptor complex binds to estrogen response elements on DNA and promotes the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics. In addition, estradiol inhibits the pituitary secretion of the gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism.
transferrin receptor-targeted anti-RRM2 siRNA CALAA-01: A proprietary transferrin receptor-targeted nanoparticle preparation of a non-chemically modified small-interfering RNA (siRNA) directed against the M2 subunit of ribonucleotide reductase (RRM2) with potential antineoplastic activity. Upon administration, transferrin receptor-targeted anti-RRM2 siRNA CALAA-01 binds to transferrin receptors (TfRs), releasing anti-RRM2 siRNA after endocytosis; anti-RRM2 siRNA silences the expression of RRM2 via the RNAi pathway, impeding the assembly of the holoenzyme ribonucleotide reductase (RR) which catalyzes the production of deoxyribonucleotides. As a result, inhibition of cellular proliferation may occur in cells expressing TfR, a cell surface protein overexpressed on various cancer cell types.
transferrin receptor-targeted liposomal p53 cDNA: A cationic liposomal, tumor-targeting p53 (TP53) gene delivery system with potential anti-tumor activity. Transferrin receptor-targeted liposomal p53 cDNA contains plasmid DNA encoding the tumor suppressor protein p53 packaged in membrane-like liposome capsules that are complexed with anti-transferrin receptor single-chain antibody (TfRscFv). Upon systemic administration, the anti-TfRscFv selectively binds to tumor cells expressing transferrin receptors. The p53 plasmid is delivered into the nucleus and as a result, p53 protein is produced in tumor cells that have altered p53 function. This results in the restoration of normal cell growth control mechanisms as well as normal response mechanisms to DNA damage.
transferrin-CRM107: A synthetic targeted protein toxin which consists of human transferrin (Tf) conjugated to a diphtheria toxin that contains a point mutation (CRM107). After binding to the transferrin receptor expressed on the tumor cell surface, transferrin-CRM107 is internalized, where the diphtheria toxin moiety exerts its cytotoxic effect intracellularly by inhibiting protein synthesis through ADP-ribosylation of elongation factor.
transgenic lymphocyte immunization vaccine: A vaccine consisting of a preparation of allogeneic lymphocytes that encode a gene for telomerase. In transgenic lymphocyte immunization, the transgenic cells are infused into the patient, where they serve as antigen- presenting cells (APCs) with the dual function of antigen synthesis and presentation. Vaccination produces an immune response targeting cancer cells expressing telomerase.
TransMID: (Other name for: transferrin-CRM107)
tranylcypromine: An orally bioavailable, nonselective, irreversible, non-hydrazine inhibitor of both monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1/BHC110), with antidepressant and anxiolytic activities, and potential antineoplastic activities. Upon oral administration, tranylcypromine exerts its antidepressant and anxiolytic effects through the inhibition of MAO, an enzyme that catalyzes the breakdown of the monoamine neurotransmitters serotonin, norepinephrine, epinephrine and dopamine. This increases the concentrations and activity of these neurotransmitters. Tranylcypromine exerts its antineoplastic effect through the inhibition of LSD1. Inhibition of LSD1 prevents the transcription of LSD1 target genes. LSD1, a flavin-dependent monoamine oxidoreductase and a histone demethylase, is upregulated in a variety of cancers and plays a key role in tumor cell proliferation, migration, and invasion.
tranylcypromine sulfate: The sulfate salt form of tranylcypromine, an orally bioavailable, nonselective, irreversible, non-hydrazine inhibitor of both monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1/BHC110), with antidepressant and anxiolytic activities, and potential antineoplastic activities. Upon oral administration, tranylcypromine exerts its antidepressant and anxiolytic effects through the inhibition of MAO, an enzyme that catalyzes the breakdown of the monoamine neurotransmitters serotonin, norepinephrine, epinephrine and dopamine. This increases the concentrations and activity of these neurotransmitters. Tranylcypromine exerts its antineoplastic effect through the inhibition of LSD1. Inhibition of LSD1 prevents the transcription of LSD1 target genes. LSD1, a flavin-dependent monoamine oxidoreductase and a histone demethylase, is upregulated in a variety of cancers and plays a key role in tumor cell proliferation, migration, and invasion.
Tranzfect: (Other name for: CRL 1005)
TrasGEX: (Other name for: glycooptimized trastuzumab-GEX)
trastuzumab: A recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2). After binding to HER2 on the tumor cell surface, trastuzumab induces an antibody-dependent cell-mediated cytotoxicity against tumor cells that overexpress HER2. HER2 is overexpressed by many adenocarcinomas, particularly breast adenocarcinomas.
trastuzumab and hyaluronidase-oysk: A ready-to-use combination of trastuzumab, a recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; receptor tyrosine-protein kinase erbB-2), and hyaluronidase-oysk, a recombinant human hyaluronidase PH20 (rHuPH20), that may be used for the treatment of HER2-overexpressing breast cancers. Upon subcutaneous administration, hyaluronidase-oysk temporarily breaks down the hyaluronan barrier, which decreases viscosity of, and allows trastuzumab to spread rapidly through the interstitial space. This improves access to lymphatic and capillary vessels and facilitates the absorption of trastuzumab into the bloodstream. Trastuzumab binds to the extracellular ligand-binding domain of HER2 and mediates the activation of an antibody-dependent cell-mediated cytotoxicity (ADCC) against HER2-expressing tumor cells. HER2 is overexpressed in many adenocarcinomas, particularly breast adenocarcinomas.
trastuzumab botidotin: An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized monoclonal antibody targeting human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated, via a cleavable linker, to the microtubule inhibitor and auristatin derivative duostatin-5 (Duo-5), with potential antineoplastic activity. Upon administration of trastuzumab botidotin, the trastuzumab moiety targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, duo-5 binds to tubulin and inhibits its polymerization, which results in cell cycle arrest and induces tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
trastuzumab conjugate BI-CON-02: A conjugated form of trastuzumab, a humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; ERBB2), with potential immunomodulating and antineoplastic activities. Upon administration, the trastuzumab conjugate BI-CON-02 targets and binds to HER2 on the tumor cell surface, thereby inducing both cytotoxic T-lymphocyte (CTL) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
trastuzumab duocarmazine: An antibody-drug conjugate (ADC) composed of the recombinant humanized anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab linked, via a cleavable linker, to the duocarmycin prodrug, seco-duocarmycin-hydroxybenzamide-azaindole (seco-DUBA), with potential antineoplastic activity. Upon administration of trastuzumab duocarmazine, the trastuzumab moiety binds to HER2 on the tumor cell surface, which triggers the endocytosis of this agent. The linker is then cleaved inside the tumor cell by proteases at the dipeptide valine-citrulline (vc), and releases the active moiety, duocarmycin. Duocarmycin binds to the minor groove of DNA, alkylates adenine at the N3 position, and induces cell death. In addition, trastuzumab induces antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed by many carcinomas and is associated with a poor prognosis.
