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NCI Drug Dictionary

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452 results found for: I

I 131 monoclonal antibody CC49
A radioimmunoconjugate of the humanized monoclonal antibody CC49 labeled with iodine I 131. Iodine I 131 monoclonal antibody CC49 delivers beta and gamma radiation-emitting I 131 radionuclide specifically to tumor cells that express tumor-associated glycoprotein (TAG)-72, allowing localization of TAG-72-expressing tumor cells with radioimaging devices in diagnostic applications or resulting in specific TAG-72-expressing tumor cell radiocytotoxicity in therapeutic applications. Monoclonal antibody CC49 binds to TAG-72, a pancarcinoma antigen, with high affinity.
I 131 monoclonal sntibody F19
A radioimmunoconjugate of a murine monoclonal antibody (MoAb) F19 labelled with Iodine 131 (I-131). MoAb F19 was raised against fibroblast activation protein (FAP), which is highly expressed by tumor stromal cells. Using MoAb F19 as a carrier for I-131 results in the targeted imaging and/or destruction of cells overexpressed FAP.
iadademstat
An orally available inhibitor of lysine specific histone demethylase 1 (KDM1A; LSD1), with potential antineoplastic activity. Upon administration, iadademstat binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9, which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family, is overexpressed in certain tumor cells and plays a key role in in the regulation of gene expression, tumor cell growth and survival.
ianalumab
A fully human combinatorial antibody library (HuCAL)-derived monoclonal antibody targeting the B-cell-activating factor receptor (BAFF-R), with potential anti-inflammatory and antineoplastic activities. Upon administration, ianalumab targets and binds to BAFF-R, which inhibits both BAFF/BAFF-R interaction and BAFF-R-mediated signaling. This may decrease cell growth in tumor cells expressing BAFF-R. BAFF-R, also known as tumor necrosis factor receptor superfamily member 13C, is overexpressed in certain tumor cell types and autoimmune diseases. In cancer cells, BAFF-R plays a key role in B-cell proliferation and survival. VAY736 was developed using HuCAL technology.
IAP antagonist TQB3728
An orally bioavailable, second mitochondria-derived activator of caspases (SMAC)-mimetic and an antagonist of inhibitor of apoptosis proteins (IAPs), with potential apoptosis-inducing and antineoplastic activities. Upon oral administration, IAP antagonist TQB3728 selectively targets, binds to and inhibits the activity of IAPs including X chromosome-linked IAP (XIAP) and cellular IAPs 1 (c-IAP1) and 2 (c-IAP2). This may restore and promote the induction of apoptosis through apoptotic signaling pathways and enhance proteasomal degradation of IAPs. Additionally, TQB3728 may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.
IAP inhibitor APG-1387
A small molecule, second mitochondria-derived activator of caspases (SMAC)-mimetic targeting inhibitor of apoptosis proteins (IAPs) with potential apoptosis-inducing and antineoplastic activities. Upon administration, IAP inhibitor APG-1387 selectively binds to and inhibits the activity of IAPs including X chromosome-linked IAP (XIAP) and cellular IAPs 1 (c-IAP1) and 2 (c-IAP2). This may restore and promote the induction of apoptosis through apoptotic signaling pathways and enhance proteasomal degradation of IAPs. Additionally, APG-1387 may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.
IAP inhibitor HGS1029
The hydrochloride salt of a small-molecule inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins with potential antineoplastic activity. IAP inhibitor HGS1029 selectively inhibits the biological activity of IAP proteins, which may restore apoptotic signaling pathways; this agent may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.
iAPA-based dendritic cells/cytotoxic T lymphocytes
A cell-based product composed of dendritic cells (DCs) pulsed with tumor-associated antigens (TAAs) and devoid of the inhibitory effect of antigen presentation attenuators (iAPA) combined with cytotoxic T-lymphocytes (CTLs) (iAPA-DC/CTL), with potential immunostimulating and antineoplastic activities. DCs are transduced with a viral vector containing small interfering RNAs (siRNAs) against APAs, which prevents the expression of APA genes and inhibits attenuation of antigen presentation. Upon administration of iAPA-DC/CTL, the DCs are able to efficiently present antigens to the immune system, stimulate the immune system against tumor-associated antigens (TAAs) and hyperactivate TAA-specific CTLs and T-helper cells. Also, the iAPA-based DCs inhibit the activity of the T-regulatory cells (Tregs), thereby abrogating their negative effect on CTL activation and preventing their immunosuppressive activity against TAAs. Altogether, this inhibits tumor cell proliferation. Additionally, the administered CTLs induce direct cancer cell lysis. APAs negatively regulate antigen presentation, activate Tregs and their immunosuppressive activity, affect inflammatory cytokine production by DCs, and negatively regulate the immunostimulatory activity of DCs; they have an overall inhibitory effect on the stimulation of the immune system.
ibandronate sodium
The sodium salt of ibadronic acid, a synthetic nitrogen-containing bisphosphonate. Ibandronic acid inhibits farnesyl pyrophosphate synthase, resulting in a reduction in geranylgeranyl GTPase signaling proteins and apoptosis of osteoclasts. This agent increases bone mineral density, decreases bone remodeling, inhibits osteoclast-mediated bone resorption, and reduces metastases-related and corticosteroid-related bone pain.
ibcasertib
An orally available, small molecule inhibitor of select serine-threonine kinases, including aurora kinase B (aurora B), vascular endothelial growth factor receptors (VEGFRs), stem cell factor receptor (c-KIT), and platelet-derived growth factor receptors (PDGFRs), with potential antineoplastic activity. Upon oral administration, ibcasertib binds to and inhibits the activity of aurora B, VEGFRs, c-kit and PDGFRs, which may result in a decrease in the proliferation of tumor cells that overexpress these kinases. These kinases are overexpressed by a variety of cancer cell types.
iberdomide
A modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with immunomodulating and pro-apoptotic activities. Upon administration, iberdomide specifically binds to the cereblon (CRBN) part of the ligase complex, thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3) which are transcriptional repressors in T cells. This leads to a reduction of their protein levels, and the modulation of the immune system, including activation of T lymphocytes. In addition, this leads to a downregulation of other proteins, including interferon regulatory factor 4 (IRF4), which plays a key role in the proliferation of certain cancer cell types. CRBN, the substrate recognition component of the E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.
iberdomide hydrochloride
The hydrochloride salt form of iberdomide, a modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and pro-apoptotic activities. Upon administration, iberdomide specifically binds to the cereblon (CRBN) part of the ligase complex, thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3) which are transcriptional repressors in T cells. This leads to a reduction of their protein levels, and the modulation of the immune system, including activation of T lymphocytes. In addition, this leads to a downregulation of other proteins, including interferon regulatory factor 4 (IRF4), which plays a key role in the proliferation of certain cancer cell types. CRBN, the substrate recognition component of the E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.
IBgard
(Other name for: peppermint oil-containing enteric-coated microspheres)
Ibrance
(Other name for: Palbociclib)
ibrexafungerp
An intravenous and orally bioavailable semisynthetic derivative of enfumafungin with potential antifungal activity. Upon administration, ibrexafungerp inhibits beta-1,3-D-glucan synthase, an enzyme essential for fungal cell wall synthesis. This results in weakening of the fungal cell wall, thereby leading to osmotic lysis and eventually fungal cell death.
ibritumomab tiuxetan
An immunoconjugate of the monoclonal antibody ibritumomab conjugated with the linker-chelator tiuxetan, a high affinity, conformationally restricted chelation site for radioisotopes. When bound to indium In 111 or yttrium Y 90, ibritumomab tiuxetan, targeting the CD20 antigen on B cell surfaces, specifically delivers a potentially cytotoxic dose of radiation to B lymphocytes. Ibritumomab is a murine IgG1 kappa monoclonal antibody directed against the CD20 antigen, which is found on the surface of normal and malignant B lymphocytes.
Ibrutinib
An orally bioavailable, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon oral administration, ibrutinib binds to and irreversibly inhibits BTK activity, thereby preventing both B-cell activation and B-cell-mediated signaling. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is required for B cell receptor signaling, plays a key role in B-cell maturation, and is overexpressed in a number of B-cell malignancies. The expression of BTK in tumor cells is also associated with increased proliferation and survival.
ibudilast
An orally bioavailable inhibitor of cyclic nucleotide phosphodiesterase (PDE), mainly PDE-3, -4, -10, and -11, with anti-(neuro)inflammatory, vasorelaxant, bronchodilator, analgesic, neuroprotective and potential anti-tumor activities. Ibudilast (IBD) is able to cross the blood-brain barrier (BBB). Upon administration, IBD exerts its potential anti-tumor activity against glioblastoma multiforme (GBM) cells by inhibiting PDE-4 and the pro-inflammatory cytokine macrophage migration inhibitory factor (MIF), which results in a decrease in MIF, its receptor CD74, and AKT expression, and attenuates the immunosuppressive properties of monocytic myeloid-derived suppressor cells (MDSCs) and reduces T-regulatory cells (Tregs). This causes GBM cell apoptosis and inhibits GBM cell proliferation. In addition, IBD reduces, through its inhibitory effect on various PDEs, the production of certain pro-inflammatory cytokines, such as interleukin-6 (IL-6), IL- 1beta, leukotriene B4, and tumor necrosis factor-alpha (TNF-a). IBD also upregulates the anti-inflammatory cytokine (IL-10), and promotes the production of neurotrophic factors, such as brain-derived neurotrophic factor (BDNF), nerve growth factor (NGF), and neurotrophin-4 (NT-4). It also blocks toll-like receptor-4 (TLR-4), inhibits nitric oxide (NO) synthesis and reduces the level of reactive oxygen species (ROS). It also prevents platelet aggregation, causes cerebral vasodilation, bronchial smooth muscle relaxation, and improves cerebral blood flow. In addition, IBD attenuates the PDE-mediated activation of glial cells and abrogates PDE-mediated neuroinflammation and neurodegeneration. MIF is secreted by cancer stem cells (CSCs) and is highly expressed within GBM and plays a key role in tumor cell proliferation. Co-expression of MIF and CD74 in GBM is associated with poor patient survival.
ibuprofen
A propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. This leads to decreased prostaglandin synthesis, by prostaglandin synthase, the main physiologic effect of ibuprofen. Ibuprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.
ibuprofen injection
A formulation for intravenous injection containing ibuprofen, a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID), with anti-inflammatory, analgesic, and antipyretic activities. Upon intravenous injection, ibuprofen inhibits the activity of the enzymes cyclooxygenase I (COX-1) and II (COX-2), resulting in a decreased formation of precursors of prostaglandins and thromboxanes. Inhibition of COX-2 specifically blocks the conversion of arachidonic acid (AA) to prostaglandins, which mediate inflammation, fever and pain.
IC-GREEN
(Other name for: indocyanine green solution)
iC9-GD2-CAR-CD28-OX40-expressing autologous NKT cells
A preparation of autologous interleukin-15 (IL-15)-expressing natural killer T cells (NKT) transduced with a retroviral vector encoding a chimeric antigen receptor (CAR) derived from the antibody 14G2a that recognizes disialoganglioside GD2 (GD2-CAR) that is coupled to the co-stimulatory domains of CD28 and OX40 (CD134), and to the zeta chain of the TCR/CD3 complex (CD3-zeta), and linked to the suicide gene inducible caspase 9 (iCasp9 or iC9), with potential immunomodulating and antineoplastic activities. Upon transfusion, the iC9-GD2-CAR-CD28-OX40-expressing autologous NKT cells recognize, bind to and induce selective cytotoxicity in GD2-expressing tumor cells. The tumor-associated antigen (TAA) GD2 is overexpressed on the surface of neuroblastoma cells and by other neuroectoderm-derived neoplasms, while it is minimally expressed on normal, healthy cells. The iCasp9 safety switch consists of a full-length caspase 9, including its caspase recruitment domain, linked to a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V). If the administered NKT cells lead to unacceptable side effects, the chemical homodimerizer AP1903, which binds to the FKBP12-F36V drug-binding domain, activates caspase 9, and results in apoptosis of the administered NKT cells, can be administered.
iC9-GD2-CD28-OX40-expressing T lymphocytes
Modified T-lymphocytes expressing a 3rd generation chimeric antigen receptor (CAR) specific for the disialoganglioside GD2, which contains the CD3zeta chain, the signaling domains of the co-stimulatory molecules CD28 and CD134 (OX-40) and the suicide gene inducible caspase 9 (iCasp9), with potential immunomodulating and antineoplastic activities. Upon administration, iC9-GD2-CD28-OX40-expressing T lymphocytes target the GD2 antigen on tumor cells, thereby providing selective toxicity towards GD2-expressing tumor cells. iCasp9 consists of a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V) linked to human caspase 9. If the administered T cells lead to unacceptable side effects, the chemical homodimerizer AP1903 can be administered, which binds to the drug binding FKBP12-F36V domain and activates caspase 9, resulting in the apoptosis of the administered T-cells. The tumor-associated antigen GD2 is overexpressed on the surface of almost all tumors of neuroectodermal origin. OX40 and CD28, both T-cell surface-associated co-stimulatory molecules, are required for full T-cell activation.
icatibant
An antagonist of the human bradykinin B2 receptor (B2R), that can be used for the treatment of hereditary angioedema (HAE). Upon administration, icatibant targets and binds to B2R, thereby preventing bradykinin from binding to the B2R. This may prevent bradykinin/B2R-mediated vasodilation, the resulting increase in vascular permeability, and the swelling, inflammation, and pain associated with HAE. This may also prevent or improve pulmonary edema not associated with HAE and improve the associated decrease in blood oxygen levels.
ICE regimen
A regimen consisting of carboplatin, etoposide and ifosfamide that can be used in the treatment of non-Hodgkin and Hodgkin lymphomas, including diffuse large B-cell lymphoma and T-cell lymphoma, mycosis fungoides/Sezary syndrome, and gestational trophoblastic neoplasia. Paclitaxel/carboplatin/oral etoposide regimen can be used for the treatment of occult primary adenocarcinoma.
Iclusig
(Other name for: ponatinib hydrochloride)
icodextrin solution
An isosmotic solution containing icodextrin, a starch-derived, water-soluble glucose polymer, used in peritoneal dialysis and for the prevention of adhesion after surgery. Due to its isoosmotic nature and inability to cross the peritoneal membrane, the icodextrin solution, upon administration into the peritoneal cavity, is able to exert osmotic pressure. This allows for the removal of excess fluids and waste products in dialysis patients. In addition, icodextrin can provide a barrier between tissue surfaces when administered during surgery. This physically separates tissues, prevents adhesion after surgery and promotes wound healing.
icosapent
The free fatty acid (FFA) form of eicosapentaenoic acid (EPA), a polyunsaturated long-chain fatty acid found in fish oil with a 20-carbon backbone and 5 double bonds, with potential supplementing, anti-inflammatory, anti-thrombotic, immunomodulating, anti-angiogenic and chemopreventive activities. Upon administration of icosapent, the free form of EPA is incorporated in cell membrane phospholipids and replaces arachidonic acid. This inhibits arachidonic acid conversion into thromboxanes and prostaglandin E2 (PGE2). Upon oral administration of icosapent, the EPA-FFA prevents and suppresses colonic neoplasia and reduces polyp formation and growth through as of yet not fully elucidated mechanisms.
icotinib hydrochloride
The hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, has been upregulated in a variety of cancer cell types.
icrucumab
A fully human IgG1 monoclonal antibody directed against human vascular endothelial growth factor receptor 1 (VEGFR-1/FLT-1) with potential antiangiogenesis and antineoplastic activities. Icrucumab specifically binds to and inhibits the activity of VEGFR-1, which may prevent the activation of downstream signaling pathways and so inhibit tumor angiogenesis; the subsequent reduction in tumor nutrient supply may inhibit tumor cell proliferation. Tumor cell overexpression of VEGFR-1 may be associated with tumor angiogenesis and tumor cell proliferation and invasion; VEGFR-1 may modulate VEGFR-2 signaling.