trastuzumab imbotolimod: An immune stimulating antibody conjugate (ISAC) consisting of trastuzumab, an anti-human epidermal growth factor receptor 2 (HER2) monoclonal antibody, conjugated to a Toll-like receptor (TLR) 7/8 dual agonist, with potential immunostimulating and antineoplastic activities. Upon administration of trastuzumab imbotolimod, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells and, simultaneously, the TLR 7/8 dual agonist moiety targets, binds to and activates TLR7/8 expressed on antigen-presenting cells (APCs), specifically dendritic cells (DCs), in the tumor microenvironment (TME). The trastuzumab binding to the tumor cells causes the engulfment of the trastuzumab imbotolimod-bound tumor cells by tumor-associated myeloid (TAM) cells and the TAMs travel to the lymph nodes. The DCs activated by the TLR7/8 agonist causes the activation of TLR7/8-mediated pathways, and stimulates the maturation and activation of DCs, thereby re-activating the immune system against the tumor cells. Activation of DCs results in the production of pro-inflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL)- and B-lymphocyte-mediated immune responses against tumor-associated antigens (TAAs), which lead to tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the innate immune system, myeloid cell responses and tumor antigen presentation. HER2 is overexpressed by a variety of tumor cell types.
trastuzumab rezetecan: An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1-kappa (IgG1k) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2) conjugated, via a cleavable linker, to rezetecan, an exatecan derivative and topoisomerase 1 inhibitor, with potential antineoplastic activity. Upon administration of trastuzumab rezetecan, the trastuzumab moiety targets and binds to HER2 expressed on tumor cells. Upon cellular uptake and linker cleavage, rezetecan stabilizes covalent topoisomerase I-DNA complexes, and results in single-stranded and double-stranded DNA breaks, the inhibition of DNA replication, the induction of apoptosis and the inhibition of tumor cell proliferation in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
trastuzumab vedotin: An antibody-drug conjugate (ADC) composed of trastuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the tumor-associated antigen (TAA) human epidermal growth factor receptor 2 (EGFR2; HER2; ErbB2), conjugated to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of trastuzumab vedotin, the trastuzumab moiety targets and binds to HER2 on the surface of tumor cells. Following internalization, MMAE targets and binds to tubulin, and inhibits microtubule polymerization. This results in G2/M phase cell cycle arrest and apoptosis in HER2-expressing tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
trastuzumab/tesirine antibody-drug conjugate ADCT-502: An antibody-drug conjugate (ADC) consisting of an engineered version of the humanized monoclonal anti-human epidermal growth factor receptor 2 (HER2) immunoglobulin G1 (IgG1) trastuzumab that is site-specifically conjugated, via a cleavable linker, to the cytotoxic, DNA cross-linking pyrrolobenzodiazepine (PBD) dimer-based drug tesirine, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the trastuzumab moiety of trastuzumab/tesirine ADC ADCT-502 targets the cell surface antigen HER2, which is expressed on various cancer cells. Upon antibody/antigen binding, internalization of the ADC and cleavage of the linker, the cytotoxic PBD moiety is released. The imine groups of tesirine bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death and inhibits the proliferation of HER2-overexpressing tumor cells. The tumor-associated antigen (TAA) HER2 is expressed by various solid tumors and is associated with a poor prognosis.
Trasylol: (Other name for: aprotinin)
Traumasept: (Other name for: povidone-iodine solution)
Traumeel S: Diluted extracts isolated from plants and minerals, including belladonna, arnica, St. Johns wort, and Echinacea. As a homeopathic mouth rinse preparation, Traumeel S exhibits antiinflammatory activity; the mechanism of action has not been fully elucidated. This agent may reduce the severity and duration of treatment-related stomatitis.
Travasol: (Other name for: Amino Acid Injection)
Trazimera: (Other name for: trastuzumab)
Treanda: (Other name for: bendamustine hydrochloride)
trebananib: An angiopoietin (Ang) 1 and 2 neutralizing peptibody, with potential antiangiogenic activity. Trebananib targets and binds to Ang1 and Ang2, thereby preventing the interaction of the angiopoietins with their target tie2 receptors. This may inhibit angiogenesis and may eventually lead to an inhibition of tumor cell proliferation.
Treg inhibitor GIM-531: An orally bioavailable small molecule inhibitor of regulatory T-cells (Tregs), with potential immunomodulatory and antineoplastic activities. Upon oral administration, Treg inhibitor GIM-531 inhibits the activity of immune suppressive Tregs through an as of yet unknown mechanism of action. This may restore antitumor immune responses.
Trelstar: (Other name for: triptorelin pamoate)
Trelstar Depot: (Other name for: triptorelin pamoate)
tremelimumab-actl: A human IgG2 monoclonal antibody directed against the T-cell receptor protein cytotoxic T-lymphocyte-associated protein 4 (CTLA4). Tremelimumab-actl binds to CTLA4 and blocks the binding of the antigen-presenting cell ligands B7-1 and B7-2 to CTLA4, resulting in inhibition of B7-CTLA4-mediated downregulation of T-cell activation; subsequently, B7-1 or B7-2 may interact with another T-cell surface receptor protein, CD28, resulting in a B7-CD28-mediated T-cell activation unopposed by B7-CTLA4-mediated inhibition.
Tremfya: (Other name for: guselkumab)
tremtelectogene empogeditemcel: A preparation of allogeneic, human leukocyte antigen (HLA) matched, cluster of differentiation 34 (CD34)-positive human hematopoietic stem and progenitor cells (HSPCs) that are ex-vivo gene-edited with the clustered regularly interspaced short palindromic repeats (CRISPR)-Cas9 nuclease complex to remove the cluster of differentiation 33 (CD33) antigen, that can potentially be used to improve hematopoietic recovery after hematopoietic cell transplantation (HCT) and CD33-targeting chemotherapy. Upon administration, tremtelectogene empogeditemcel increases and restores the number of HSPCs, which may prevent or decrease infection and other complications of HCT and chemotherapy-induced neutropenia (CIN). The removal of CD33 protects VOR33 from the cytotoxic effects of CD33-targeted agents administered after HCT.
Trental: (Other name for: pentoxifylline)
treosulfan: The prodrug of a bifunctional sulfonate alkylating agent with myeloablative, immunosuppressive, and antineoplastic activities. Under physiological conditions, treosulfan converts nonenzymatically to L-diepoxybutane via a monoepoxide intermediate. The monoepoxide intermediate and L-diepoxybutane alkylate DNA at guanine residues and produce DNA interstrand crosslinks, resulting in DNA fragmentation and apoptosis. In escalated doses, this agent also exhibits myeloablative and immunosuppressive activities.
tretinoin: A naturally-occurring acid of retinol. Tretinoin binds to and activates retinoic acid receptors (RARs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of tumorigenesis. This agent also inhibits telomerase, resulting in telomere shortening and eventual apoptosis of some tumor cell types. The oral form of tretinoin has teratogenic and embryotoxic properties.