Idamycin
(Other name for: idarubicin hydrochloride)
Idamycin PFS
(Other name for: idarubicin hydrochloride)
idarubicin hydrochloride
The hydrochloride salt of the anthracycline antineoplastic antibiotic idarubicin. Idarubicin intercalates into DNA and inhibits topoisomerase II, thereby inhibiting DNA replication and ultimately, interfering with RNA and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes more efficiently than other anthracycline antibiotic compounds
idarubicin-eluting beads
A sustained-release drug delivery embolization system containing small polymeric beads impregnated with the anthracycline antibiotic idarubicin with potential antineoplastic activity. The beads consist of polyvinyl alcohol (PVA) microspheres modified with sulfonic acid groups and loaded with idarubicin. During transarterial chemoembolization (TACE) in the hepatic artery, idarubicin-eluting beads embolize to the tumor vasculature, occlude tumor blood vessels and induce ischemic necrosis of tumor tissue due to mechanical blockage of the tumor vasculature. Simultaneously, idarubicin-eluting beads release cytotoxic idarubicin locally and in a sustained manner. This may result in idarubicin-mediated inhibition of tumor cell proliferation.
idasanutlin
An orally available, small molecule, antagonist of MDM2 (mouse double minute 2; Mdm2 p53 binding protein homolog), with potential antineoplastic activity. Idasanutlin binds to MDM2 blocking the interaction between the MDM2 protein and the transcriptional activation domain of the tumor suppressor protein p53. By preventing the MDM2-p53 interaction, p53 is not enzymatically degraded and the transcriptional activity of p53 is restored. This may lead to p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger nuclear phosphoprotein and negative regulator of the p53 pathway, is often overexpressed in cancer cells and has been implicated in cancer cell proliferation and survival.
idecabtagene vicleucel
A preparation of autologous peripheral blood T lymphocytes (PBTLs) that have been genetically modified to express a chimeric antigen receptor (CAR) specific for the B-cell maturation antigen (BCMA), with potential immunostimulating and antineoplastic activities. Upon administration, idecabtagene vicleucel specifically recognizes and kills BCMA-expressing tumor cells. BCMA, a tumor-specific antigen and a receptor for both a proliferation-inducing ligand (APRIL) and B-cell activating factor (BAFF), is a member of the tumor necrosis factor receptor superfamily (TNFRSF) and plays a key role in plasma survival; it is found on the surfaces of plasma cells and overexpressed on malignant plasma cells.
idelalisib
An orally bioavailable, small molecule inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Idelalisib inhibits the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), preventing the activation of the PI3K signaling pathway and inhibiting tumor cell proliferation, motility, and survival. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in hematopoietic lineages. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells.
IDH1 inhibitor KY100001
An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble) mutant forms, with potential antineoplastic activity. Upon administration, IDH1 inhibitor KY100001 specifically binds to and inhibits certain mutant forms of IDH1, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH1 mutations. IDH1 mutations are highly expressed in certain malignancies; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.
IDH1 inhibitor TQB3454
An orally bioavailable, small molecule inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble) mutant forms, with potential antineoplastic activity. Upon oral administration, IDH1 inhibitor TQB3454 specifically binds to and inhibits certain mutant forms of IDH1, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH1 mutations. IDH1 mutations are highly expressed in certain malignancies; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.
IDH1(R132) inhibitor IDH305
An inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity. Upon administration, IDH305 specifically inhibits IDH1(R132) mutant forms in the cytoplasm, which inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1(R132)-expressing tumor cells. IDH1(R132) mutations are highly expressed in certain malignancies, including gliomas. They initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.
IDH1R132H mutation-targeting IDH1 peptide vaccine
A peptide vaccine consisting of a 20-mer peptide derived from isocitrate dehydrogenase type 1 (IDH1) containing the point mutation R132H (IDH1R132H), with potential antineoplastic activity. Upon subcutaneous vaccination with the IDH1R132H mutation-targeting IDH1 peptide vaccine, the vaccine stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells that express the IDH1R132H protein. R132H is a point mutation, which contains an amino acid substitution where arginine is replaced by histidine at position 132 of IDH1, and is highly expressed in gliomas as well as other tumor types; this mutation is associated with increased production of the oncometabolite R-2-hydroxyglutarate (2HG).
IDH1R132H-specific peptide vaccine PEPIDH1M
A peptide vaccine consisting of a peptide derived from isocitrate dehydrogenase 1 (IDH1) containing the point mutation R132H (IDH1R132H), with potential antineoplastic activity. Intradermal vaccination with the IDH1R132H-specific peptide vaccine PEPIDH1M may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the IDH1R132H protein. The IDH1 point mutation of amino acid residue 132 is highly expressed in gliomas and is associated with increased production of the oncometabolite R-2-hydroxyglutarate (2HG).
IDH2 mutant inhibitor SH1573
An orally bioavailable inhibitor of mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2; IDH-2) R140Q mutant, with potential antineoplastic activity. Upon oral administration, IDH2 mutant inhibitor SH1573 specifically inhibits mutant IDH2 (mIDH2) R140Q protein, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mIDH2 R140Q. IDH2 is mutated in a variety of cancers, and mutated IDH2 initiates and drives cancer growth by catalyzing the formation of 2HG and blocking cell differentiation.
IDH2 mutant inhibitor TQB3455
An orally bioavailable inhibitor of mutated mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2; IDH-2), with potential antineoplastic activity. Upon oral administration, IDH2 mutant inhibitor TQB3455 specifically inhibits mutated IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing mutated IDH2. IDH2 is mutated in a variety of cancers, and mutated IDH2 initiate and drive cancer growth by catalyzing the formation of 2HG and blocking cell differentiation.
Idhifa
(Other name for: enasidenib mesylate)
idiotype-pulsed autologous dendritic cell vaccine APC8020
A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with tumor-derived clonal immunoglobulin (Ig) with potential immunostimulatory and antineoplastic activities. Upon administration, idiotype-pulsed autologous dendritic cell vaccine APC8020, containing idiotype (Id) protein structures that can be recognized by antibodies and by CD41 T lymphocytes and CD81 T lymphocytes, may stimulate antitumoral cytotoxic T lymphocyte (CTL) and antibody responses against Id-expressing tumor cells. The Id represents the unique antigenic determinants in the variable regions of the clonal Ig.
IDO peptide vaccine IO102
A second-generation peptide vaccine derived from the immunomodulatory enzyme indoleamine 2,3-dioxygenase (IDO) with potential immunomodulating and antineoplastic activities. Vaccination with IDO peptide vaccine IO102 may activate the immune system to induce an immune response against IDO-expressing tumor cells. This may restore the proliferation and activation of various immune cells including cytotoxic T lymphocytes (CTLs), natural killer cells (NKs), and dendritic cells (DCs), and may eradicate IDO-expressing tumor cells through a CTL-mediated response. IDO, a cytosolic enzyme responsible for tryptophan catabolism and conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs) and plays an important role in immunosuppression mainly through suppression of CTL activation.
IDO-1 inhibitor LY3381916
An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor LY3381916 specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, LY3381916 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells, thereby inhibiting the growth of IDO1-expressing tumor cells. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
IDO-1 inhibitor PF-06840003
An orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor PF-06840003 targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, PF-06840003 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes; PF-06840003 also induces increased interferon (IFN) production, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1, a cytosolic enzyme responsible for tryptophan catabolism and the conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs); it plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
IDO/TDO inhibitor HTI-1090
An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1) and the kynurenine-producing hepatic enzyme tryptophan 2,3-dioxygenase (TDO), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1/TDO inhibitor HTI-1090 specifically targets and binds to both IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine, and TDO, a hepatic enzyme catalyzing the first step of tryptophan degradation. By inhibiting IDO1 and TDO, HTI-1090 decreases kynurenine levels in tumor cells, restores tryptophan and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells and T lymphocytes. This reduces the number of tumor-associated regulatory T cells (Tregs) and activates the immune system to induce a cytotoxic T-lymphocyte (CTL) response against the IDO1/TDO-expressing tumor cells, thereby inhibiting the growth of the tumor cells. IDO1 and TDO, both overexpressed by multiple tumor cell types, play important roles in immunosuppression and the promotion of tumor cell survival and proliferation. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
IDO/TDO inhibitor LY-01013
An orally bioavailable, small-molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1) and the kynurenine-producing hepatic enzyme tryptophan 2,3-dioxygenase (TDO), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1/TDO inhibitor LY-01013 specifically targets and binds to both IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine, and TDO, a hepatic enzyme catalyzing the first step of tryptophan degradation. By inhibiting IDO1 and TDO, LY-01013 decreases kynurenine levels in tumor cells, restores tryptophan and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells and T lymphocytes. This reduces the number of tumor-associated regulatory T cells (Tregs) and activates the immune system to induce a cytotoxic T-lymphocyte (CTL) response against the IDO1/TDO-expressing tumor cells, thereby inhibiting the growth of the tumor cells. IDO1 and TDO, both overexpressed by multiple tumor cell types, play important roles in immunosuppression and the promotion of tumor cell survival and proliferation. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
IDO1 inhibitor
Any agent that inhibits the activity of the enzyme indoleamine 2,3-dioxygenase 1 (IDO1; IDO).
IDO1 inhibitor KHK2455
An orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1 inhibitor KHK2455 targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, KHK2455 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes; KHK2455 also induces increased interferon (IFN) production, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1, a cytosolic enzyme responsible for tryptophan catabolism and the conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs); it plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
IDO1 inhibitor RiMO-401
An inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1), with potential immunomodulating and antineoplastic activities. Upon intra-tumoral administration, IDO1 inhibitor RiMO-401 specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, RiMO-401 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Re-activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against the IDO1-expressing tumor cells, thereby inhibiting the growth of IDO1-expressing tumor cells. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system.
IDO1/TDO2 inhibitor DN1406131
An inhibitor of both the enzymes indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1) and tryptophan 2,3-dioxygenase 2 (TDO2; TDO-2), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1/TDO2 inhibitor DN1406131 targets, binds to and inhibits both IDO1 and TDO2, which catalyze the first and rate-limiting step in the production of the immunosuppressive transcription factor aryl hydrocarbon receptor (AhR) ligand kynurenine (KYN). This inhibits the IDO1/TDO2-KYN-AhR pathway. Abrogation of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs) and regulatory T cells (Tregs) in the tumor microenvironment (TME). This may restore the immune response against tumor cells in which IDO1 and/or TDO2 are overexpressed. The IDO1/TDO2-KYN-AhR pathway is overexpressed in a variety of tumor cell types, plays a key role in immunosuppression and its expression is correlated with poor prognosis.
IDO1/TDO2 inhibitor M4112
An inhibitor of both the enzymes indoleamine 2,3-dioxygenase 1 (IDO1; IDO-1) and tryptophan 2,3-dioxygenase 2 (TDO2; TDO-2), with potential immunomodulating and antineoplastic activities. Upon administration, IDO1/TDO2 inhibitor M4112 targets, binds to and inhibits both IDO1 and TDO2, which catalyze the first and rate-limiting step in the production of the immunosuppressive transcription factor aryl hydrocarbon receptor (AhR) ligand kynurenine (Kyn). This inhibits the IDO1/TDO2-KYN-AhR pathway. Abrogation of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs) and regulatory T cells (Tregs) in the tumor microenvironment (TME). This may restore the immune response and may stimulate cytotoxic T-lymphocyte (CTL) immune response against tumor cells in which IDO1 and/or TDO2 are overexpressed. The IDO1/TDO2-KYN-AhR pathway is overexpressed in a variety of tumor cell types and plays a key role in immunosuppression. Its expression is correlated with poor prognosis.
idoxuridine
An iodinated analogue of deoxyuridine, with antiviral activity against herpes simplex virus (HSV) and potential radiosensitizing activities. Upon ocular administration, idoxuridine (IUdR) is converted to its mono-, di-, and triphosphate forms, is incorporated into DNA and disrupts viral replication. Upon oral administration of the idoxuridine prodrug ropidoxuridine and hepatic conversion by aldehyde oxidase into idoxuridine, this agent incorporates into DNA and sensitizes cells to ionizing radiation by increasing DNA strand breaks.
idronoxil
A synthetic flavonoid derivative. Idronoxil activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death.
idronoxil suppository NOX66
A proprietary, suppository-based formulation composed of idronoxil, a synthetic flavonoid derivative, surrounded by a proprietary lipid that protects idronoxil from phase 2 degradation, with potential chemo- and radio-sensitizing activities. Upon administration, idronoxil blocks the activity of ecto-NOX disulfide-thiol exchanger 2 (ENOX2; tNOX), a tumor-specific external NADH oxidase that maintains the transmembrane electron potential across the plasma membrane and is overexpressed in certain cancer cell types while absent in normal, healthy cells. Loss of this potential directly inhibits certain pro-survival signal transduction pathways, such as the PARP1/PI3 kinase/Akt signaling pathway. The inhibition of these pathways prevents resistance to standard chemo- and radio-therapy and makes tumor cells more susceptible to the anti-tumor activity of conventional chemotherapeutic agents and radiotherapy. The formulation prevents detoxification of idronoxil to an inactive form by bypassing phase 2 metabolism; this increases idronoxil’s bioavailability as compared to idronoxil alone.
idroxioleic acid
An orally bioavailable, synthetic analog of the fatty acid oleic acid, with potential antitumor activity. Upon administration,idroxioleic acid activates sphingomyelin synthase (SMS), thereby increasing the concentration of sphingomyelin (SM) and diacylglycerol (DAG) in the tumor cell membrane and decreasing membrane levels of phosphatidylethanolamine (PE) and phosphatidylcholine (PC). This restores the normal, healthy levels and ratios of membrane lipids. By restoring normal membrane lipid structure and composition, this agent inhibits membrane-protein associated signaling and the aberrant activity of signaling pathways in certain tumor cells, including the Ras/MAPK and PI3K/AKt pathways. This inhibits tumor cell proliferation, induces tumor cell differentiation, and eventually can cause cell death.
iduronicrin genleukocel-T
A preparation of autologous plasmablasts genetically engineered to express alpha-L-iduronidase (IDUA; laronidase) using the Sleeping Beauty (SB) transposon system, that may potentially be used for enzyme replacement therapy for Mucopolysaccharidosis type I (MPS I; Hurler syndrome). Upon administration, iduronicrin genleukocel-T expresses and replaces IDUA. IDUA, an enzyme required for the lysosomal degradation of glycosaminoglycans (GAGs), hydrolyzes the non-reducing terminal alpha-L-iduronic acid residues in GAGs, including dermatan sulfate and heparan sulfate. IDUA deficiency causes accumulations of heparan sulfate and dermatan sulfate in various tissues of the body which leads to progressive damage. Mutations in the IDUA gene are responsible for the deficiency of IDUA.
ifebemtinib
An orally bioavailable inhibitor of the non-receptor, cytoplasmic tyrosine kinase protein tyrosine kinase 2 (focal adhesion kinase 1; FAK1; FAK: PTK2) with potential antineoplastic activity. Upon oral administration, ifebemtinib targets and inhibits, in an adenosine triphosphate (ATP)-competitive manner, PTK2. This prevents PTK2-mediated downstream signaling and inhibits migration, proliferation, invasion, and survival in PTK2-overexpressing tumor cells. The cytoplasmic tyrosine kinase PTK2, a signal transducer for integrins overexpressed in various tumor cell types, is involved in tumor cell invasion, migration and proliferation.
ifetroban sodium
The sodium salt form of ifetroban, an orally bioavailable thromboxane (TxA2) and prostaglandin H2 (PGH2) (TP) receptor antagonist, with anti-thrombotic, anti-hypertensive, anti-asthmatic and potential anti-metastatic activities. Upon administration, ifetroban targets and binds to TxA2 and PGH2 receptors, thereby preventing the activity of both TxA2 and PGH2 and disrupting their downstream signaling pathways. This prevents platelet activation, aggregation and thrombosis. It also prevents vascular constriction and causes vasodilation. In addition, as cancer cells use platelets to metastasize to different parts of the body, ifetroban can reduce the stickiness of the platelets and prevent metastasis. TxA2 causes vascular contraction and platelet activation.