Trexall: (Other name for: methotrexate sodium)
tri-specific NK cell engager CC-92328: A tri-specific natural killer (NK) cell engager, with potential immunomodulating and antineoplastic activities. Upon administration, the tri-specific NK cell engager CC-92328 binds to as of yet unelucidated proteins expressed on both cancer cells and NK cells, thereby bringing cancer cells and NK cells together. This stimulates the NKs and allows for NK-mediated cancer cell killing. In addition, the NKs activate T and B cells, and enhance a cytotoxic T-lymphocyte (CTL) immune response against cancer cells.
tri-virus/GD2-specific allogeneic cytotoxic T-lymphocytes: Allogeneic tri-viral specific, Epstein-Barr virus (EBV), cytomegalovirus (CMV) and adenovirus (Ad), cytotoxic T-lymphocytes (tV-CTLs) expressing a chimeric antigen receptor (CAR) specific for disialoganglioside GD2 with potential antineoplastic activity. Tri-virus/GD2-specific allogeneic CTLs are produced by transducing tV-CTLs with a GD2-specific CAR retroviral vector. Upon administration, after an allogeneic hematopoietic stem cell transplant, these CTLs may be selective towards EBV, CMV, and Ad-infected cells and GD2-expressing tumor cells. The human glycosphingolipid GD2 is a tumor associated antigen overexpressed on the surface of all tumors of neuroectodermal origin.
TriAb: (Other name for: monoclonal antibody 11D10 anti-idiotype vaccine)
triamcinolone: A synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.
triamcinolone acetonide: The acetonide salt form of triamcinolone, a synthetic glucocorticosteroid with immunosuppressive and anti-inflammatory activity. Triamcinolone acetonide binds to specific cytosolic glucocorticoid receptors and subsequently interacts with glucocorticoid receptor response element on DNA and alters gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions are accomplished.
triamcinolone acetonide transdermal system SUN-131: A transdermal system (TDS) containing triamcinolone acetonide, a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon application of the TDS to the eyelid, triamcinolone acetonide binds to intracellular glucocorticoid receptors, ultimately inducing the expression of glucocorticoid-responsive genes and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T lymphocytes is also inhibited. Triamcinolone acetonide also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.
triapine: A synthetic heterocyclic carboxaldehyde thiosemicarbazone with potential antineoplastic activity. Triapine inhibits the enzyme ribonucleotide reductase, resulting in the inhibition of the conversion of ribonucleoside diphosphates to deoxyribonucleotides necessary for DNA synthesis. This agent has been shown to inhibit tumor growth in vitro.
triazinate: A synthetic dihydrotriazine derivative with antineoplastic properties. As an antifolate agent related to methotrexate (MTX), triazinate inhibits the enzyme dihydrofolate reductase (DHFR), resulting in decreased tetrahydrofolate production and interference with thymidylate synthesis. Unlike MTX, this agent is not converted to polyglutamate forms. Triazinate also inhibits the transport of folates and may be selectively toxic to MTX-resistant tumor cells.
triazine derivative TriN2755: A synthetic triazene derivative with antineoplastic activity. Upon metabolic activation via N-demethylation, TriN2755 is converted into highly reactive carbocations that can alkylate DNA and other macromolecules, thereby resulting in DNA cross links, inhibiting DNA replication and repair, and subsequently inducing apoptosis. This agent has high hydrophilicity and photostability and shows a favorable toxicity profile over the other triazenes.
tributyrin: A triglyceride prodrug of butyric acid with potential antineoplastic activity. Butyrate, the active metabolite of tributyrin, inhibits histone deacetylase, resulting in increased differentiation, decreased proliferation, cell cycle arrest, and apoptosis in some tumor cell lines.
tricaprin: An orally available precursor of decanoic acid (DA), a 10-carbon fatty acid and major component of medium chain triglyceride oils, with potential antiandrogen and antihyperglycemic properties. Upon oral administration, tricaprin is hydrolyzed to DA, which binds to and partially activates peroxisome proliferator-activated receptor (PPAR)-gamma, as well as PPAR-alpha and PPAR-beta/delta, without inducing adipogenesis. Additionally, tricaprin may improve insulin sensitivity and decrease androgen production.
trichostatin A: A natural derivative of dienohydroxamic acid isolated from species of the bacterial genus Streptomyces. Trichostatin A (TSA) reversibly and specifically inhibits histone deacetylases, resulting in hyperacetylation of core histones which modulate chromatin structure. The increase in histone acetylation promotes selective gene transcription and the inhibition of tumor growth. This agent is a potent inducer of tumor cell growth arrest, differentiation and apoptosis in a variety of transformed cells in culture and in tumor-bearing animals.
triciribine phosphate: The phosphate salt of the synthetic, cell-permeable tricyclic nucleoside triciribine with potential antineoplastic activity. Triciribine inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. Akts are anti-apoptotic serine/theronine-specific protein kinases that phosphorylate and inactivate components of the apoptotic machinery, including Bcl-xL/Bcl-2-associated death promoter (BAD) and caspase 9.
triclosan/copolymer/fluoride toothpaste: A fluoride-based toothpaste containing the anti-inflammatory and broad-spectrum antibacterial agent triclosan and polyvinylmethyl ether maleic acid copolymer (PVM/MA), with potential antibacterial, anti-inflammatory, and protective activities. Upon application of the triclosan/copolymer/fluoride toothpaste to the teeth, the toothpaste helps remove plaque accumulation. The fluoride protects the teeth against cavities while the triclosan prevents inflammation and may protect against gingivitis and mucositis. The copolymer in the toothpaste enhances the uptake of triclosan by enamel and buccal epithelial cells, thereby prolonging its protective effect and enhancing its activity.
Tricor: (Other name for: fenofibrate)
trientine hydrochloride: The hydrochloride salt form of a metal chelating agent with potential anti-angiogenic activity. Trientine chelates excess copper (Cu) ions in the body; the excess copper is subsequently removed from the body through the kidneys. As Cu is an essential cofactor for cuproenzymes, such as superoxide dismutase 1 (SOD1), depletion of copper may inhibit the activation of signal transduction pathways required for cellular proliferation and angiogenesis. In addition, trientine may inhibit copper-induced secretion of interleukin-8 (IL-8).
trifluoperazine hydrochloride: The hydrochloride salt of trifluoperazine, a phenothiazine derivative and a dopamine, alpha-adrenergic, and anticholinergic antagonist with antipsychotic, anxiolytic, and antiemetic activities. Trifluoperazine blocks central dopamine receptors, which may prevent or mitigate delusions and hallucinations caused by an excess of dopamine; dopamine blockade in the chemoreceptor trigger zone (CTZ) may result in an antiemetic effect. This agent binds to central adrenergic receptors, which may result in anxiolytic effects.Trifluoperazine also functions as a calmodulin inhibitor, elevating cytosolic calcium.
trifluridine: A fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity.
trifluridine and tipiracil hydrochloride: An orally bioavailable combination agent composed of the cytotoxic pyrimidine analog trifluridine (5-trifluoro-2'-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor (TPI) tipiracil hydrochloride, in a molar ratio of 1.0:0.5 (TFT:TPI), with potential antineoplastic activity. After oral administration of TAS-102, TFT is phosphorylated to the active monophosphate form TF-TMP, which binds covalently to the active site of thymidylate synthase, thereby reducing the nucleotide pool levels required for DNA replication. Furthermore, the triphosphate form TF-TTP can be incorporated into DNA, which induces DNA fragmentation and leads to the inhibition of tumor growth. TPI exhibits a dual effect: 1) an anti-angiogenic effect mediated through the inhibition of thymidine phosphorylase, which plays important role in nucleotide metabolism and a variety of development processes, including angiogenesis, 2) increased bioavailability of the normally short-lived antimetabolite TFT by preventing its degradation into the inactive form trifluorothymine (TF-Thy). The synergistic effect of the components in TAS-10 may demonstrate antitumor activity in 5-FU-resistant cancer cells.
trigriluzole: A formulation comprised of a prodrug form of the benzothiazole derivative riluzole, with potential anti-depressant, anxiolytic and antineoplastic activities. Following oral administration, trigriluzole is converted into the active form riluzole. While the mechanism of action of riluzole is unknown, its pharmacological activities, some of which may be related to its effect, include the following: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) interference with intracellular events that follow transmitter binding at excitatory amino acid receptors. These activities may result in myorelaxation and sedation due to the blockade of glutamatergic neurotransmission. Additionally, these activities may result in the inhibition of enzymes that are necessary for cell growth, which may decrease tumor cell growth and metastasis.
trilaciclib: A small molecule, competitive inhibitor of cyclin dependent kinases 4 and 6 (CDK4/6), with potential antineoplastic and chemoprotective activities. Upon intravenous administration, trilaciclib binds to and inhibits the activity of CDK4/6, thereby blocking the phosphorylation of the retinoblastoma protein (Rb) in early G1. This prevents G1/S phase transition, causes cell cycle arrest in the G1 phase, induces apoptosis, and inhibits the proliferation of CDK4/6-overexpressing tumor cells. In patients with CDK4/6-independent tumor cells, G1T28 may protect against multi-lineage chemotherapy-induced myelosuppression (CIM) by transiently and reversibly inducing G1 cell cycle arrest in hematopoietic stem and progenitor cells (HSPCs) and preventing transition to the S phase. This protects all hematopoietic lineages, including red blood cells, platelets, neutrophils and lymphocytes, from the DNA-damaging effects of certain chemotherapeutics and preserves the function of the bone marrow and the immune system. CDKs are serine/threonine kinases involved in the regulation of the cell cycle and may be overexpressed in certain cancer cell types. HSPCs are dependent upon CDK4/6 for proliferation.
Trileptal: (Other name for: oxcarbazepine)
Trilipix: (Other name for: fenofibric acid)
Trilisate: (Other name for: choline magnesium trisalicylate)
trilostane: A synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex, resulting in the decreased synthesis of mineralocorticoids and glucocorticoids and the decreased conversion of pregnenolone to progesterone.
trimeric GITRL-Fc OMP-336B11: A Fc-engineered human fusion protein composed of two trimers of tumor necrosis factor (ligand) superfamily, member 18 (TNFSF18; GlTRL) linked to an immunoglobulin Fc domain (GITRL-Fc), with potential immunostimulatory and antineoplastic activities. Upon administration, trimeric GITRL-Fc OMP-336B11 targets, binds to and activates its co-stimulatory surface receptor (glucocorticoid-induced tumor necrosis factor receptor (GITR; TNFRSF18) expressed on T lymphocytes and certain tumor cell types. This activates T lymphocytes, causes T-lymphocyte proliferation and suppresses the activity of regulatory T cells (Treg). This promotes cytotoxic T-lymphocyte (CTL)-mediated killing of tumor cells. GITRL, a member of the tumor necrosis factor (TNF) family of ligands, functions to activate the co-stimulatory receptor GITR to enhance T-cell-modulated immune responses.
trimetazidine: An orally available small molecule compound with anti-ischemic, and potential immunomodulating and antineoplastic properties. Although its exact mechanism is not yet fully elucidated, it is postulated that upon administration, trimetazidine selectively inhibits long-chain 3-ketoacyl coenzyme A thiolase (LC 3-KAT), the final enzyme in the free fatty acid (FFA) beta-oxidation pathway. This stimulates glucose oxidation, which requires less oxygen usage and cellular energy than in the beta-oxidation process. This optimizes myocardial energy metabolism and cardiac functioning in an ischemic condition. In cancer cells, the inhibition of fatty acid oxidation (FAO) alters the metabolic processes needed for tumor cell function and proliferation, thereby inducing tumor cell apoptosis. In addition, inhibition of FAO may potentially block the immunosuppressive functions of myeloid-derived suppressor cells (MSDCs), which are thought to promote malignant cell proliferation and migration by inhibiting T-cell function.
Trimethoprim-Sulfamethoxazole: A synthetic combination of two antibacterial agents, trimethoprim and sulfamethoxazole. This synergistic combination, also known as Co-Trimoxazole, inhibits two sequential steps in the bacterial metabolism of folic acid. Trimethoprim is a pyrimidine inhibitor of dihydrofolate reductase; sulfamethoxazole is a sulfamide inhibitor of bacterial dihydrofolate synthase.
trimethylcolchicinic acid: A colchicine analog with potential antineoplastic activity. Trimethylcolchicinic acid binds to tubulin, inhibiting its polymerization into microtubules and preventing cell division.
trimetrexate glucuronate: A lipid soluble methotrexate derivative with potential antineoplastic activity. Trimetrexate glucuronate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylate, with subsequent inhibition of DNA and RNA synthesis. Trimetrexate glucuronate also exhibits antiviral activity.
Trimo San: (Other name for: oxyquinoline sulfate/sodium lauryl sulfate vaginal gel)
Trimo-San: (Other name for: oxyquinoline sulfate/sodium lauryl sulfate vaginal gel)
Trimox: (Other name for: amoxicillin)
Triostat: (Other name for: liothyronine sodium)
Tripedia: (Other name for: diphtheria toxoid/tetanus toxoid/acellular pertussis vaccine adsorbed)
triptolide analog: A water soluble analog of the diterpenoid triepoxide triptolide isolated from the Chinese herb Tripterygium wilfordii Hook.f., with potential antineoplastic activity. Upon intravenous administration, the triptolide analog inhibits heat shock protein 70 (HSP70) and prevents HSP70-mediated inhibition of apoptosis. This leads to both the induction of apoptosis and a reduction of cancer cell growth. HSP70, a molecular chaperone upregulated in various cancer cells, plays a key role in the inhibition of caspase-dependent and -independent apoptosis.
triptorelin: A synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men.
triptorelin pamoate: The pamoate salt of triptorelin, a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion after prolonged administration. After chronic, continuous administration, a sustained decrease in LH, FSH and testicular and ovarian steroidogenesis is observed. The serum testosterone concentration may fall to levels typically seen in surgically castrated men.
tris-acryl gelatin microspheres: An embolic particle composed of water-soluble, compressible, nonabsorbable tris-acryl gelatin microspheres, with potential use for embolization. Upon administration, the tris-acryl gelatin microspheres (TAGM) serve as an embolic agent before surgery for highly vascularized areas, such as those seen in certain tumors, by penetrating into the vascular system and blocking blood flow. These microspheres may be used to encapsulate various therapeutic agents; drug-loaded microspheres can then be used as drug delivery vehicles during embolization of tumor vasculature.