Ifex
(Other name for: ifosfamide)
ifinatamab deruxtecan
An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against the immunoregulatory protein B7-homologue 3 (B7-H3, CD276) conjugated, via an enzymatically cleavable tetrapeptide-based linker, to the cytotoxic DNA topoisomerase I inhibitor and exatecan (DX-8951) derivative DXd (MAAA-1181a; MAAA-1181), with potential antineoplastic activity. Upon administration of the anti-B7-H3/DXd ADC DS-7300a, the anti-B7-H3 antibody targets and binds to B7-H3-expressing tumor cells. Upon cellular uptake and lysosomal degradation of the linker, DXd targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication and apoptosis. This inhibits the proliferation of B7-H3-expressing tumor cells. B7-H3, a type I transmembrane protein and a member of the B7 co-stimulatory protein superfamily, is overexpressed on certain tumor cell types and on various immune cells. It plays a key role in tumor growth and immune responses. The ADC allows for reduced systemic exposure and enhanced delivery of the cytotoxic agent DXd.
ifosfamide
A synthetic analogue of the nitrogen mustard cyclophosphamide with antineoplastic activity. Ifosfamide alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.
Ifupinostat Hydrochloride
The hydrochloride salt form of ifupinostat,, an inhibitor of both phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon administration, ifupinostat binds to and inhibits the activity and mediated signaling of both PI3K and HDAC. In addition, ifupinostat may also inhibit other signaling pathways. This may prevent growth of PI3K and/or HDAC-expressing tumor cells.
IGF-1R antagonist BMS-754807
An oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity. Dual IGF-IR/InsR inhibitor BMS-754807 binds reversibly to and inhibits the activities of IGF-1R and InsR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R and InsR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in mitogenesis, angiogenesis, and tumor cell survival.
IGF-1R antisense oligodeoxynucleotide-treated autologous glioma cells IGV-001
A preparation of irradiated autologous glioma cells treated ex vivo with IMV-001, an antisense oligodeoxynucleotide of insulin-like growth factor receptor 1 (IGF-1R/AS ODN), and encapsulated within bio-diffusion chambers, with potential antineoplastic activity. The IGF-1R/AS ODN IMV-001-treated autologous glioma cells IGV-001 are encapsulated within implantable and removable bio-diffusion chambers with additional IMV-001, irradiated, and implanted into the patient. The IGF-1R/AS ODN binds to IGF-1R mRNA in glioma cells, and shuts down the translation of IGF-1R in the glioma cells. Downregulation of IGF-1R, in addition to irradiation, induces apoptosis and causes the release of exosomes, which contain tumor-associated antigens (TAAs). The diffusion of exosomes together with the additional IMV-001 from the bio-diffusion chambers may activate the patient's immune system and mount a cytotoxic T-lymphocyte (CTL) response against cells expressing these TAAs. IGF-1R, a receptor tyrosine kinase, is overexpressed in a variety of tumor cell types and is essential for tumor cell growth, transformation and survival.
IGF-1R inhibitor PL225B
An orally bioavailable inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. IGF-1R inhibitor PL225B selectively binds to and inhibits the activities of IGF-1R, which may result in both the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis in IGF-1R-overexpressing tumor cells. IGF-1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a significant role in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.
IGF-1R/IR inhibitor KW-2450
An orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.
IGF-methotrexate conjugate
A conjugate containing the antimetabolite and antifolate agent methotrexate conjugated to insulin-like growth factor (IGF), with potential antineoplastic activity. After intravenous administration, the IGF moiety of the IGF-methotrexate conjugate binds to and is internalized by IGF receptors (IGFR) on the surface of tumor cells. Following cell entry, the methotrexate then binds to and inhibits the enzyme dihydrofolate reductase, which catalyzes the conversion of dihydrofolate to tetrahydrofolate. This results in both the inhibition of DNA and RNA synthesis and the induction of death in rapidly dividing cells. Binding to IGFR can localize the cytotoxic effect of methotrexate in tumor cells. This may increase its efficacy while decreasing its toxicity to normal, healthy cells. IGFR is overexpressed on many types of cancer cells and has been implicated in metastasis and resistance to apoptosis.
IgM-enriched immunoglobulins
An immunoglobulin preparation consisting of immunoglobulin G (IgG) and immunoglobulin A (IgA), supplemented with immunoglobulin M (IgM), with potential antibacterial and immunomodulatory properties. Upon intravenous administration, IgM-enriched immunoglobulins may increase the elimination of infectious pathogens in comparison to immunoglobulin regimens lacking IgM. IgM is the major immunoglobulin secreted during the primary immune response and plays a significant role in compliment activation and in the neutralization of bacterial endo- and exotoxins.
IH636 grape seed proanthocyanidin extract
An oligomeric proanthocyanidin extracted from grape seeds. IH636 grape seed proanthocyanidin extract exhibits dose-dependent free-radical scavenging and antioxidant properties.
IKKb-matured RNA-loaded autologous dendritic cells DCIKKb
A cancer vaccine consisting of autologous, monocyte-derived dendritic cells (DCs) that are matured with tumor necrosis factor-alpha (TNF-alpha), interleukin-1 (IL-1) beta, IL-6, prostaglandin E2 (PGE2) and IkB kinase b (IKKb), and loaded by electroporation with autologous total tumor RNA (TTRNA), RNA coding for tumor-associated antigens (TAAs) that may include gp100, tyrosinase, PRAME, MAGE-A3 and/or IDO, and RNA coding for driver mutations that may include GNAQ/GNA11Q209, R183, SF3B1R625, CYSLTR2L129Q and/or PLCB4D630, with potential immunostimulatory and antineoplastic activities. Upon administration, IKKb-matured, RNA-loaded autologous DCs DCIKKb may elicit a highly specific cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the TAAs and driver mutations encoded by the loaded RNA.
IKZF1/IKZF3 protein degrader GLB-002
An orally bioavailable protein degrader of the transcription factors Ikaros (Ikaros family zinc finger protein 1; IKZF1) and Aiolos (Ikaros family zinc finger protein 3; IKZF3), with potential immunomodulating and antineoplastic activities. Upon oral administration, IKZF1/IKZF3 protein degrader GLB-002 modulates the E3 (ubiquitin) ligase and targets IKZF1 and IKZF3 for ubiquitination, and induces proteasome-mediated degradation of IKZF1 and IKZF3. This reduces the levels of these transcription factors, which are transcriptional repressors in T cells, and modulates the activity of the immune system. This also leads to the downregulation of other proteins, including interferon regulatory factor 4 (IRF4), which may result in apoptosis and the inhibition of tumor cell proliferation. IKZF1 and IKZF3 play a key role in B- and T-cell differentiation. IRF4, overexpressed in certain malignancies, is a transcription factor and key regulator of multiple genes controlling tumor cell survival.
IKZF2 protein degrader DKY709
A low molecular weight (MW) degrader of the protein IKZF2 (Helios), with potential immunomodulating and antineoplastic activities. Upon administration, IKZF2 protein degrader DKY709 modulates the E3 (ubiquitin) ligase and allows for the interaction between the E3 ubiquitin ligase substrate receptor and its target protein IKZF2, thereby targeting IKZF2 for ubiquitination. This induces proteasome-mediated degradation of IKZF2, which is a transcriptional repressor in T cells, and modulates the activity of the immune system. This may induce the activation of T-lymphocytes and the induction of T-cell-mediated anti-tumor immune responses. IKZF2, a zinc finger transcription factor expressed on the majority of regulatory T cells (Tregs) and a member of the Ikaros transcription factor family, plays a key role in cancer immune signal transduction and immunosuppression.
IL-10 immunomodulator MK-1966
An agent that downregulates the activity of the anti-inflammatory cytokine human interleukin-10 (IL-10), with potential immunomodulating and antineoplastic activities. Upon administration, IL-10 immunomodulator MK-1966 blocks the activity of IL-10 and may abrogate the IL-10-induced immunosuppressive tumor microenvironment. This activates cell-mediated immunity against cancer cells, increases cytokine production, including interferon-gamma (IFN-g), decreases T regulatory cell (Treg) activity, and induces a tumor-specific cytotoxic CD8+ T-cell-mediated immune response, which enhances tumor cell death.
IL-10-armed anti-CD19 CAR-T cells Meta10-19
A preparation of T lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) targeting the tumor-associated antigen (TAA) CD19, and armed with the anti-inflammatory cytokine interleukin-10 (IL-10), with potential immunostimulating and antineoplastic activities. Upon administration, IL-10-armed anti-CD19 CAR-T cells Meta10-19 recognize and bind to CD19-expressing tumor cells, thereby inducing selective toxicity in CD19-expressing tumor cells. CD19 antigen is a B-cell specific cell surface antigen overexpressed in B-cell lineage malignancies. IL-10 may stimulate the differentiation and expansion of tumor specific cytotoxic CD8+ T cells.
IL-12-expressing exosome CDK-003
Exosome engineered to display the human pro-inflammatory cytokine interleukin-12 (IL-12) in a fully active form on the surface via the exosome surface glycoprotein prostaglandin F2 receptor negative regulator (PTGFRN; CD315), with potential immunostimulating and antineoplastic activities. Upon intralesional administration of IL-12-expressing exosome CDK-003, IL-12 expressed by the exosome may activate the immune system in the tumor microenvironment (TME) by promoting the activation of natural killer (NK) cells, inducing secretion of interferon-gamma (IFN-g) and inducing cytotoxic T-lymphocyte (CTL) responses against tumor cells. This may result in immune-mediated tumor cell death, inhibition of tumor cell proliferation and inhibition of tumor angiogenesis. The exosome-based formulation may provide targeted anti-tumor immunity while minimizing off-target toxicity. PTGFRN, expressed on the surface of the exosome, enables the engagement of the IL-12 receptor (IL-12R) on immune effector cells such as T cells and NK cells.
IL-12-expressing HSV-1 NSC 733972
A genetically engineered, replication selective, infected cell protein (ICP) 34.5 gene-deleted, oncolytic human simplex virus type 1 (HSV-1) expressing the human immunostimulating cytokine interleukin-12 (IL-12), with potential antineoplastic activity. Upon intratumoral administration of HSV-1 expressing IL-12 NSC 733972, the IL-12-expressing HSV-1 preferentially infects and replicates in tumor cells of neuronal origin causing viral-mediated tumor cell lysis. The released virus particles, in turn, infect and replicate in neighboring tumor cells. In addition, the IL-12-expressing HSV-1 promotes the secretion of IL-12 by the tumor cells. IL-12 promotes the activation of natural killer cells, which induces both the secretion of interferon-gamma and a cytotoxic T-lymphocyte (CTL) response against the tumor cells. This results in both immune-mediated tumor cell death and further inhibition of tumor cell proliferation. Deletion of the gene encoding for ICP34.5 imparts tumor selectivity by preventing replication in healthy cells.
IL-12-expressing mesenchymal stem cell vaccine GX-051
Human mesenchymal stem cells (MSCs) transduced with a retroviral vector encoding a modified form of the cytokine interleukin-12 (IL-12), with potential immunomodulating and antineoplastic activities. Upon intratumoral administration, IL-12-expressing MSC vaccine GX-051 secretes IL-12. IL-12 activates the immune system by both promoting the secretion of interferon-gamma, which activates natural killer cells (NKs), and inducing cytotoxic T-cell responses, which may result in both decreased cell proliferation and increased cell death in tumor cells.
IL-12-Fc fusion protein KGX101
An engineered fusion protein composed of the human pro-inflammatory cytokine interleukin-12 (IL-12) fused to a Fc domain and masked with protein domains, with potential immunomodulatory and antineoplastic activities. Upon administration of IL-12-Fc fusion protein KGX101, IL-12 is bound to the proteins and pharmacologically inactive. IL-12 does not become active until cleaved by tumor-specific matrix metalloproteinases in the tumor microenvironment (TME). Upon proteolytic cleavage, unbound and active IL-12 locally activates the immune system by promoting the secretion of interferon-gamma (IFN-g) and activating CD8+ T cells, CD4+ T cells and natural killer cells (NKs). The activation and expansion of these immune cells mediate cytolytic immune responses against tumor cells, thereby killing tumor cells and inhibiting tumor cell proliferation. The Fc domain prolongs the half-life and exposure in the tumor.
IL-12/Anti-CTLA-4 monoclonal antibody-expressing oncolytic viral vector TG6050
A genetically engineered oncolytic vaccinia viral (VV) vector expressing the human immunostimulating cytokine interleukin-12 (IL-12) and a full-length antibody directed against the human inhibitory T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4; CTLA4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon intavenous administration, IL-12/anti-CTLA-4 monoclonal antibody-expressing oncolytic VV TG6050 specifically infects and replicates in tumor cells causing viral-mediated tumor cell lysis. The released virus particles, in turn, infect and replicate in neighboring tumor cells, thereby further killing tumor cells. Tumor antigens released from the lysed tumor cells also activate the immune system to induce a tumor-specific systemic immune and cytotoxic T-lymphocyte (CTL) response, thereby killing nearby non-infected tumor cells. In addition, the expression of IL-12 promotes the activation of natural killer (NK) cells, which induces the secretion of interferon-gamma and a CTL-mediated response against uninfected tumor cells. This results in immune-mediated tumor cell death and further inhibition of tumor cell proliferation. The anti-CTLA-4 antibody released by the infected cells targets and binds to CTLA-4 expressed on T cells and inhibits the CTLA-4-mediated downregulation of T-cell activation, which promotes T-cell activation and further enhances a CTL-mediated anti-tumor immune response. CTLA-4, an inhibitory receptor and member of the immunoglobulin superfamily (IgSF), plays a key role in the downregulation of the immune system.
IL-12sc, IL-15sushi, IFNa and GM-CSF mRNA-based immunotherapeutic agent SAR441000
An immunotherapeutic agent utilizing mRNA to encode the cytokines interleukin-12sc (IL-12sc), interleukin-15sushi (IL-15sushi), interferon alpha (IFNa) and granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunomodulating and antineoplastic activities. Upon intratumoral administration of IL-12sc, IL-15sushi, IFNa and GM-CSF mRNA-based immunotherapeutic agent SAR441000, mRNA is picked up by nearby cells, translated and released into the local tumor microenvironment (TME). Secretion of these cytokines activate the immune system by promoting the activation of natural killer cells (NKs) and inducing cytotoxic T-lymphocyte (CTL) responses, which may result in an immune-mediated destruction of tumor cells.