Trisenox: (Other name for: arsenic trioxide)
trivalent influenza vaccine: A synthetic vaccine consisting of three inactivated influenza viruses, two different influenza type A strains and one influenza type B strain. Trivalent influenza vaccine is formulated annually, based on influenza strains projected to be prevalent in the upcoming flu season. This agent may be formulated for injection or intranasal administration.
trivalent live-attenuated influenza vaccine: A weakened live virus vaccine containing three seasonal influenza reassortants with prophylactic activity against influenza subtypes A and B. The trivalent live-attenuated influenza vaccine (LAIV) contains 2 strains of the influenza subtype A, one for H1N1 and one for H3N2, and one strain of subtype B. Upon intranasal administration by sprayer of the trivalent LAIV, the live viruses replicate in the upper respiratory tract and induce an immune response leading to active immunization against influenza subtypes A and B.
Trivora: (Other name for: ethinyl estradiol/levonorgestrel)
TRK inhibitor AZD6918: An orally available liquid suspension containing the tropomyosin receptor kinase (Trk) inhibitor AZD6918 with potential antineoplastic activity. AZD6918 binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation, and may eventually result in cell cycle arrest and apoptosis of tumor cells that express Trk. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.
TRK inhibitor LOXO-195: An orally bioavailable, selective tropomyosin-related-kinase (tyrosine receptor kinase; TRK) inhibitor, with potential antineoplastic activity. Upon oral administration, LOXO-195 specifically targets and binds to TRK, including the fusion proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1), 2 (NTRK2), and 3 (NTRK3). This prevents neurotrophin-TRK interaction and TRK activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress TRK and/or express NTRK fusion proteins. LOXO-195 targets specific point mutations that occur after treatment with and result in acquired resistance to another TRK inhibitor; therefore, LOXO-195 is able to overcome acquired resistance to other TRK inhibitors. TRK, a family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression of either mutated forms of or fusion proteins involving NTRK family members results in uncontrolled TRK signaling and plays an important role in tumor cell growth and survival.
TRK inhibitor TQB3558: An orally available inhibitor of tropomyosin receptor kinase (Trk), with potential antineoplastic activity. Upon oral administration, Trk inhibitor TQB3558 targets and binds to Trk, thereby preventing neurotrophin-Trk interaction and Trk activation. This may lead to apoptosis of Trk-expressing tumor cells and the inhibition of tumor cell proliferation in Trk-expressing tumors. Trk, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth and survival.
TRK inhibitor TQB3811: An orally bioavailable inhibitor of tropomyosin receptor kinase (TRK), with potential antineoplastic activity. Upon oral administration, TRK inhibitor TQB3811 targets and binds to TRK, thereby preventing neurotrophin-TRK interaction and TRK activation. This may lead to apoptosis of TRK-expressing tumor cells and the inhibition of tumor cell proliferation in TRK-expressing tumors. Members of TRK, a family of receptor tyrosine kinases activated by neurotrophins, are mutated in a variety of cancer cell types and play an important role in tumor cell growth and survival.
TRK inhibitor VC004: An orally bioavailable, second-generation tropomyosin-related-kinase (TRK) inhibitor, with potential antineoplastic activity. Upon oral administration, TRK inhibitor VC004 specifically targets and binds to TRK, TRK mutations and fusion proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1; TrkA), 2 (NTRK2; TrkB), and 3 (NTRK3; TrkC). This inhibits neurotrophin-TRK interaction and TRK activation, thereby preventing the activation of downstream signaling pathways, including the PI3K, RAS/MAPK/ERK and PLC-gamma pathways that are activated by these kinases. This results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress TRK and/or express NTRK fusion proteins. TRK, a family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression of either mutated forms of, or fusion proteins involving NTRK family members results in uncontrolled TRK signaling, which plays an important role in tumor cell growth, survival, invasion and treatment resistance.
TRK/RET inhibitor ND-003: An orally bioavailable small molecule inhibitor of multiple kinases, including tropomyosin-related-kinase (TRK) and rearranged during transfection (RET), with potential antineoplastic activity. Upon oral administration, TRK/RET inhibitor ND-003 targets and binds to TRK and fusion proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK). This inhibits neurotrophin-TRK interaction and TRK activation, thereby preventing the activation of downstream signaling pathways, including the PI3K, RAS/MAPK/ERK and PLC-gamma pathways that are activated by these kinases. This results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress TRK and/or express NTRK fusion proteins. TRK/RET inhibitor ND-003 also targets and binds to RET, thereby inhibiting the activity of RET. This results in an inhibition of cell growth of tumors that exhibit increased RET activity. TRK, a family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression of either mutated forms of, or fusion proteins involving NTRK family members results in uncontrolled TRK signaling, which plays an important role in tumor cell growth, survival, invasion and treatment resistance. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types. Dysregulated RET activity plays a key role in the development and progression of certain cancers.
TRK/ROS1/ALK inhibitor SIM1803-1A: An orally available inhibitor of multiple kinases, including the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), and the tropomyosin-related-kinase (tyrosine receptor kinase; TRK), with potential antineoplastic activity. Upon oral administration, TRK/ROS1/ALK inhibitor SIM1803-1A targets, binds to and inhibits wild-type, point mutants and fusion proteins of ALK, ROS1, and TRK, including fusion proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1; TrkA), 2 (NTRK2; TrkB), and 3 (NTRK3; TrkC). Inhibition of these kinases leads to the disruption of downstream signaling pathways and the inhibition of cell growth of tumors in which these kinases are overexpressed, rearranged or mutated. TRK, a family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression of either mutated forms of, or fusion proteins involving, NTRK family members results in uncontrolled TRK signaling, which plays an important role in tumor cell growth, survival, invasion and treatment resistance. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.
TrkA inhibitor VMD-928: An orally bioavailable, selective inhibitor of tropomyosin receptor kinase A (TrkA; neurotrophic tyrosine receptor kinase (NTRK) type 1; NTRK1; TRK1-transforming tyrosine kinase protein), with potential antineoplastic activity. Upon oral administration, VMD-928 specifically targets and binds to TrkA, inhibits neurotrophin-TrkA interaction and prevents TrkA activation. This prevents the activation of downstream signaling pathways and inhibits cell growth in tumors that overexpress TrkA. Uncontrolled TrkA signaling plays an important role in tumor cell growth, survival, invasion and treatment resistance.
Trodelvy: (Other name for: sacituzumab govitecan-hziy)
trodusquemine: A naturally-occurring cholestane and non-competitive, allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B), with potential hypoglycemic, anti-diabetic, anti-obesity, and antineoplastic activities. Upon administration, trodusquemine selectively targets and inhibits PTP1B, thereby preventing PTP1B-mediated signaling. This prevents the dephosphorylation of the insulin receptor, which improves insulin signaling and insulin sensitivity, and decreases blood glucose levels. In susceptible cancer cells, inhibition of PTP1B causes a reduction of tumor cell proliferation. In addition, as trodusquemine can cross the blood-brain barrier (BBB), it centrally suppresses appetite and causes weight loss. PTP1B, a tyrosine phosphatase, is elevated in certain cancer cells; it is specifically upregulated in human epidermal growth factor receptor 2 (HER2)-driven cancers where it promotes cell growth, and is correlated with a poor prognosis and increased metastatic potential. In diabetes, PTP1B upregulation plays a major role in insulin resistance.
trofosfamide: An orally bioavailable oxazaphosphorine prodrug with antineoplastic activity. Trofosfamide (TFF) is metabolized predominantly to the cyclophosphamide analogue ifosfamide (IFO), which is then metabolized by liver cytochrome P450s to the active isophosphoramide mustard (IPM). IPM alkylates DNA to form DNA-DNA cross-links, which may result in inhibition of DNA, RNA and protein synthesis, and tumor cell apoptosis.
troglitazone: An orally-active thiazolidinedione with antidiabetic and hepatotoxic properties and potential antineoplastic activity. Troglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation.
tropisetron: An indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, tropisetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy-and radiotherapy-induced nausea and vomiting.
tropisetron hydrochloride: The hydrochloride salt form of tropisetron, a selective, competitive serotonin 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist, with antinauseant and antiemetic activities. Tropisetron competitively binds to and blocks the action of serotonin at 5HT3 receptors peripherally on vagus nerve terminals located in the gastrointestinal (GI) tract as well as centrally in the chemoreceptor trigger zone (CTZ) of the area postrema of the central nervous system (CNS). This results in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
trotabresib: An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, trotabresib preferentially binds to the second bromodomain (BD2) of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that contain two homologous bromodomains, the BD1 and BD2 domains. They play an important role during development and cellular growth.
TroVax: (Other name for: recombinant modified vaccinia Ankara-5T4 vaccine)
trovostobart: An engineered, human immunoglobulin (Ig) G1 monoclonal antibody directed against the negative immune checkpoint regulatory protein V-domain Ig suppressor of T-cell activation (VISTA; programmed death 1 homolog; PD1H; PD-1H), with potential negative immune checkpoint regulatory and antineoplastic activities. Upon administration, trovostobart targets and binds to VISTA on myeloid cells and T cells within the tumor microenvironment (TME). This inhibits VISTA-mediated signaling, decreases the presence of monocytic myeloid-derived suppressor cells (MDSCs), increases the presence of natural killer cells (NKs), activates dendritic cells (DCs) and abrogates VISTA-induced suppression of T-lymphocyte immune responses. This enhances cytotoxic T-cell infiltration, proliferation and activation within the TME, increases cytokine production by T cells, and inhibits tumor cell growth. VISTA, a negative checkpoint molecule of immune activation, is highly expressed on myeloid cells, T cells and in several tumor types. It plays a key role in the suppression of T-cell function.
troxacitabine: A dioxolane derivative and a novel L-configuration deoxycytidine analogue with potent antineoplastic activity. When incorporated into growing chain during DNA replication, troxacitabine stops DNA polymerization due to its unnatural L-configuration, in contrast to the normal nucleotides with D-configuration. As a result, this agent terminates DNA synthesis upon incorporated into DNA molecules, and consequently interrupts tumor cell proliferation.
troxacitabine nucleotide prodrug MIV-818: A liver-targeting nucleotide phosphoramidate prodrug of troxacitabine monophosphate (TRX-MP), a dioxolane derivative and L-configuration deoxycytidine analogue, with potential antineoplastic activity. Upon oral administration, MIV-818 is rapidly and specifically hydrolyzed in hepatocytes by liver carboxylesterase 1 (carboxylesterase 1, CE-1), generating high levels of the chain-terminating nucleotide, troxacitabine triphosphate (TRX-TP) in the liver. TRX-TP is then incorporated into tumor cell DNA, leading to termination of DNA synthesis and inhibition of tumor cell proliferation.
Troxatyl: (Other name for: troxacitabine)
TRP2 mRNA-electroporated autologous langerhans-type dendritic cell vaccine: A cancer cell vaccine composed of autologous human Langerhans-type dendritic cells (also known as Langerhans cells or LCs) that are electroporated with mRNA encoding full-length murine tyrosinase-related peptide 2 (TRP2), with potential antineoplastic and immunomodulating activities. Upon vaccination, the TRP2 mRNA-electroporated autologous Langerhans-type dendritic cell vaccine may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against TRP2-expressing tumor cells. TRP2, a tautomerase involved in the synthesis of melanin, is only expressed in melanomas, melanocytes, and the retina. The LCs are differentiated from CD34 positive hematopoietic progenitor cells.
TRPV6 calcium channel inhibitor SOR-C13: An inhibitor of transient receptor potential cation channel vanilloid family member 6 (TRPV6, CaT1 or CATL) with potential antineoplastic activity. TRPV6 calcium channel inhibitor SOR-C13 binds to TRPV6 and prevents the influx of calcium ions into TRPV6-expressing tumor cells. This inhibits the activation of nuclear factor of activated T-cell (NFAT) transcription complex which may result in an inhibition of calcium-dependent cancer cell proliferation and an induction of apoptosis in tumor cells overexpressing TRPV6. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective for calcium compared to other cations; it is overexpressed in a variety of tumors and initiates tumor cell growth, proliferation and metastases.
Trulance: (Other name for: plecanatide)
truncated tissue factor/NGR peptide: A vascular-targeting agent composed of the extracellular domain of the trunctated form of issue factor (tTF) conjugated to the C-terminal peptide GNGRAHA (NGR), with potential procoagulatory and antineoplastic activities. Upon administration, the NGR peptide moiety of tTF-NGR targets and binds to the surface protein aminopeptidase N (CD13) expressed on endothelial cells in tumor vessels. Upon deamidation of the NGR peptide moiety, this agent also binds to integrin alphaVbeta3 (aVb3; CD51/CD61) in the tumor vasculature. In turn, the tTF causes occlusion of the tumor blood vessels, which causes an inhibition of blood supply and flow in the tumor, nutrition and induced tumor cell death and an inhibition of tumor cell proliferation. TF plays a key role in the coagulation cascade. NGR is a asparagine-glycine-arginine containing peptide and ligand of CD13. Both aVb3 and CD13 are surface proteins that are upregulated on endothelial cells of tumor vessels.
Truphylline: (Other name for: aminophylline)
Truqap: (Other name for: capivasertib)
Truseltiq: (Other name for: infigratinib phosphate)
Truxima: (Other name for: rituximab)
tryptophanase: Encoded by human TDO2 Gene, 406-aa 48-kDa Tryptophanase is a homotetramer that may bind protoheme IV involved in tryptophan catabolism with broad specificity towards tryptamine and derivatives including tryptophan, 5-hydroxytryptophan, and serotonin.