IL-15 superagonist SOT201
A cis-acting immunocytokine and human Fc fusion protein composed of a humanized, Fc-silenced monoclonal antibody against the human negative immunoregulatory checkpoint receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) fused to a covalent receptor-linker interleukin-15 (RLI-15) complex containing a human attenuated IL-15 mutein linked to the high-affinity binding sushi domain site of the IL-15 receptor alpha (IL-15Ralpha; IL-15Ra), with potential immunomodulatory and antineoplastic activities. Upon administration, IL-15 superagonist SOT201 targets and binds, with its anti-PD-1 moiety, to PD-1-expressing tumor-infiltrating lymphocytes (TILs), thereby blocking PD-1-mediated T-cell signaling in these cells in the tumor microenvironment (TME). This brings the IL-15 moiety to PD-1-expressing TILs in the TME. The attenuated IL-15 mutein moiety targets and binds, via the IL-2/IL-15betagamma receptor (IL-2/IL-15 receptor beta-common gamma chain), to antigen-specific PD-1-positive CD8+ T cells and natural killer cells (NK cells) without stimulating regulatory T cells (Tregs). This activates and increases the levels of NKs and antigen-specific PD-1-positive CD8+ T cells. The cytotoxic T lymphocytes (CTLs) enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. This may increase CTL-mediated tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T and NK cell development, activation, and proliferation. The Fc moiety allows for an extended half-life of SOT201 while cross linking IL-15 with IL-15Ra sushi domain improves stability. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands, programmed cell death-1 ligand 1 (PD-L1; B7-H1; CD274) and 2 (PD-L2); it plays an important role in tumor evasion from host immunity.
IL-15(N72D)/IL-15Ralpha-sFc fusion protein complex FL115
A long-acting form of the cytokine interleukin (IL)-15 and a fusion protein complex composed of a mutated form of IL-15, with an asparagine to aspartic acid substitution at amino acid 72 (N72D) (IL-15N72D), complexed with a soluble IL-15 receptor alpha (IL-15 Ralpha; IL-15Ra) Fc domain (IL-15Ra-sFc) (IL-15N72D/IL-15Ra-sFc), with potential antineoplastic activity. Upon administration, IL-15(N72D)/IL-15Ra-sFc fusion protein complex FL115 targets and binds to the IL-2/IL-15 receptor beta-common gamma chain (IL-2Rbetagamma) receptor on natural killer (NK) and CD8+ T lymphocytes, which activates and increases the levels of NK cells and memory CD8+(CD44high) T cells. The memory T cells enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. This may increase tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T and NK cell development, activation and proliferation. By coupling IL-15 to IL-15Ra-sFc, this agent has a prolonged drug half-life and shows an increased ability to bind IL-2Rbetagamma, which enhances its immune stimulatory activity as compared to IL-15 alone.
IL-15/IL-15 receptor alpha heterodimer NIZ985
A soluble, recombinant human heterodimer composed of the cytokine interleukin (IL)-15 and the IL-15 receptor alpha (IL-15Ra), with potential antineoplastic activity. Upon subcutaneous administration, the IL-15/IL-15Ra heterodimer (hetIL-15) NIZ985 targets and binds to interleukin-2 (IL-2)/IL-15 receptor beta/gamma. This activates and increases the levels of natural killer (NK) cells and memory CD8+ T cells. The memory T cells enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. This may increase tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T- and NK-cell development, activation and proliferation. NIZ985 does not require endogenous IL-15Ra for its activation.
IL-2 fusion protein PTX-912
A fusion protein consisting of the cytokine interleukin-2 (IL-2) fused to an as of yet not fully elucidated protein, with potential immunopotentiating and antineoplastic activities. Upon administration, IL-2 fusion protein PTX-912 targets and binds to IL-2 receptors, and activates IL-2 receptor-mediated signaling in immune cells. This 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). This leads to T-cell-mediated cytotoxic immune responses against tumor cells and inhibits tumor cell proliferation.
IL-2 mutein/Fc fusion protein HM16390
A recombinant fusion protein and long-acting analog of the human cytokine interleukin 2 (IL-2; IL2) consisting of a variant form of IL-2, IL-2 mutein, fused to a human immunoglobulin G4 (IgG4) Fc molecule via a flexible non-peptidyl linker, with potential immunomodulatory and antineoplastic activities. Upon subcutaneous administration of IL-2 mutein/Fc fusion protein HM16390, the IL-2 mutein moiety preferentially binds to the IL-2 receptor beta subunit (IL-2Rbeta; CD122), and binds to the IL-2 receptor subunit alpha (IL-2Ralpha; CD25) with a lower affinity. The binding of the IL-2 mutein moiety to IL-2Rbeta activates IL-2Rbeta-mediated signaling. This 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), which leads to T-cell-mediated cytotoxic immune responses against tumor cells and inhibits tumor cell proliferation. The lower binding affinity of HM16390 to IL-2Ralpha reduces IL-2Ralpha-mediated adverse effects of IL-2. Fusion to the Fc increases the stability and half-life of HM16390.
IL-2 plasmid DNA/lipid complex
An immunotherapeutic agent consisting of a plasmid DNA encoding human Interleukin-2 (IL-2) complexed with a cationic lipid, 1,2-dimyristyloxypropyl-3-dimethyl-hydroxyethyl ammonium bromide/dioleyl-phosphatidyl-ethanolamine (DMRIE/DOPE), in a 5:1 ratio. Due to the lipophilic nature of this cation liposome complex, this gene transfer system may improve the efficiency of introducing the IL-2 gene into the cells, thereby increasing the production of IL-2 and inducing an immune response.
IL-2 recombinant fusion protein ALT-801
A recombinant protein consisting of the cytokine interleukin-2 (IL-2) fused to a humanized soluble T-cell receptor (TCR) directed against a tumor suppressor p53-derived antigen with potential immunopotentiating and antineoplastic activities. The TCR moiety of IL-2 recombinant fusion protein ALT-801 binds to tumor cells displaying p53 epitope/MHC complexes; subsequently, the tumor cell-localized IL-2 moiety may stimulate natural killer (NK) cell and T cell cytotoxic immune responses against p53-expressing tumor cells.
IL-2/9/15 gamma chain receptor inhibitor BNZ-1
A pegylated peptide antagonist that binds to the common gamma chain (gc; IL2RG; CD132) of the signaling receptor for the pro-inflammatory cytokines interleukin (IL)-2, IL-9, and IL-15, with potential immunomodulating and antineoplastic activities. Upon administration, IL-2/9/15 gc receptor inhibitor BNZ-1 specifically targets and binds to the IL binding site on the gc receptor and blocks IL-2, IL-9 and IL-15 binding, thereby inhibiting IL-2-, IL-9-, and IL-15-mediated signaling and downstream pathways. This may inhibit proliferation of tumor cells that are dependent on IL-2/9/15 signaling for their growth. IL-2/9/15 are upregulated in certain tumor cell types and play a key role in tumor progression and survival.
IL-2/anti-IL-2 antibody conjugate SLC-3010
A noncovalent conjugate consisting of the cytokine interleukin-2 (IL-2; IL2) and TCB2, a humanized antibody directed against the IL-2 receptor subunit alpha (IL2Ra; CD25) binding site on IL-2, with potential immunomodulatory and antineoplastic activities. Upon administration of IL-2/anti-IL-2 antibody conjugate SLC-3010, the IL-2 moiety binds to the IL-2 receptor beta (CD122) and gamma (CD132) subunit (IL2Rb/g) expressed on CD8+ T-effector cells and natural killer (NK) cells, thereby activating IL2Rb/g-mediated signaling within these immune cells. This activates cytotoxic T lymphocytes (CTLs) and NK cells and induces expression of certain cytotoxic cytokines, such as interferon-gamma (IFNg) and transforming growth factor-beta (TGFb). This leads to T-cell-mediated cytotoxic immune responses against tumor cells and inhibition of tumor cell proliferation. The TCB2 moiety binds to the IL2Ra binding site on IL-2, preventing the binding of IL-2 to IL2Ra expressed on regulatory T lymphocytes (Tregs). Signaling through IL2Ra activates CD4-positive immunosuppressive Tregs, which would suppress tumor cell killing. In addition, the binding of the TCB2 moiety to IL-2 induces an allosteric effect that increases the binding affinity of IL-2 to the heterodimeric IL2Rb/g, which further activates T-cell-mediated cytotoxic immune responses against tumor cells.
IL-2/IL-12-based fusion protein CLN-617
A single-chain fusion protein composed of the human cytokine interleukin-2 (IL-2), the collagen-binding domain leukocyte-associated immunoglobulin-like receptor 2 (LAIR2), linked, through glycine/serine linkers, to human serum albumin (HSA) and human IL-12, with potential immunoregulatory and antineoplastic activities. Upon intratumoral (IT) administration of CLN-617, both the IL-2 and IL-12 moieties bind to their respective receptors expressed on CD8+ T cells and natural killer (NK) cells in the tumor microenvironment (TME), thereby activating IL-2- and IL-12-mediated signaling. This synergistically activates and expands CD8+ T cells and NK cells and leads to cytolytic immune responses against tumor cells, which kills tumor cells and inhibits tumor cell proliferation, and triggers systemic anti-tumor immunity. LAIR2 and HSA specifically retain CLN-617 in the injected tumor by binding collagen and increasing molecular weight (MW), respectively. The specific delivery and retention into the tumor increase efficacy of CLN-617 while sparing the unwanted toxic effects of IL-2 and IL-12.
IL-2/Lptn gene-modified allogeneic neuroblastoma tumor cell vaccine
A cancer vaccine consisting of allogeneic neuroblastoma tumor cells have been genetically modified to secrete the human cytokine interleukin-2 (IL-2) and the human chemokine lymphotactin (Lptn) with potential immunostimulating and antineoplastic activities. Upon administration, IL-2 and Lptn are secreted by the IL-2/Lptn gene-modified allogeneic neuroblastoma tumor cell vaccine, potentially enhancing the cytotoxic T lymphocyte (CTL) response elicited by vaccine neuroblastoma tumor-associated antigens (TAAs) against host neuroblastoma tumor cells. Produced by activated progenitor T cells, Lptn belongs to the C chemokine subfamily and is a potent chemotactic factor for lymphocytes; IL-2 stimulates natural killer (NK) cells and may enhance a vaccine-elicited CTL immune response against tumor cells.
IL-34 inhibitor
Any inhibitor that targets and inhibits the cytokine interleukin-34 (IL-34).
IL13Ralpha2-specific hinge-optimized 4-1BB-co-stimulatory CAR/Truncated CD19-expressing autologous TN/MEM Cells
A preparation of ex vivo expanded, genetically modified autologous naïve and memory T cells (TN/MEM) transduced with a replication incompetent, self-inactivating (SIN) lentiviral vector expressing a hinge-optimized, chimeric antigen receptor (CAR) specific for interleukin-13 receptor alpha 2 (IL13Ra2), and containing the cluster of differentiation 137 (CD137; 4-1BB) co-stimulatory signaling domain fused to the signaling domain of the T-cell antigen receptor complex zeta chain (CD3-zeta), and a truncated form of human cluster of differentiation 19 (CD19t), with potential immunostimulating and antineoplastic activities. Upon intratumoral or intracavitary administration, IL13Ra2-specific hinge-optimized 4-1BB-co-stimulatory CAR/truncated CD19-expressing autologous TN/MEM cells are directed to, and induce selective toxicity and cytolysis in, IL13Ra2-expressing tumor cells. IL13Ra2, overexpressed by a variety of tumor cell types, is associated with increased proliferation, migration and invasiveness of tumor cells. The co-stimulatory signaling domain enhances both proliferation of T cells and antitumor activity. Hinge optimization prevents the recognition and clearance of the CAR by endogenous Fc receptors (FcRs). CD19t is used as a surface marker to both track and quantify the modified T cells in vivo.
IL13Ralpha2-specific hinge-optimized 41BB-co-stimulatory CAR truncated CD19-expressing autologous T-lymphocytes
A preparation of ex vivo expanded, genetically modified autologous central memory-enriched T-cells (Tcm) transduced with a replication-incompetent, self-inactivating (SIN) lentiviral vector expressing a hinge-optimized, chimeric antigen receptor (CAR) specific for interleukin-13 receptor alpha 2 (IL13Ra2), and containing the cluster of differentiation 137 (CD137; 4-1BB) co-stimulatory signaling domain fused to the signaling domain of the T cell antigen receptor complex zeta chain (CD3-zeta), and a truncated form of human cluster of differentiation 19 (CD19t), with potential immunostimulating and antineoplastic activities. Upon intratumoral or intracavitary administration, IL13Ra2-specific, hinge-optimized, 41BB-co-stimulatory CAR/truncated CD19 expressing T-lymphocytes are directed to, and induce selective toxicity and cytolysis in IL13Ra2-expressing tumor cells. IL13Ra2, overexpressed by a variety of tumor cell types, is associated with increased tumor cell proliferation, migration and invasiveness. The costimulatory signaling domain enhances both proliferation of T cells and antitumor activity. Hinge optimization prevents the recognition and clearance of the CAR by endogenous Fc receptors (FcRs). CD19t is used as a surface marker to both quantify and track the gene-modified T cells in vivo.
ilaprazole
A substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity. A weak base, ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.
Ilaris
(Other name for: canakinumab)
ilginatinib
An orally bioavailable, small molecule inhibitor of Janus-associated kinase 2 (JAK2) and Src-family kinases, with potential antineoplastic activity. Ilginatinib competes with ATP for binding to JAK2 as well as the mutated form JAK2V617F, thereby inhibiting the activation of JAK2 and downstream molecules in the JAK2/STAT3 (signal transducer and activator of transcription 3) signaling pathway that plays an important role in normal development, particularly hematopoiesis. In addition, ilginatinib inhibits the Src family tyrosine kinases. This eventually leads to the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); JAK2V617F is a constitutively activated kinase that activates the JAK/STAT signaling pathway and dysregulates cell growth and function, and its expression transforms hematopoietic cells to cytokine-independent growth.
ilixadencel
An off-the-shelf immune primer consisting of allogeneic monocyte-derived dendritic cells (MoDCs) that have been stimulated with a combination of activating factors to produce pro-inflammatory factors including tumor necrosis factor-alpha (TNF-alpha), interleukin-1 beta (IL-1 beta), interleukin-12, p70 (IL-12 p70), C-C motif chemokine 4 (CCL4; macrophage inflammatory protein 1-beta; MIP-1-beta), C-C motif chemokine 5 (CCL5; RANTES), and C-X-C motif chemokine 10 (CXCL10), with potential immunostimulating and antineoplastic activities. Upon intratumoral injection of ilixadencel, the dendritic cells (DCs) release type 1 T-helper cell (Th1)-associated chemokines, including CCL4, CCL5 and CXCL10, that may recruit natural killer (NK)-cells and pre-DCs into the tumor microenvironment (TME). The interaction between NK cells and ilixadencel DCs may induce NK-cell-mediated killing of tumor cells, resulting in release of tumor-associated-antigens (TAAs). The production of interferon-gamma (IFN-gamma) by activated NK-cells and TNF-alpha/beta released by ilixadencel DCs will induce maturation and promote cross-presentation of TAAs by recruited endogenous "bystander" DCs. Migration of these antigen-loaded and matured "bystander" DCs to the tumor-draining lymph node will lead to a Th1-polarized activation of tumor-specific T-cells.
Ilopan
(Other name for: dexpanthenol cream)
iloprost
A prostacyclin analogue with potential chemopreventive activity. Iloprost binds to the prostacyclin receptor in various target cells, thereby causing vasodilation, inhibition of platelet aggregation, and decreased tumor cell adhesion to endothelium among other effects. Prostacyclin is a naturally occurring eicosanoid with anti-inflammatory, antineoplastic, and anti-metastatic properties.
ilorasertib
An orally bioavailable, adenosine triphospate mimetic, and inhibitor of Aurora kinases, vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptor (PDGFRs), with potential antineoplastic activity. Upon administration, ilorasertib selectively binds to and inhibits Aurora kinases A, B and C, which may disrupt both the assembly of the mitotic spindle apparatus and chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. In addition, ilorasertib selectively binds to and inhibits VEGFRs and PDGFRs, which may result in the inhibition of both angiogenesis and tumor cell proliferation in VEGFR/PDGFR-overexpressing tumor cells. This agent also inhibits the Src family of cytoplasmic tyrosine kinases. Aurora kinases A, B and C, are serine/threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of tumor cell types. Both VEGFRs and PDGFRs are receptor tyrosine kinase families whose members may be upregulated in various tumor cell types.
Ilotycin
(Other name for: erythromycin)
Iluyma
(Other name for: tildrakizumab)
Imagent
(Other name for: perflubron)
imaging agent QRH-882260 heptapeptide
An orally bioavailable fluorescent imaging agent composed of the near-infrared (NIR) fluorophore cyanine 5 (Cy5) linked to a seven-amino acid long peptide that specifically binds to the tumor-associated antigen (TAA) epithelial growth factor receptor (epidermal growth factor receptor; EGFR), that can potentially be used for the imaging of EGFR-expressing tumor cells. Upon oral administration of the fluorescent imaging agent QRH-882260 heptapeptide, the peptide moiety selectively binds to EGFR expressed on tumor cells in the gastrointestinal (GI) tract. Upon fluorescence imaging, EGFR-expressing tumor cells can be visualized. EGFR, a member of the epidermal growth factor receptor family, is overexpressed on the surfaces of various tumors cells.
imalumab
A human, recombinant monoclonal antibody (MoAb) against macrophage migration inhibitory factor (MIF), with potential immunomodulating, anti-inflammatory and antineoplastic activities. Upon intravenous administration, imalumab binds to MIF, blocking its activity and preventing the MIF-mediated secretion of certain cytokines, including interleukin-1 beta and tumor necrosis factor-alpha. This may lead to an inhibition of cancer cell proliferation in MIF-overexpressing tumor cells. MIF, a pro-inflammatory cytokine overexpressed in some cancers, plays a key role in inflammation, immune responses and cancer cell proliferation.
imatinib mesylate
The mesylate salt of imatinib, a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST).
Imbruvica
(Other name for: Ibrutinib)
Imdelltra
(Other name for: tarlatamab-dlle)
imetelstat sodium
The sodium salt of imetelstat, a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a "telomerase template antagonist"), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis.
imexon
A 2-cyanoaziridine derivative with antitumor activity in multiple myeloma. Although its mechanism of action is not clearly known, imexon may induce apoptosis via a pathway involving cleaved caspase-3, caspase-9, and/or caspase-8. Other cytotoxic mechanisms of action of this agent may involve thiol depletion, generation of reactive oxygen species (ROS), and decreases in the mitochondrial membrane potential.
Imfinzi
(Other name for: durvalumab)
imgatuzumab
A glycoengineered monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Imgatuzumab binds to the extracellular domain of EGFR, preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization may result in an inhibition of downstream ERK and JNK signaling pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various solid tumor cell types.
imidazole mustard
A synthetic derivative of imidazole with potent antineoplastic properties. Imidazole mustard alkylates DNA, preferentially at guanine residues, resulting in DNA interstrand crosslinks and inhibition of DNA replication and RNA and protein synthesis.
imidazolyl ethanamide pentandioic acid
An orally bioavailable small molecule, with potential hematopoiesis inducing and antiviral activities. Upon oral administration, myelo001 stimulates the differentiation of bone marrow cells of the leukocytic, lymphocytic, and erythrocytic lineages, and prevents apoptosis of hematopoietic cells. This prevents chemotherapy-induced neutropenia (CIN), inhibits the risk of infections, increases tolerance and allows for the continuation of the neutropenia-inducing chemotherapeutic agent. In addition, myelo 001 has antiviral properties.
imifoplatin
A platinum (Pt)-based agent belonging to the phosphaplatin family comprised of Pt complexed to a pyrophosphate ligand, with potential antineoplastic activity. Although the exact mechanisms through which imifoplatin exerts its effect have yet to be fully elucidated, this agent, upon intravenous administration, binds to certain transmembrane proteins and activates several genes involved in tumor suppression and apoptosis. This leads to the activation of various signal transduction pathways, induces S/G2 phase cell cycle, and causes tumor cell apoptosis. In addition, imifoplatin may inhibit angiogenesis. Unlike conventional Pt-based chemotherapeutics, imifoplatin does not bind to DNA and is able to overcome drug resistance, which occurs with conventional Pt-based chemotherapeutics; it also has a more favorable side effect profile and is more stable in plasma.
imipenem
A broad-spectrum, semi-synthetic beta-lactam carbapenem derived from thienamycin, produced by Streptomyces cattleya. Imipenem binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes that are involved in the last stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. This inactivation results in the weakening of the bacterial cell wall and eventually causes cell lysis. Imipenem has the greatest affinity for PBP 1A, 1B, and 2, and its lethal effect is related to binding to PBP 2 and 1B. This antibiotic is active against a wide range of gram-positive and gram-negative organisms and is stable in the presence of beta-lactamases.
imipenem-cilastatin-relebactam
A parenteral antibiotic preparation containing imipenem, cilastatin sodium and relebactam, with bactericidal activity. Imipenem, a broad spectrum beta-lactam carbapenem antibiotic, binds to and inactivates penicillin-binding proteins (PBP) on the inner membrane of the bacterial cell wall, thereby interfering with the cross-linkage of peptidoglycan chains critical for bacterial cell wall strength and rigidity. Cilastatin sodium, a renal dehydropeptidase inhibitor, reduces the breakdown of imipenem by renal dehydropeptidase. Relebactam, a beta-lactamase inhibitor, reduces the breakdown of imipenem by certain serine beta-lactamases among gram-negative bacteria. Imipenem is active against a wide range of gram-positive and gram-negative organisms, and the imipenem, cilastatin sodium and relebactam combination may be used to treat infections caused by resistant gram-negative bacteria.
imipramine
A synthetic tricyclic derivative, antidepressant Imipramine enhances monoamine neurotransmission in certain areas of the brain. It also induces sedation through histamine 1 receptor blockage; hypotension through beta-adrenergic blockage; and diverse parasympatholytic effects. Imipramine has less sedative effect than other members of its therapeutic family. It is used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders.
imiquimod
A synthetic agent with immune response modifying activity. As an immune response modifier (IRM), imiquimod stimulates cytokine production, especially interferon production, and exhibits antitumor activity, particularly against cutaneous cancers. Imiquimod's proapoptotic activity appears to be related to Bcl-2 overexpression in susceptible tumor cells.
imisopasem manganese
A manganese-based non-peptidyl mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with potential antioxidant and chemo/radioprotective activities. Upon administration, imisopasem manganese mimics the activity of MnSOD and scavenges reactive oxygen species (ROS), such as superoxide anion, which prevents oxygen free radical damage to macromolecules such as DNA. This reduces ROS-mediated lipid peroxidation, prevents apoptosis and protects against oxygen free radical-induced toxicity in normal tissues.
Imitrex
(Other name for: sumatriptan succinate)
Imjudo
(Other name for: tremelimumab-actl)
Imkeldi
(Other name for: imatinib mesylate)
imlunestrant
An orally available selective estrogen receptor degrader (SERD), with potential antineoplastic activity. Upon oral administration, imlunestrant specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that results in ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells.
Imlygic
(Other name for: talimogene laherparepvec)
immediate-release afuresertib
An immediate-release (IR) tablet formulation containing afuresertib, an inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Upon oral administration of the IR formulation, afuresertib binds to and inhibits the activity of Akt, which may result in the inhibition of PI3K/Akt signaling pathway, decreased tumor cell proliferation and the induction of tumor cell apoptosis in Akt-expressing tumor cells. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.
immediate-release bupropion
An immediate-release (IR) tablet formulation of the aminoketone bupropion, with antidepressant activity and for potential use in promoting smoking cessation, increasing sexual desire, and reducing cancer-related fatigue. Bupropion is a weak blocker of the neuronal uptake of serotonin, dopamine and norepinephrine, and is a central nicotinic acetylcholine receptor antagonist. Bupropion may also reduce circulating levels of tumor necrosis factor (TNF) and normalize hypothalamic-pituitary-adrenal (HPA) axis functioning, which is dysregulated in certain cases of cancer-related fatigue.
immediate-release onapristone
An immediate-release (IR) formulation of onapristone, an orally bioavailable progesterone receptor (PR) antagonist, with antineoplastic activity. Onapristone binds to the PR and inhibits both PR activation and the associated expression of PR-responsive genes. This may inhibit PR-mediated proliferative effects in cancer cells overexpressing PR. PR is expressed in certain cancer cell types and plays a key role in proliferation and survival.
ImmTher
(Other name for: disaccharide tripeptide glycerol dipalmitoyl)
Immucell WGP
(Other name for: beta-glucan)
ImmuCyst
(Other name for: BCG vaccine)
Immun-Aid
(Other name for: arginine/omega-3 fatty acids/nucleotides oral supplement)
immune globulin subcutaneous human–klhw
A subcutaneous injectable formulation containing human immune globulins (Ig), mainly IgGs, with a broad spectrum of antibodies against bacterial, viral, parasitic, and mycoplasmal agents and their toxins, that can be used in the treatment of various primary humoral immunodeficiencies. Upon subcutaneous administration, immune globulin subcutaneous human provides a wide variety of opsonizing and neutralizing IgG antibodies, thereby restoring abnormally low IgG levels to normal concentrations and providing preventive activity against various infections.
immunoadjuvant QS-DG
A synthetic saponin, chemically identical to the natural saponin QS-21, with immunoadjuvant activity. When co-administered with vaccine antigens, immunoadjuvant QS-DG may increase total antitumoral vaccine-specific antibody responses and cytotoxic T-lymphocyte (CTL) responses.
Immunocal
(Other name for: whey protein isolate)
immunocytokine NHS-IL12
A fusion protein consisting of the heavy-chains of the human antibody NHS76, raised against DNA released by necrotic tumor cells, and fused to two molecules of a genetically modified human interleukin-12 (IL-12) with potential immunostimulating and antineoplastic activities. Upon administration, the antibody moiety of immunocytokine NHS-IL12 binds to DNA released from necrotic tumor cells located primarily at the core of necrotic solid tumors, thereby delivering the IL-12 moiety. In turn, the IL-12 moiety of this agent stimulates the host immune system to mount an immune response against tumor cells, thereby inhibiting tumor growth. IL-12 is a proinflammatory cytokine with numerous immunoregulatory functions and may augment host immune responses to tumor cells. By targeting tumor cells, NHS-IL-12 may reduce the toxicity associated with systemic administration of recombinant human IL-12.
immunocytokine NHS-IL2-LT
A fusion protein consisting of a mouse-human chimeric antibody directed against DNA released by necrotic tumor cells fused to two molecules of a genetically modified human interleukin-2 (IL-2) with potential antineoplastic activity. Upon administration, the antibody moiety of immunocytokine NHS-IL2-LT binds to DNA released by necrotic tumor cells located primarily at the core of necrotic solid tumors, delivering the IL-2 moiety. In turn, the IL-2 moiety of this agent activates the immune system to mount a cytotoxic T-lymphocyte response against nearby tumor cells.
immunogenic cell death inducer CAN2109
A long-acting, bi-functional immunogenic cell death (ICD) inducer, with potential immunostimulating and antineoplastic activities. Upon intratumoral (IT) administration, ICD inducer CAN2109 may directly kill tumor cells through as of yet undisclosed mechanism of action (MoA). This releases tumor neoantigens, which may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the neoantigens, resulting in tumor cell lysis. CAN2109 retains in the tumor microenvironment (TME) for a long time with minimal release to the systemic circulation after IT administration.
immunomodulator LAM-003
An orally bioavailable immunomodulating agent with potential antineoplastic activity
immunomodulator OHR/AVR118
A peptide-nucleic acid immunomodulator with proinflammatory, broad-spectrum antiviral, and potential antineoplastic activities. Immunomodulator OHR/AVR118 stimulates the peripheral blood mononuclear cell (PBMC) production of the proinflammatory cytokines IFN-y, IL-1b, IL-6 and TNF-a. This agent may reduce HIV-1 p24 antigen; viral reverse transcriptase activity; syncitial cell formation; and viral mRNA in infected PBMCs and human CD4+ lymphocyte H9 cells, and may decrease viral loads and increase CD4+ and CD8+ T-cell counts in HIV patients. In vitro, immunomodulator OHR/AVR118 has been shown to induce the maturation of HL60 leukemic cells and to inhibit the invasive and metastatic properties of a highly malignant breast cancer cell line.
immunomodulatory agent CC-11006
A proprietary, orally available, small molecule and thalidomide analog, with potential immunomodulating and antineoplastic activity. CC-11006 appears to have a similar mechanism to thalidomide and may modulate the expression of proinflammatory and regulatory cytokines.
immunotherapeutic combination product CMB305
An immunotherapeutic combination product composed of LV305, an engineered lentiviral vector that both targets dendritic cells (DCs) and contains nucleic acids encoding the human tumor-associated cancer-testis antigen NY-ESO-1 (CTAG1), and G305, a cancer vaccine comprised of an NY-ESO-1 recombinant protein and glucopyranosyl lipid adjuvant (GLA)-stable emulsion (GLA-SE), with potential synergistic immunostimulatory and antineoplastic activities. Upon intradermal administration of LV305, the DC-targeting lentiviral vector targets and binds to dermal DCs via the DC-specific intercellular adhesion molecule-3-grabbing non-integrin (DC-SIGN) receptor. Upon internalization of the vector, the NY-ESO-1 protein is expressed, which stimulates DC maturation, and activates the immune system to mount a cytotoxic T-lymphocyte (CTL) response against NY-ESO-1-expressing cells; this may result in tumor cell lysis. Upon the sequential intramuscular injection of G305, the adjuvant portion of G305 binds to toll-like receptor 4 (TLR-4) expressed on various immune cells, including DCs, monocytes, macrophages and B-cells. The activated DCs present the NY-ESO-1 antigen to CD4-positive Th1 T-lymphocytes. The induction of antigen-specific CD4-positive T-lymphocytes further induces a CTL response against NY-ESO-1-expressing tumor cells. In addition, G305 induces an NY-ESO-1-specific antibody response. NY-ESO-1, expressed in normal testes and on the surfaces of various tumor cells, plays a key role in tumor cell proliferation and survival.
immunotherapeutic gel SRG-514
An injectable biodegradable hydrogel, with potential immunostimulating and antineoplastic activities. Upon intraoperative injection into the site of surgical tumor resection, the immunotherapeutic gel SRG-514 releases an as of yet unidentified immunotherapeutic agent locally and may, through an as of yet unidentified mechanism of action, stimulate the cancer-suppressed immune system to eliminate any remaining cancer cells locally and systemically which may prevent cancer recurrence and metastasis after cancer surgery.
immunotherapy regimen MKC-1106-MT
An immunotherapy regimen containing three components: a plasmid encoding portions of the two melanoma-associated antigens Melan A (also called MART-1) and tyrosinase and two synthetic analogs of Melan-A and tyrosinase antigen epitopes with potential immunostimulating and antitumor activities. First, the plasmid is injected directly into lymph nodes in order to sensitize or prime antigen-presenting cells (APCs) and central memory T cells in lymph nodes to plasmid-expressed Melan A and tyrosinase. After several priming injections with plasmids, the Melan A and tyrosinase synthetic epitope analogs are injected directly into lymph nodes; upon binding to major histocompatibility complex (MHC) molecules on APC cell surfaces, these synthetic epitope analogs may stimulate a "primed" cytotoxic T lymphocyte (CTL) response against melanoma tumor cells, resulting in tumor cell lysis. Melan-A and tyrosinase are overexpressed by melanoma tumor cells.
immunotoxin CMD-193
A humanized immunotoxin directed against the Lewis Y antigen conjugated with calicheamicin, a hydrophobic enediyne antibiotic, with potential antineoplastic activity. CMD193 binds to the Lewis Y antigen, a tetrasaccharide expressed on the cell surfaces of many tumor cell types. Upon binding, CMD-193 is internalized, thereby delivering the attached calicheamicin to Lewis Y antigen-expressing tumor cells. Calicheamicin binds non-covalently to the minor groove of DNA and prompts conformational changes and DNA oxidation, thereby inhibiting DNA synthesis and inducing apoptosis.
immunotoxin D2C7-(scdsFv)-PE38KDEL
A recombinant immunotoxin fusion protein consisting of single-chain variable-region antibody fragments (scFvs), which contain disulfide stabilized heavy- (Vh) and light- (Vl) chain variable regions of the monoclonal antibody D2C7 (D2C7-scdsFv), targeting both the wild-type form (EGFRwt) and the in-frame deletion mutant form (EGFRvIII) of epidermal growth factor receptor (EGFR), and fused, via a 15-amino acid peptide linker to domains II and III of the Pseudomonas exotoxin A (PE38KDEL) (D2C7-(scdsFv)-PE38KDEL), with potential antineoplastic activity. Upon intratumoral administration by convection-enhanced delivery, the scFv moiety of immunotoxin anti-EGFR scFv monoclonal antibody fragment immunotoxin D2C7-(scdsFv)-PE38KDEL targets and binds to a specific amino acid epitope present in the extracellular domain of both the EGFRwt and EGFRvIII proteins. This binding facilitates the internalization of the immunotoxin by tumor cells. Inside the cells, the exotoxin portion of the fusion protein binds to translation elongation factor 2 (EF-2), and deactivates EF-2 through ADP ribosylation. This results in the inhibition of protein synthesis, the induction of apoptosis and a reduction in cell proliferation of EGFRwt/EGFRvIII-expressing tumor cells. Compared to intact IgG antibodies and single-chain antibodies, scFvs are smaller with increased tumor-penetrating capacity which may enhance therapeutic efficacy. The EGFR gene, a transmembrane receptor tyrosine kinase, and its mutant form, EGFRvIII, which contains a deletion of exons 2-7 of the EGFR gene, are frequently amplified and overexpressed in a variety of cancers. KDEL increases the toxin's intracellular retention, thereby enhancing its cytotoxicity.