TS-1: (Other name for: Tegafur-gimeracil-oteracil Potassium)
TSP-1 activator VT1021: A cyclic pentapeptide and stimulator of thrombospondin 1 (TSP-1; THBS1), with potential anti-angiogenic, immunomodulating and antineoplastic activities. Upon administration, TSP-1 activator VT1021 specifically stimulates TSP-1 expression in inflammatory myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment (TME), which binds to TSP-1 receptors, mainly CD36 and CD47. This activates CD36-mediated signaling and induces apoptosis in tumor and endothelial cells, which may result in the inhibition of tumor cell proliferation. The binding of TSP-1 to CD47 prevents the interaction between CD47 and the signal regulatory protein alpha (SIRPalpha; SIRPa) that is expressed on phagocytic cells. This prevents CD47/SIRPa-mediated signaling and abrogates the CD47/SIRPa-mediated inhibition of macrophage activation and phagocytosis of cancer cells. In addition, VT1021 can reprogram the immunosuppressive TME, skewing macrophages from the immune suppressive M2 phenotype to an effector M1 phenotype, increasing the infiltration of cytotoxic T lymphocytes (CTLs) while decreasing regulatory T cells (Tregs) in the TME, thereby stimulating an anti-tumor immune response and further killing tumor cells.
TSP-1 mimetic fusion protein CVX-045: A fusion protein containing two thrombospondin (TSP-1)-derived nonamer peptides covalently attached, via a proprietary diketone linker, to a proprietary humanized catalytic monoclonal aldolase monoclonal antibody with potential antiangiogenic and antineoplastic activities. The TSP-1 mimetic peptide moieties of TSP-1 mimetic fusion protein CVX-045 bind to TSP-1 receptors, such as CD36, and inhibit tumor angiogenesis, which may result in the inhibition of tumor cell proliferation. The proprietary humanized catalytic monoclonal aldolase monoclonal antibody contains reactive lysine residues in its binding sites, which react covalently with compounds having a diketone function; the TSP-1 mimetic peptide moieties are then covalently attached to the diketone linkers via a proprietary spacer.
TTI-237: A small synthetic molecule of triazolopyrimidine derivative with potential antitumor activity. With a novel mechanism of action distinct from the action of other vinca alkaloid compounds, TTI-237 specifically binds to tubulin at the vinca site, and promotes the polymerization of tubulin into microtubules. TTI-237 stabilizes tubulin and inhibits microtubule disassembly. This results in cell cycle arrest at the G2/M phase, and leading to cell death.
TTK/PLK1 inhibitor BAL0891: An inhibitor of threonine tyrosine kinase (TTK; monopolar spindle 1 kinase; Mps1) and polo-like kinase 1 (PLK1; PLK-1; STPK13), with potential mitotic checkpoint inhibiting (MCI) and antineoplastic activities. Upon administration, TTK/PLK1 inhibitor BAL0891 selectively targets, binds to and inhibits TTK and PLK1. This disrupts and inactivates the spindle assembly checkpoint (SAC), which results in chromosomal misalignment and missegregation, mitotic checkpoint complex destabilization, and induces G2/M-phase cell-cycle arrest, aberrant cell division and apoptosis in TTK- and PLK1-overexpressing tumor cells. PLK1, a serine/threonine kinase that is crucial for the activation of the mitotic SAC and regulation of mitosis, plays a key role in tumor cell proliferation, transformation and invasion. PLK1 expression is upregulated in a variety of tumor cell types and high expression is associated with increased aggressiveness and poor prognosis. TTK, a tyrosine and serine/threonine kinase expressed in proliferating normal tissues, is essential for proper SAC functioning, chromosome alignment and segregation. Overexpressed in various human tumors, TTK plays a key role in uncontrolled tumor cell growth.
tubercidin: An antibiotic and adenosine analog isolated from the bacterium Streptomyces tubercidicus with potential antineoplastic activity. Tubercidin is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.
tubulin inhibitor ALB 109564(a): A semi-synthetic derivative of the vinka alkaloid vinblastine with potential antineoplastic activity. Tubulin inhibitor ALB 109564(a) binds to tubulin monomers and inhibits microtubule formation, resulting in disruption of mitotic spindle assembly and arrest of tumor cells in the G2/M phase of the cell cycle.
tubulin inhibitor-containing antibody-drug conjugate: Any antibody-drug conjugate (ADC) that contains a tubulin inhibitor as the cytotoxic payload.
tubulin polymerization inhibitor AB8939: A small molecule tubulin polymerization inhibitor with potential antineoplastic activity. Upon administration, tubulin polymerization inhibitor AB8939 binds to tubulin and prevents its polymerization in tumor blood vessel endothelial cells and tumor cells. This blocks the formation of the mitotic spindle and leads to cell cycle arrest at the G2/M phase. As a result, this agent disrupts the tumor vasculature and tumor blood flow, deprives tumor cells of nutrients and induces tumor cell apoptosis. In addition, this agent has a direct cytotoxic effect on tumor cells by inhibiting tubulin polymerization. Additionally, unlike similar agents of this class, AB8939 may be able to circumvent some drug resistance mechanisms.
tubulin-binding agent SSR97225: An antimitotic tubulin-binding agent with potential antineoplastic activity. Tubulin-binding agent SSR97225 binds to tubulin, arresting the cell cycle at the G2/M checkpoint and preventing mitosis.
tucatinib: An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Tucatinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.
tucidinostat: An orally bioavailable benzamide-type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Upon administration, tucidinostat binds to and inhibits HDACs, leading to an increase of acetylation levels of histone proteins. This agent also inhibits the expression of kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide-type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life.
tucotuzumab celmoleukin: A recombinant fusion protein comprised of a human monoclonal antibody directed against the epithelial cell adhesion molecule (EpCAM or KS) linked to an active interleukin-2 (IL2) molecule with potential antineoplastic activity. The humanized monoclonal antibody moiety of tucotuzumab celmoleukin recognizes and binds to EpCAM, a cell surface epithelial protein that is expressed on a wide variety of cancer cells, thereby concentrating IL2 in EpCAM-expressing tumor tissue. Subsequently, the localized IL2 moiety of this fusion protein may stimulate a cytotoxic T-cell antitumor immune response.
Tukysa: (Other name for: tucatinib)
tulmimetostat: An orally available selective inhibitor of the histone lysine methyltransferase (HMT) enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral administration, tulmimetostat selectively targets, binds to and inhibits the activity of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, an HMT class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis.
tumor necrosis factor ligand superfamily member 10: Tumor necrosis factor ligand superfamily member 10 (281 aa, ~33 kDa) is encoded by the human TNFSF10 gene. This protein plays a role in the induction of apoptosis.
tumor peptide-loaded myeloid dendritic cells: A cell-based cancer vaccine composed of myeloid dendritic cells (myDCs) pulsed with tumor peptides with potential immunostimulatory and antineoplastic activities. Upon administration, the tumor peptide-loaded myDCs stimulate a specific cytotoxic T-lymphocyte (CTL) response against the tumor cells, resulting in tumor cell lysis.
tumor-cells apoptosis factor hormone-peptide: A synthetic 14-amino acid peptide derived from a novel human peptide hormone, Tumor-Cells Apoptosis Factor (TCApF), with potential antineoplastic activity. Upon intravenous administration, tumor-cells apoptosis factor hormone-peptide binds to the T1/ST2 receptor (IL1RL1) and activates both caspase 8 and Bcl-2 mediated apoptosis, in addition to the activation of p38 MAPK and JNK signaling cascades in tumor cells. Furthermore, this agent inhibits angiogenesis by suppressing the expressions of vascular endothelial growth factor A (VEGFA) and fms-related tyrosine kinase 1 (VEGFR1). Tumor-cells apoptosis factor hormone-peptide also modulates immune system responses via increasing the expressions of interleukin-10 and anti-angiogenic interleukin. T1/ST2 receptor, a member of the toll/interleukin-1 receptor superfamily, is overexpressed in certain cancer cells.
tunlametinib: An orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK), with potential antineoplastic activity. Upon administration, tunlametinib selectively binds to and inhibits the activity of MEK, preventing the activation of MEK-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a threonine/tyrosine kinase, plays a key role in the activation of the RAS/RAF/MEK/ERK pathway that regulates cell growth. This pathway is often dysregulated in a variety of tumor cell types through BRAF, KRAS and NRAS mutations.