Immunox
(Other name for: thymopentin)
Imodium A-D
(Other name for: loperamide hydrochloride)
imofinostat
An orally bioavailable N-hydroxyacrylamide-derived inhibitor of both human pan-histone deacetylase (HDAC) enzymes and the serine/threonine protein kinase Akt (protein kinase B), with potential antineoplastic activity. Upon administration, imofinostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in both an induction of chromatin remodeling, and the selective transcription of tumor suppressor genes. This prevents cell division and induces both cell cycle arrest and apoptosis, which may inhibit the proliferation of susceptible tumor cells. In addition, imofinostat inhibits the phosphorylation and activation of Akt, which prevents the activation of downstream signaling pathways, independent of its HDAC inhibitory activity. HDACs, upregulated in many tumor cell types, are a family of enzymes that deacetylate histone proteins. Akt, overexpressed in many tumor cell types, plays a key role in tumor cell proliferation and survival.
Imovax Rabies
(Other name for: Wistar rabies virus strain PM-1503-3M vaccine)
Impact
(Other name for: arginine/omega-3 fatty acids/nucleotides oral supplement)
Imprime PGG
(Other name for: odetiglucan)
IMREG-1
A low molecular weight fraction of human leukocyte dialysates with potential immunostimulatory activity. IMREG-1 is shown to augment and accelerate human delayed type hypersensitivity (DTH) to recall antigen in vivo, potentiate production of interleukin-2 (IL-2) and interferon gamma, and induce expression of IL-2 receptor in peripheral blood mononuclear cells. These effects are attributed to the peptides Tyr-Gly and Tyr-Gly-Gly, which are identical to the N-terminal end of the enkephalins. Studies in HIV patients have shown that this agent may delay progression to more serious disease and improve laboratory markers.
imsidolimab
A humanized monoclonal antibody directed against the interleukin-36 receptor (IL-36R), with potential anti-inflammatory and immunomodulatory activities. Upon administration, imsidolimab targets, binds to and prevents the activity of IL-36R by the pro-inflammatory cytokine IL-36. This prevents IL-36/IL-36R-mediated signaling pathways. This may inhibit skin inflammation in which the IL-36/IL-36R plays a key role. IL-36 is highly upregulated in certain skin inflammatory conditions.
IMT-1012 immunotherapeutic vaccine
A multi-peptide cancer vaccine with potential immunostimulating and antineoplastic activities. IMT-1012 immunotherapeutic vaccine contains twelve different synthetic peptides or tumor associated antigens (TAAs), including cyclin I (CCNI), cyclin-dependent kinase CDC2, EDDRI and TACE/ADAM17, each of which is involved in a different pathway associated with tumor growth, survival, and metastasis. Each antigen in the vaccine elicits a specific cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing that antigen. This multi-antigen/multi-pathway targeting strategy provides broad immunotherapeutic coverage with respect to tumor complexity and heterogeneity and may result in enhanced vaccine efficacy.
Imuran
(Other name for: azathioprine sodium)
Imuthiol
(Other name for: ditiocarb sodium)
Imvamune
(Other name for: MVA-BN smallpox vaccine)
In 111 monoclonal antibody B3
A radioimmunoconjugate of monoclonal antibody (MoAb) B3 labeled with Indium 111 (In-111). MoAb B3 is a murine MoAb that recognizes a Lewis Y carbohydrate antigen present on the surface of many carcinomas. This radioimmunoconjugate emits gamma radiation and X-Ray photons that can be captured by gamma camera, allowing imaging of Lewis Y expressing tissues.
In 111 monoclonal antibody Hu3S193
A radioimmunoconjugate of humanized monoclonal antibody (MoAb) 3S193 labelled with Indium 111 (In-111). MoAb Hu3S193 recognizes a Lewis Y carbohydrate antigen present on the surface of many carcinomas. This radioimmunoconjugate emits gamma radiation and X-ray photons, thereby allowing detection of tumor localization and distribution of MoAb HuS193 in diagnostic imaging procedures.
inactivated oncolytic virus particle GEN0101
An inactivated, non-replicating particle of hemagglutinating virus of Japan (HVJ), an oncolytic virus of the paramyxovirus family, with potential immunostimulating and antineoplastic activities. Upon intracutaneous administration, GEN0101 targets and binds to the cytosolic nucleic acid receptor retinoic acid-inducible gene I (RIG-I). This induces RIG-I-mediated signaling and a potent innate immune response against tumor cells, leading to the activation of natural killer (NK) cells and cytotoxic T lymphocytes (CTL), and apoptosis in tumor cells. GEN0101 also activates dendritic cells (DCs) to produce cytokine interleukin-6 (IL-6), suppressing the function of regulatory T cells (Treg), a negative regulator of immune responses. The suppression of Treg activity helps maintain the induced immune responses.
inactivated poliovirus vaccine
A vaccine consisting of inactivated poliovirus (IPV) types 1,2 and 3, with active immunizing activity against poliomyelitis. Upon intramuscular vaccination, inactivated poliovirus vaccine (IPV) activates the immune system to develop antibodies against polioviruses.
inalimarev
A cancer vaccine comprised of a recombinant vaccinia viral vector encoding the carcinoembryonic antigen (CEA), MUC-1 (mucin-1), a transmembrane glycoprotein secreted by glandular tissues, and TRICOM, comprised of the three co-stimulatory molecule transgenes B7-1, ICAM-1 and LFA-3. Upon administration, inalimarev may enhance CEA and MUC-1 presentation to antigen presenting cells (APC) and may activate a cytotoxic T lymphocyte (CTL) response against CEA- and MUC-1-expressing tumor cells.
Inapsine
(Other name for: droperidol)
inavolisib
An orally available inhibitor of phosphatidylinositol 3-kinase (PI3K), with potential antineoplastic activity. Upon administration, inavolisib binds to and inhibits various members of the PI3K family, including activating mutations in the catalytic alpha isoform PIK3CA. PI3K inhibition prevents the activation of the PI3K-mediated signaling pathway and results in the inhibition of growth and survival of PI3K-overexpressing tumor cells. Dysregulation of the PI3K signaling pathway is frequently associated with tumorigenesis and tumor resistance to a variety of antineoplastic agents and radiotherapy. PIK3CA, which encodes the p110-alpha catalytic subunit of the class I PI3K, is frequently mutated in a variety of cancer cell types and plays a key role in cancer cell growth and invasion.
Incel
(Other name for: biricodar dicitrate)
Incivek
(Other name for: telaprevir)
incomplete Freund's adjuvant
A water-in-oil emulsion that stimulates the T-cell immune response to antigens and may be used in various types of cancer vaccines.
incyclinide
A chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.
Inderal
(Other name for: propranolol hydrochloride)
India ink
An aqueous suspension containing carbon particulates from charcoal powder and paramagnetic oxygen (O2) sensor, that can potentially be used to assess oxygen levels using electron paramagnetic resonance (EPR) oximetry. Upon injection into tissue, the India ink has a particular EPR spectra that is very sensitive to oxygen and on the oxygen levels in tissues, and the line width of the EPR spectrum can be broadened by oxygen. Upon using EPR Oximetry, this spectrum can provide sensitive, repeated, and direct measurements of tissue oxygen and oxygenation status of tumors.
indibulin
A synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines.
indicine-N-oxide
A natural pyrrolizidine alkaloid with antineoplastic properties. Indicine-N-oxide alkylates and crosslinks DNA.
indigotindisulfonate sodium
The sodium salt form of indigotindisulfonate, a synthetic blue dye and food colorant derived from indigo, that can be used as a stain in medical imaging and as a redox and pH indicator. Upon intravenous administration, indigotindisulfonate is filtered rapidly by the kidneys from the blood and colors the urinary tract which enables the urinary tract to be seen during surgery. It can also be used ex vivo to stain certain specimens, differentiate between benign and malignant lesions, and help stage and diagnose certain types of cancers.
indinavir sulfate
A synthetic antiviral agent. Indinavir selectively binds to the active site of human immunodeficiency virus (HIV) protease and inhibits its activity, preventing the protease-mediated cleavage of gag-pol viral polyproteins; as a result immature, noninfectious virions are produced.
Indium 111 ProstaScint
(Other name for: indium In 111 capromab pendetide)
indium In 111 anti-CD45 monoclonal antibody BC8
A radioimmunoconjugate containing the murine IgG1 anti-CD45 monoclonal antibody (MoAb) BC8 labeled with the gamma-emitting isotope indium 111 (In 111), with potential radioimaging application. Upon administration, indium In 111 anti-CD45 monoclonal antibody BC8 binds to CD45 antigen, a receptor protein tyrosine phosphatase expressed on the surface of most of the normal and malignant hematopoietic cells. After binding and internalization by CD45-expressing tumor cells, radioactive In 111 allows for the detection of BC8 distribution and tumor localization using gamma scintigraphy.
indium In 111 anti-EGFR monoclonal antibody ABT-806
A radioimmunoconjugate composed of a humanized monoclonal antibody IgG1 directed against the epidermal growth factor receptor (EGFR) and labeled with the radioisotope indium In 111, with potential radioimaging activity. Indium In 111 anti-EGFR monoclonal antibody ABT-806 binds to a specific epitope of either wild-type or EGFR variant III mutant on tumor cells, thereby allowing imaging of EGFR-expressing tumor cells using gamma scintigraphy. ABT-806 is the humanized version derived from the predecessor chimeric monoclonal antibody 806. EGFR, a receptor tyrosine kinase overexpressed on the cell surfaces of many tumor cell types, plays a key role in tumor cell proliferation.
indium In 111 bevacizumab
A radioimmunoconjugate comprised of the recombinant humanized monoclonal antibody bevacizumab conjugated with the gamma-emitting radioisotope indium In 111. Indium I 111 bevacizumab binds to vascular endothelial growth factor (VEGF), allowing the detection of VEGF distribution using gamma scintigraphy.
indium In 111 capromab pendetide
A radioimmunoconjugate consisting of the murine IgG1 kappa monoclonal antibody capromab (7E11-C5.3), conjugated to the linker-chelator glycyl-tyrosyl-(N,-diethylenetriaminepentaacetic acid)-lysine hydrochloride (GYK-DTPA-HCl) and labeled with radioisotope indium In 111, with ligand-binding and gamma-emitting activities. Upon intravenous administration, indium In 111-capromab pendetide binds to a cytoplasmic epitope of human prostate specific membrane antigen (PSMA) expressed on prostate tumor cell surfaces via its capromab moiety and, upon internalization, allows radioimmunolocalization with gamma scintigraphy. PSMA is a cell surface glycoprotein abundantly expressed by prostate epithelium and is typically overexpressed by prostate cancer cells.
indium In 111 chimeric monoclonal antibody 806
A recombinant chimeric, mouse-human monoclonal antibody IgG1, directed against the epidermal growth factor receptor (EGFR) and labeled with the radioisotope indium-111, with potential radioimaging activity. Indium 111 chimeric monoclonal antibody 806 binds to a specific epitope on EGFR-expressing tumor cells, allowing imaging of EGFR-expressing tumor cells using gamma scintigraphy. EGFR is a receptor tyrosine kinase that is involved in the regulation of cell growth and is found to be overexpressed on the cell surfaces of many tumor cell types.
indium In 111 CHX-A DTPA trastuzumab
An indium I 111-labeled trastuzumab with potential use as an imaging agent. Indium In 111 CHX-A DTPA trastuzumab is chemically conjugated via a bifunctional metal chelator molecule, 2-(p-isothiocyanatobenzyl)-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-A DTPA), a backbone-substituted derivative of DTPA. This agent may allow radioimmunolocalization of HER2-positive cells. Trastuzumab, a recombinant humanized monoclonal antibody that selectively binds with high affinity to the extracellular domain of human epidermal growth factor receptor 2 (HER2), may elicit an antibody-dependent cellular cytotoxicity (ADCC) against tumor cells that overexpress HER2.
indium In 111 FPI-2058
A radioconjugate consisting of the neurotensin receptor type 1 (NTR1; NTSR1) antagonist, IPN01087 (3BP-227) that is linked to the radioisotope indium In 111, with potential imaging activity during single photon emission computed tomography (SPECT)/computed tomography (PET/CT). Upon administration, indium In 111 IPN01087 targets and binds to NTR1 expressed on certain tumor cells. Upon binding and radioimaging, NTR1-expressing tumor cells can be visualized and the biodistribution of IPN01087 can be assessed. NTR1, a G-protein coupled receptor, is highly expressed in ductal pancreatic adenocarcinoma but not in normal pancreatic tissue.
indium In 111 FPI-2071
A radioimmunoconjugate composed of FPI-2053, a humanized bispecific antibody targeting epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (HGFR; c-Met), conjugated to the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), and radiolabeled with the radioisotope indium In 111, with potential radioimaging activity. Upon administration of indium In 111 FPI-2071, the FPI-2053 moiety targets and binds to the extracellular domains of both EGFR and c-Met expressed on certain cancer cells, followed by internalization and retention of the radioisotope. This allows for imaging of EGFR- and c-Met-expressing tumor cells using gamma scintigraphy. EGFR and c-Met, both upregulated or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation. EGFR and c-Met are co-expressed on the surface of various cancer cell types while co-expression on normal, healthy cells is minimal.
indium In 111 ibritumomab tiuxetan
A targeted radioimmunoconjugate composed of a murine monoclonal anti-CD20 antibody (ibritumomab) linked by a chelator (tiuxetan) to the imaging radioisotope indium-111. This radioimmunoconjugate binds to CD20-positive cells, permitting radioimmuno-localization of CD20-positive cell biodistribution.
indium In 111 minigastrin analog CP04
A radioconjugate consisting of the minigastrin analog, CP04, labeled with the gamma-emitting radioisotope indium-111, with radioimaging potential. Upon intravenous administration, 111In-CP04 binds to and is subsequently internalized by cells expressing cholecystokinin receptor subtype 2 (CCK2R), which is overexpressed in certain tumor types. 111In-CP04 emits gamma radiation and X-ray photons that allow detection of tumor localization and distribution using gamma scintigraphy.