Turalio: (Other name for: pexidartinib hydrochloride)
tusamitamab ravtansine: An immunoconjugate consisting of anti-carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5) conjugated to a cytotoxic agent, with potential antineoplastic activity. Upon administration of tusamitamab ravtansine the antibody moiety targets CEACAM5 on tumor cells. Upon antibody/antigen binding and internalization, the immunoconjugate releases the cytotoxic agent, which results in tumor cell death. CEACAM5, a member of the CEA family of proteins that plays a key role in cell migration, cell invasion, and cell adhesion, is overexpressed by a variety of cancer cell types.
tuvusertib: An orally available inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, tuvusertib selectively inhibits ATR activity and blocks the downstream phosphorylation of the serine/threonine protein kinase checkpoint kinase 1 (CHK1). This prevents ATR-mediated signaling, which results in the inhibition of DNA damage checkpoint activation, the disruption of DNA damage repair, and the induction of tumor cell apoptosis. ATR, a serine/threonine protein kinase upregulated in a variety of cancer cell types, plays a key role in DNA repair, cell cycle progression and survival. It is activated by DNA damage caused during DNA replication-associated stress.
Ty21a typhoid vaccine: A live attenuated bacteria oral vaccine used to prevent typhoid, which is caused by Salmonella typhi.
Tybost: (Other name for: cobicistat)
Tygacil: (Other name for: tigecycline)
Tykerb: (Other name for: lapatinib ditosylate)
Tylenol: (Other name for: acetaminophen)
Tymlos: (Other name for: abaloparatide)
type-1 polarized dendritic cell-induced antigen-specific autologous cytotoxic T lymphocytes: A preparation of autologous cytotoxic T lymphocytes (CTL), specifically reactive to melanoma-associated antigen 3 (MAGE-3), MAGE-4, survivin, human epidermal growth factor receptor 2 (HER2; ERBB2) and cyclooxygenase-2 (COX-2), with potential immunomodulating activity. Peripheral blood mononuclear cells (PBMCs) are collected from the patient. Subsequently, autologous dendritic cells (DCs) are separated, treated with a certain combination of cytokines to produce polarized type-1 DCs (DC1), and then are loaded with MAGE-3/MAGE-4/survivin/HER2/COX-2 CTL epitope peptides. In turn, autologous CTLs are collected, exposed ex vivo to the antigen-loaded DC1s and subsequently expanded in vitro. Upon re-infusion of the DC1-induced MAGE-3/MAGE-4/survivin/HER2/COX-2-specific autologous CTLs, the CTLs target and lyse tumor cells expressing the tumor-associated antigens (TAAs). Exposure to DC1s generates more potent CTLs and thus induces a more potent CTL response against TAA-expressing tumor cells. The targeted TAAs play key roles in cellular proliferation and are overexpressed by a variety of cancer cell types.
typhoid vaccine: A bacterial vaccine used to prevent typhoid fever, which is caused by Salmonella typhi bacteria.
tyroserleutide: A tripeptide consisting of tyrosine, serine, and leucine with potential antineoplastic activity. Although the mechanism of its antitumor activity has yet to be fully elucidated, tyroserleutide appears to inhibit the expression of ICAM-1 (CD54), a cell adhesion factor of the immunoglobulin (Ig) superfamily that plays an important role in the invasion, adhesion, and metastasis of tumor cells. In addition, this agent may influence the Ca2+/calmodulin pathway, inhibiting phosphatidylinositol 3 kinase (PI3K); PI3K is upregulated in tumor cells and is involved in cellular proliferation.
tyrosinase peptide: One of a number of recombinant peptides consisting of amino acid residues of the enzyme tyrosinase, a protein frequently expressed by melanoma cells. Vaccination with tyrosinase peptide may stimulate cytotoxic T lymphocyte response against tyrosinase-expressing tumor cells, resulting in decreased tumor growth.
tyrosinase-related protein-1: A recombinant peptide of the tyrosinase-related protein 1 (TRP1) used in vaccine therapy. Expressed by cells of melanocyte origin, TRP1 is an enzyme involved in the process that converts tyrosinase to melanin pigments. Vaccination with TRP1 may stimulate cytotoxic T cell responses to melanoma cells.
tyrosine kinase inhibitor IDRX-42: An orally bioavailable small molecule inhibitor of an as of yet undisclosed tyrosine kinase, with potential antineoplastic activity. Upon oral administration, tyrosine kinase inhibitor IDRX-42 inhibits the activity of an as of yet undisclosed tyrosine kinase. This may result in antitumor activity in tumor cells in which the tyrosine kinase is upregulated or dysregulated.
tyrosine kinase inhibitor OSI-930: A selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. Tyrosine kinase inhibitor OSI-930 inhibits stem cell factor receptor (c-Kit) and the vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of both tumor cell proliferation and tumor angiogenesis. Both c-Kit and VEGFR2 are overexpressed in a variety of cancers.
tyrosine kinase inhibitor TL-895: An orally bioavailable inhibitor of tyrosine kinase, with potential anti-inflammatory and antineoplastic activities. Upon oral administration, tyrosine kinase inhibitor TL-895 targets, binds to, and inhibits tyrosine kinase. This may result in the inhibition of tumor angiogenesis and cell proliferation, and the inhibition of immune-mediated inflammatory processes. Tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis. In addition, they play important roles in the activation of leukocytes and in many immune-mediated inflammatory and autoimmune conditions.
tyrosine kinase inhibitor XL228: A synthetic molecule that targets multiple tyrosine kinases with potential antineoplastic activity. Tyrosine kinase inhibitor XL228 binds to and inhibits the activities of multiple tyrosine kinases, such as the insulin-like growth factor 1 receptor (IGF1R), Src tyrosine kinase, and Bcr-Abl tyrosine kinase. Blockade of these kinases may result in the inhibition of tumor angiogenesis, cell proliferation, and metastasis. In addition, this agent may be a potent inhibitor of the T315I mutant form of the Abl protein, which is associated with the resistance of chronic myelogenous leukemia (CML) to other tyrosine kinase inhibitors. IGF1R and Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis. Bcr-Abl translocation leads to constitutive activation of ABL kinase and is commonly associated with Philadelphia-positive acute lymphocytic leukemia (ALL).
Tysabri: (Other name for: natalizumab)
Tyzeka: (Other name for: telbivudine)