indium In 111 monoclonal antibody BrE-3
A humanized monoclonal antibody conjugated to the imaging radioisotope (indium-111). This radioimmunoconjugate binds to the breast epithelial mucin antigen, which is found primarily on breast cancer cells, permitting radioactive immunodetection of mucin-positive tumor cells and an estimate of radiation dosimetry prior to administration of cytotoxic radiotherapy.
indium In 111 monoclonal antibody HuJ591
A radioimmunoconjugate containing the recombinant humanized monoclonal antibody J591 directed against the extracellular domain of prostate-specific membrane antigen (PSMA) and labeled with the gamma-emitting isotope indium 111 (In 111; 111In), with potential radioimaging application. Upon administration, indium In 111 monoclonal antibody J591 targets and binds to PSMA expressed on tumor cells. The use of gamma scintigraphy allows for the detection and imaging of the radioactive In 111, which can be used to determine the distribution and tumor localization of PSMA. PSMA is a transmembrane peptidase that is highly expressed on prostate tumor cells.
indium In 111 monoclonal antibody huPAM4
The humanized monoclonal antibody huPAM4, directed against the pancreatic cancer antigen MUC-1 and radiolabled with the gamma-emitting radioisotope indium I 111, with radioisotopic and antibody activities. Upon administration, indium In 111 monoclonal antibody huPAM4 may bind to MUC-1-positive tumor cells, allowing radioimmunolocalization with gamma scintigraphy. Overexpressed by many tumor cell types, MUC-1 antigen, a mammary-type apomucin, is a high-molecular-weight transmembrane glycoprotein.
indium In 111 panitumumab
A radioimmunoconjugate composed of panitumumab, a human immunoglobulin G2 (IgG2) monoclonal antibody directed against the epidermal growth factor receptor (EGFR; HER1; ErbB1), labeled with the radioisotope indium In 111, with potential use as an imaging agent upon single photon emission computed tomography/computed tomography (SPECT/CT). Upon administration of Indium In 111 panitumumab, the antibody moiety targets and binds to the extracellular domain of EGFR on tumor cells. Upon SPECT/CT imaging, EGFR-expressing tumor cells can be visualized and assessed. EGFR, a receptor tyrosine kinase overexpressed on the cell surfaces of many tumor cell types, plays a key role in tumor cell proliferation.
indium In 111 pentetate
A sterile, non-pyrogenic, isotonic solution of radioactive indium In 111 diethylenetriamine pentaacetate (DTPA). When administered intrathecally, indium In 111 pentetate percolates up the spinal canal with the cerebrospinal fluid (CSF) to the basal cisterns of the posterior and middle cranial fossas. This agent is used in radionuclide cisternography to image the flow of CSF, for the identification of abnormalities in CSF circulation, for location of sites of CSF leakage, and for evaluation of CSF shunt patency. Normally, this agent does not penetrate into the brain ventricles.
indium In 111 pentetreotide
An indium 111 radioconjugate of pentetreotide, the diethylenetriaminopentaacetic (DTPA) conjugate of the human hormone somatostatin peptide analogue (octreotide), used for radioimaging neuroendocrine tumor cells. The pentetreotide moiety of indium In 111 pentetreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate allows for specific imaging of neuroendocrine tumors that overexpress somatostatin using scintigraphic imaging techniques. In addition, high dose indium In 111 pentetreotide may specifically deliver a cytotoxic dose of gamma radiation to SSTR-positive cells thereby killing SSTR-expressing tumor cells.
indium In 111 pertuzumab
A radioimmunoconjugate composed of a humanized recombinant monoclonal antibody directed against the extracellular dimerization domain of the tyrosine kinase receptor human epidermal growth factor-2 (HER-2) and linked to the gamma-emitting radioisotope indium In 111, with potential use in radioimaging. Upon administration, indium In 111 pertuzumab binds to HER-2. After binding and internalization into HER-2-expressing tumor cells, radioactive In 111 facilitates the detection of HER-2-expressing tumor cells using single photon emission computed tomography (SPECT). This may predict or evaluate the tumor's response to certain HER-2-targeting chemotherapeutics.
indium In 111 tabituximab barzuxetan
A radioconjugate consisting of tabituximab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against Frizzled-10 (FZD10; CD350), conjugated to the diethylenetriaminepentaacetic acid (DTPA) chelator derivative barzuxetan and labeled with the gamma-emitting isotope indium In 111, which may be used to detect FZD10-expressing tumor cells upon gamma scintigraphy. Upon administration of indium In 111 tabituximab barzuxetan, tabituximab targets and binds to FZD10 expressed on tumor cells. This allows for visualization of FZD10-expressing tumor cells upon gamma scintigraphy. FZD10, a member of the Frizzled family of G protein-coupled receptors, is one of the components in the Wnt/beta-catenin signaling pathway that plays key roles in embryogenesis and cancer growth.
indium In 111 vofatamab
A radioimmunoconjugate composed of vofatamab, a human immunoglobulin G1 (IgG1) monoclonal antibody directed against the fibroblast growth factor receptor type 3 (FGFR3) labeled, via a bifunctional chelate, with the radioisotope indium In 111, with potential use as an imaging agent upon single photon emission computed tomography/computed tomography (SPECT/CT). Upon administration of Indium In 111 vofatamab, the vofatamab moiety specifically targets and binds to FGFR3. Upon SPECT/CT imaging, FGFR3-expressing tumor cells can be visualized. FGFR3, a receptor tyrosine kinase upregulated or mutated in many tumor cell types, plays a key role in tumor cell proliferation.
indium In 111-ABD147
A radioimmunoconjugate consisting of ABD147, an antibody fragment directed against the tumor-associated antigen (TAA) delta-like protein 3 (DLL3) conjugated to the radioisotope indium In 111 (111In), with potential imaging activity. Upon administration of indium In 111-ABD147, ABD147 targets and binds to DLL3 on DLL3-expressing tumor cells. Upon uptake and imaging, DLL3-expressing tumor cells can be visualized. This allows the assessment of DLL3 expression on tumor cells as well as tumor uptake of the agent. 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.
indium In 111-autologous CMV-pp65-LAMP mRNA-loaded dendritic cells
A radioimmunoconjugate composed of mature autologous dendritic cells (DCs) generated from peripheral blood leukocytes pulsed with mRNA encoding for a fusion protein comprised of the human cytomegalovirus (CMV) matrix protein pp65 (65 kDa lower matrix phosphoprotein; UL83) fused with the lysosome-associated membrane protein (pp65-LAMP) and radiolabeled with the isotope indium In 111, with potential ability to track DC migration upon single-photon emission computed tomography (SPECT)/ computed tomography (CT). Upon intradermal injection of the indium In 111-autologous CMV pp65-LAMP mRNA loaded DCs into the groin area, the DCs migrate in vivo to the inguinal lymph nodes. Upon SPECT/CT imaging, DC in vivo migration to the lymph nodes can be assessed.
indium In 111-CMD-193
A radiolabeled antibody-targeted antineoplastic antibiotic consisting of the enediyne antibiotic calicheamicin conjugated with anti-Lewis Y antibody and labeled with indium In 111. In 111 CMD-193 binds to Lewis Y antigen-expressing tumor cells via its antibody moiety and is internalized; subsequently, the calicheamicin moiety binds to the minor groove of tumor cell DNA, causing double-strand DNA breaks, the inhibition of DNA synthesis, and apoptosis. The indium In 111 radiolabel allows the detection of CMD-193 distribution and tumor localization using gamma scintigraphy.
indium In 111-DOTA-basiliximab
A radioimmunoconjugate composed of basiliximab, a chimeric, mouse-human monoclonal antibody directed against the alpha subunit of interleukin-2 receptor (IL-2R alpha, CD25 or Tac antigen), and conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with the radioisotope indium In 111, with potential use as an imaging agent. Upon administration of indium In 111-DOTA- basiliximab, the basiliximab moiety targets and binds to IL-2R alpha expressed on the surface of activated T lymphocytes. Upon binding and gamma scintigraphy, IL-2R alpha-expressing T cells can be visualized and the binding and biodistribution of basiliximab can be assessed.
indium In 111-DOTA-biotin
A radioimmunoconjugate of biotin conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with indium 111 (In-111). Biotin is a water-soluble B-complex vitamin, present in minute amounts in every living cell, while its level in cancerous tissue is higher than that of normal tissue. In 111-DOTA-Biotin could be used in 3-step pre-targeting radioimmunotherapy that employs tumor targeting antibody conjugated with streptavidin, the natural ligand of biotin.
indium In 111-DOTA-daratumumab
A radioimmunoconjugate containing daratumumab, a human immunoglobulin G1 kappa (IgG1k) monoclonal antibody directed against the cell surface glycoprotein CD38, conjugated to the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA), and labeled with the radioisotope indium In 111, with potential use as an imaging agent. Upon administration, the monoclonal antibody moiety of indium In 111-DOTA-daratumumab specifically targets and binds to cell surface antigen CD38. Upon binding and gamma scintigraphy, CD38-expressing tumor cells can be visualized, and the binding and biodistribution of daratumumab can be assessed. CD38, a cell surface glycoprotein, is expressed on various hematopoietic cells and is overexpressed on multiple myeloma (MM) cells.
indium In 111-DOTA-exendin-4
A radiopharmaceutical composed of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the positron-emitting radionuclide indium In 111, with potential use in diagnostic imaging upon positron emission tomography (PET). Upon administration of indium In 111-DOTA-exendin-4, the exendin-4 moiety binds to GLP-1R and is subsequently internalized. The radionuclide moiety can be detected using PET and GLP-1R-expressing tumors can be localized. GLP-1R, located on beta cells, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors.
indium In 111-DOTA-girentuximab
A radioimmunoconjugate comprised of the chimeric monoclonal antibody girentuximab conjugated with the gamma-emitting radioisotope indium In 111. Indium In 111-DOTA-girentuximab binds to G250, allowing the localization of G250-expressing tumor cells using gamma scintigraphy. Found in the majority of renal cell carcinomas (RCCs), G250 or carbonic anhydrase isozyme IX (CA IX) is a cell surface tumor-associated antigen (TAA).
indium In 111-DOTA-h11B6
A radioimmunoconjugate containing the recombinant immunoglobulin G1 (IgG1) kappa humanized monoclonal antibody h11B6 that targets human kallikrein-2 (HK2) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with the radioisotope indium In 111, with potential use as an imaging agent. Upon administration of indium In 111-DOTA-h11B6, the h11B6 moiety targets and binds to HK2. Upon binding and radioimaging, HK2-expressing tumor cells can be visualized and the binding of h11B6 can be assessed. HK2 is overexpressed on a variety of cancer cells.
indium In 111-FL-020
A radioconjugate composed of FL-020, a human prostate-specific membrane antigen (PSMA)-targeting ligand, conjugated to the radioisotope indium In 111, with potential imaging activity during single photon emission computed tomography (SPECT)/computed tomography (PET/CT). Upon administration of indium In 111-FL-020, FL-020 targets and binds to PSMA-expressing tumor cells, followed by internalization and retention of the radioisotope. This allows for imaging of PSMA-expressing tumor cells using gamma scintigraphy. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells as well as a variety of other solid tumors.
indium In 111-FPI-1547
A radioimmunoconjugate composed of FPI-1175 (AVE1642), a humanized monoclonal antibody against insulin-like growth factor-1 receptor (IGF-1R) linked, via the bifunctional chelate FPI-1397, to the radioisotope indium-111 (111In or In-111), with potential imaging activity upon single photon emission computed tomography (SPECT). Upon administration of indium In 111-FPI-1547, the FPI-1547 moiety targets and binds to IGF-1R expressed on tumor cells. Upon uptake and imaging, IGF-1R-expressing tumor cells can be visualized. This allows assessment of IGF-1R expression on tumor cells as well as tumor uptake of the agent. The linker promotes increased clearance of the radioisotope.
indium In 111-labeled autologous peripheral blood mononuclear cells
A preparation of autologous peripheral blood mononuclear cells (PBMCs) radiolabeled with indium In 111 with radioisoptoic activity. Autologous PBMCs are isolated, expanded ex vivo, radiolabeled with indium In 111, and then infused back into the patient. Gamma scintigraphy may then be used to image gamma ray-emitting indium In 111 PBMCs localized in lymhoma tissue.
indium In 111-labeled autologous polymorphonuclear leukocytes
A preparation of autologous peripheral polymorphonuclear (PMNLs) radiolabeled with indium In 111 with radioisoptic activity. Autologous PMNLs are isolated, expanded ex vivo, radiolabeled with indium In 111, and then infused back into the patient. Gamma scintigraphy may then be used to image gamma ray-emitting indium In 111 PMNLs localized in lymphoma tissue.
indium In 111-XYIMSR-01
A radioconjugate consisting of XYIMSR-01, a bivalent low molecular weight ligand targeting two separate sites on carbonic anhydrase IX (CAIX), conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and labeled with indium In 111 (111In), with potential imaging activity during single photon emission computed tomography (SPECT). Upon administration of indium In 111-XYIMSR-01, XYIMSR-01 targets and binds to CAIX-expressing tumor cells, followed by internalization and retention of the radioisotope. This allows for imaging of CAIX-expressing tumor cells upon SPECT. CAIX is overexpressed in various tumors and plays a key role in intra- and extracellular pH regulation, cancer cell progression, survival, migration and invasion.
indium In-111-DOTA-di-HSG peptide IMP-288
A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide indium (In) 111. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered indium-In-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; In-111 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized scintigraphically.
individualized MVA-based vaccine TG4050
An off-the-shelf (OTS) individualized vaccine comprised of a modified Vaccinia virus Ankara (MVA) viral vector encoding tumor-specific neoantigens (TSNAs), with potential immunostimulatory and antineoplastic activities. Following administration of the individualized MVA-based vaccine TG4050, the neoantigens are expressed and presented to the immune system, which induces the activation of a specific cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing the patient-specific neoantigens.
Indocin
(Other name for: indomethacin)
indocyanine green solution
A sterile solution of a nontoxic tricarbocyanine dye with a peak spectral absorption at 790 nm, with application in determining cardiac output, hepatic function, liver blood flow, as well as ophthalmic angiography. Designed to be administered intravenously, indocyanine green solution (ICG) contains less than 5% sodium iodide. Upon intravenous injection, ICG rapidly binds to its principle carrier, plasma protein, and is thereby confined to the vascular space. This agent, with a half-life of 150 to 180 seconds, is removed exclusively by the liver from circulation to bile juice. Furthermore, due to poor uptake, ICG is not suitable for angiography or functional output analysis of kidney, lung, cerebro-spinal, or peripheral tissues.
indocyanine green/albumin solution
A solution containing a non-toxic, fluorescent tricarbocyanine dye with a peak spectral absorption at 790 nm bound to the plasma protein albumin, that may be used in sentinel node mapping using a near infrared (NIR) imaging system. Upon injection of the indocyanine green (ICG)/albumin solution around the tumor, the ICG/albumin complex, travels though the vascular system. Using a NIR imaging system, the ICG, which emits light in the NIR range, permits the visualization of sentinel nodes and may help in cancer staging.
indole-3-carbinol
A naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, a natural compound present in a wide variety of plant food substances including members of the family Cruciferae with antioxidant and potential chemopreventive properties. Indole-3-carbinol scavenges free radicals and induces various hepatic cytochrome P450 monooxygenases. Specifically, this agent induces the hepatic monooxygenase cytochrome P4501A1 (CYP1A1), resulting in increased 2-hydroxylation of estrogens and increased production of the chemoprotective estrogen 2-hydroxyestrone.
indole-3-carbinol/calcium/Schizandra/vitamin D3/milk thistle/stinging nettle/lignan-based nutritional capsule
An orally available capsule-based nutritional supplement containing indole-3-carbinol, calcium-D-glucarate, Schizandra, vitamin D3, milk thistle, stinging nettle and hydroxymatairesinol (HMR) lignans, with potential estrogen modulating, antiproliferative and antioxidant activity. Indole-3-carbinol, found in vegetables of the Cruciferae family, may inhibit mammary cell growth and exerts antiestrogenic activity; Milk thistle (Silybum marianum) and Schizandra chinensis may enhance some of the phase II detoxification enzymes; calcium-D-glucarate and vitamin D3 may inhibit mammary cell growth; stinging nettle may exert its effect through its aromatase inhibiting activity; HMR lignans may have a beneficial effect on estrogen balance and levels. Therefore, ingredients in indole-3-carbinol/calcium/Schizandra/vitamin D3/milk thistle/stinging nettle/lignan-based nutritional capsule may alter estrogen balance and may protect against mammary carcinogenesis.
indoleamine 2,3-dioxygenase peptide vaccine
A peptide vaccine against the immunomodulatory enzyme indoleamine 2,3-dioxygenase (IDO), with potential immunomodulating and antineoplastic activities. Vaccination with indoleamine 2,3-dioxygenase peptide vaccine may activate the immune system to induce an immune response against IDO-expressing cells. This may increase and restore the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T-lymphocytes, and may eradicate IDO-expressing tumor cells. IDO, a cytosolic enzyme responsible for tryptophan catabolism and conversion of tryptophan into kynurenine, is overexpressed by a variety of tumor cell types and antigen presenting cells (APCs) and plays an important role in immunosuppression; tryptophan depletion inhibits T-lymphocyte proliferation and activation, and suppresses the immune system.
indomethacin
A synthetic nonsteroidal indole derivative with anti-inflammatory activity and chemopreventive properties. As a nonsteroidal anti-inflammatory drug (NSAID), indomethacin inhibits the enzyme cyclooxygenase, thereby preventing cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines. This agent also may inhibit the expression of multidrug-resistant protein type 1, resulting in increased efficacies of some antineoplastic agents in treating multi-drug resistant tumors. In addition, indomethacin activates phosphatases that inhibit the migration and proliferation of cancer cells and downregulates survivin, which may result in tumor cell apoptosis.
indoximod
A methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.
indoximod prodrug NLG802
An orally bioavailable prodrug of indoximod, a methylated tryptophan, with immune checkpoint inhibitory and antineoplastic activities. Upon oral administration, the indoximod prodrug NLG802 is converted to indoximod. Indoximod targets, binds to and inhibits the enzyme indoleamine 2,3-dioxygenase (IDO; IDO1), which converts the essential amino acid tryptophan into the immunosuppressive metabolite kynurenine. By increasing tryptophan levels and decreasing kynurenine levels, indoximod restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may induce a cytotoxic T-lymphocyte (CTL) response against IDO1-expressing tumor cells, thereby inhibiting their growth. IDO1, overexpressed by multiple tumor cell types, plays an important role in immunosuppression. Tryptophan depletion inhibits T-lymphocyte proliferation and activation, and subsequently suppresses the immune system. NLG802 elicits increased plasma concentrations of indoximod and improves its efficacy, compared to the direct administration of indoximod.
inducible CD4+CD25+ regulatory T cells
Inducible regulatory T-lymphocytes that express CD4, CD25 (the alpha chain of the interleukin 2 receptor) and forkhead box P3 (FOXP3), with potential immunomodulating activity. Inducible CD4+CD25+ T regulatory cells (iTregs) are a subset of CD4+ T lymphocytes that are induced from CD25- precursors in peripheral lymphoid organs with interleukin-2 and transforming growth factor-beta. These regulatory T cells are essential in maintaining immunologic homeostasis. They may also prevent autoimmunity by suppressing self-reactive T cells, and may induce tolerance to allogeneic organ transplants such as in hematopoietic stem cell transplants.
inebilizumab
A humanized immunoglobulin IgG1 kappa monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential immunostimulating and antineoplastic activities. Inebilizumab binds to CD19, which may result in a cytotoxic T-lymphocyte (CTL) response and antibody-dependent cellular cytotoxicity (ADCC) to CD19-expressing B-cells. The Fc portion of inebilizumab does not contain a fucose sugar moiety, which may contribute to its enhanced ADCC activity. CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.
inecalcitol
An analog of calcitriol and a vitamin D3 receptor (VDR) agonist, with potential antineoplastic activity. Upon administration, inecalcitol targets and binds to VDR. This activates VDR and VDR-mediated signal transduction pathways. This modulates the VDR-mediated expression of certain genes, including the expression of anti-cancer genes, enhances cellular differentiation, induces tumor cell apoptosis and inhibits tumor cell growth. VDR plays a central role in calcium homeostasis and in the growth of certain cancer cells.
inetetamab
An Fc-engineered monoclonal antibody targeting the tyrosine kinase receptor epidermal growth factor receptor 2 (HER2; ErbB2), with potential immunomodulating and antineoplastic activities. Upon administration, inetetamab targets and specifically binds to HER2 on tumor cells, thereby blocking HER2-mediated signaling. This may inhibit proliferation of HER2-expressing tumor cells. In addition, the Fab region of inetetamab may induce antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed in a variety of cancer cell types and is associated with increased tumor cell proliferation.
Infanrix
(Other name for: diphtheria toxoid/tetanus toxoid/acellular pertussis vaccine adsorbed)
Infasurf
(Other name for: calfactant)
infasurf intratracheal suspension
(Other name for: calfactant)
Infergen
(Other name for: interferon alfacon-1)
infigratinib phosphate
The phosphate salt form of infigratinib, an orally bioavailable pan-inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. Upon administration, infigratinib selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of angiogenesis and cell proliferation, and the induction of cell death in tumors with activating FGFR amplifications, mutations, or fusions. FGFRs are a family of receptor tyrosine kinases that are involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival. Activating FGFR amplifications, mutations, or fusions occur in various cancer cell types.
infliximab
A recombinant chimeric, mouse-human monoclonal antibody directed against tumor necrosis factor alpha (TNF-alpha), a protein involved in inflammation, cell survival, and apoptosis. Infliximab may be pro- apoptotic or anti-apoptotic, depending on cell type.
Infugem
(Other name for: gemcitabine hydrochloride)
Infumorph
(Other name for: morphine sulfate)
ingenol derivative LEO 43204 gel
A topical, aqueous gel formulation containing a derivative of ingenol, a selective small-molecule activator of protein kinase C (PKC) that is isolated from the sap of Euphorbia species, with the potential to treat preneoplastic skin lesions. Upon topical application of the ingenol derivative LEO 43204 gel, the agent presumably activates various PKC isoforms, which may induce apoptosis in abnormal cells found in severely sun-damaged skin with multiple actinic keratoses. This may decrease the number of actinic keratoses and prevent the development of skin neoplasms. The PKC family consists of signaling isoenzymes that regulate many cell processes, including proliferation, differentiation, and apoptosis.
ingenol mebutate
A selective small-molecule activator of protein kinase C (PKC) isolated from the plant Euphorbia peplus with potential antineoplastic activity. Ingenol mebutate (I3A) activates various protein kinase C (PKC) isoforms, thereby inducing apoptosis in some tumor cells, including myeloid leukemia cells, melanoma cells, and basal cell carcinoma cells. The PKC family consists of signaling isoenzymes that regulate many cell processes including proliferation, differentiation, and apoptosis.
ingenol mebutate gel
A topical, aqueous gel formulation containing the mebutate salt form of ingenol, a selective small-molecule activator of protein kinase C (PKC) that is isolated from the sap of Euphorbia species, with potential antineoplastic activity. Upon topical application of the ingenol mebutate gel, ingenol activates various PKC isoforms, which induces apoptosis in certain tumor cells, including myeloid leukemia cells, melanoma cells, and basal cell carcinoma cells. The PKC family consists of signaling isoenzymes that regulate many cell processes, including proliferation, differentiation, and apoptosis.
inhaled voriconazole
An inhaled formulation of voriconazole, a synthetic triazole with antifungal activity. Upon administration by inhalation, voriconazole selectively inhibits 14-alpha-lanosterol demethylation in fungi, preventing the production of ergosterol, an essential constituent of the fungal cell membrane, and resulting in fungal cell lysis.
iniparib
A small molecule iodobenzamide with potential cytotoxic and antineoplastic activities. Although the mechanism of action is unknown, iniparib appears to be cytotoxic in cells with DNA alterations or DNA damage, like that found in tumor cells with mutations in the ataxia telangiectasia mutated (ATM) gene. ATM encodes a serine/threonine protein kinase and mutations of the gene are associated with ataxia telangiectasia and contribute to certain cancers such as T-cell acute lymphoblastic leukemia, B-cell chronic lymphocytic leukemia and B-cell non-Hodgkin lymphomas.
injectable Astragalus membranaceus polysaccharide
An injectable form of a polysaccharide isolated from the radix of Astragalus membranaceus (PG2), used in traditional Chinese medicine, with potential hematopoiesis inducing and immunomodulating activities. Upon injection, APS may be able to relieve certain chemotherapy-induced side effects, including myelosuppression, fatigue, mucositis, pain, nausea and vomiting, as well as loss of appetite and body weight. Also, APS may exert immunostimulatory activities by stimulating B-lymphocytes, activating T-lymphocytes, inducing cytokine production, and activating macrophages and natural killer cells through as of yet unidentified mechanism(s). APS may improve compliance of radiotherapy and/or chemotherapy.
Injectafer
(Other name for: ferric carboxymaltose solution)
iNKT cell agonist ABX196
A synthetic glycolipid agonist for natural killer T cells (NKTs) expressing an invariant (alpha, beta) T-cell receptor (iNKTs), with potential immunomodulating and antineoplastic activities. Upon infusion of the iNKT cell agonist ABX196, this agent targets and binds to iNKTs, thereby activating iNKTs. In turn, iNKTs 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.
Inlyta
(Other name for: axitinib)
innate defense regulator SGX942
A synthetic, 5-amino acid peptide and innate defense regulator (IDR), with immunomodulating, anti-inflammatory, anti-infective and anti-mucositis activities. Upon intravenous administration, SGX942 binds to the ZZ domain of sequestosome-1, also called p62, and activates regulatory signaling transduction pathways involved in the modulation of the innate immune system, such as those mediated by mitogen-activated protein kinase (MAPK) p38 and CCAAT-enhancer-binding protein. This agent promotes monocyte and macrophage recruitment to, and accelerates healing in damaged and infected tissue; it suppresses inflammation through the regulation of the expression of multiple cytokines. This agent may prevent or decrease chemo- or radiotherapy-induced mucositis as well as other types of infection. p62, an intracellular adaptor protein that functions downstream of certain signaling receptors, plays a key role in the activation of the innate immune system.
innate immunostimulator rBBX-01
A recombinant 19 kDa protein derived from the Apicomplexa protozoan Eimeria with potential immunostimulating and antitumor activities. Upon administration, innate immunostimulator rBBX-01 activates dendritic cells (DCs), stimulates the Toll-like receptor 11 (TLR-11)-mediated release of interleukin-12 (Il-12) from DCs, and induces a T-helper 1 (Th1) type immune response, which may induce an immune response against tumor cells. Infection with Eimeria, a coccidian commonly infecting the intestine, may be negatively correlated with tumorigenesis.
Inno-hep
(Other name for: tinzaparin sodium)
Innohep
(Other name for: tinzaparin sodium)
INO-1001
A isoindolinone derivative and potent inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with chemosensitization and radiosensitization properties. INO-1001 inhibits PARP, which may result in inhibition of tumor cell DNA repair mechanisms and, so, tumor cell resistance to chemotherapy and radiation therapy. PARP enzymes are activated by DNA breaks and have been implicated in the repair of DNA single-strand breaks (SSB).
inodiftagene vixteplasmid
A recombinant DNA plasmid carrying the gene for diphtheria toxin-A (dT-A) chain under the regulation of the H19 promoter, with potential antineoplastic activity. Upon intravesical administration, dT-A chain expression is triggered by the presence of H19 transcription factors that are upregulated in tumor cells. The dT-A chain binds to nicotinamide adenine dinucleotide (NAD) and inactivates the ADP-ribosylation of elongation factor 2 (EF2), resulting in the inhibition of protein synthesis and cell death leading to tumor cell destruction. Inodiftagene Vixteplasmid does not carry the gene for the diphtheria toxin-B (dT-B) chain, thereby preventing the transfer of the toxic dT-A chain between cells. H19, a paternally imprinted, oncofetal gene, is highly expressed in embryonic and certain malignant tissues, but minimally expressed in normal, adult tissues.
inosine 5'- monophosphate dehydrogenase inhibitor FF-10501-01
An orally bioavailable inhibitor of inosine 5'- monophosphate dehydrogenase (IMPDH), with potential antineoplastic activity. Upon administration, IMPDH inhibitor FF-10501-01 competitively inhibits the enzyme IMPDH, thereby preventing the conversion of inosine monophosphate to xanthosine monophosphate. This inhibits the synthesis of guanine nucleotides, deprives cancer cells of guanosine triphosphate (GTP), disrupts DNA and RNA synthesis, and decreases tumor cell proliferation. Tumor cells are highly susceptible to IMPDH inhibition because they are rapidly dividing cells that are dependent on rapid DNA synthesis, which requires a high concentration of nucleotides. IMPDH, an enzyme that catalyzes the rate-limiting step in the synthesis of guanosine triphosphate (GTP), is overexpressed in numerous tumor cell types.
inosine dialdehyde
A toxic purine analogue. Inosine dialdehyde inhibits ribonucleotide reductase, resulting in decreased synthesis of DNA, RNA, and proteins, and G2/M-phase cell cycle arrest. This agent also forms stable covalent crosslinks in proteins, thereby inhibiting the activity of enzymes involved in nucleic acid synthesis.
inosine pranobex
A formulation containing inosine, 4-acetamidobenzoic Acid, and N,N-dimethylaminoisopropanol, with immunomodulatory and antiviral activities. Although the exact mechanism of action is unknown, inosine pranobex appears to act as a thymus hormone analog; following administration, this agent may both induce T-cell differentiation and potentiate lymphoproliferative responses against transformed or virally-infected cells.
inositol
A natural sugar found in cell membrane phospholipids, plasma lipoproteins, and (as the phosphate form) in the nucleus with potential chemopreventive properties. As one of a number of intracellular phosphate compounds, inositol is involved in cell signaling and may stimulate tumor cell differentiation.
inotersen
An antisense oligonucleotide (ASO) targeting transthyretin (TTR), which has potential use in the treatment of TTR amyloidosis (ATTR). Upon subcutaneous administration, inotersen targets and binds to messenger RNA (mRNA) for both variant and wild-type forms of TTR inside liver cells, thereby inhibiting translation of both mutant and wild-type TTR. Inhibition of TTR protein synthesis lowers TTR blood levels and decreases the amount of and/or prevents TTR amyloid deposits, which accumulate in and cause damage to various body organs and tissues. ATTR is caused by mutations in the TTR gene, which lead to TTR protein misfolding; misfolded wild-type and mutant forms of TTR protein accumulate in tissues as amyloid deposits in most ATTR patients.
inotuzumab ozogamicin
A CD22-targeted cytotoxic immunoconjugate composed of a humanized IgG4 anti-CD22 antibody covalently linked to N-acetyl-gamma-calicheamicin dimethyl hydrazide (CalichDMH) with potential antineoplastic activity. Inotuzumab ozogamicin is rapidly internalized upon binding of the antibody moiety to B cell-specific CD22 receptors, delivering the conjugated CalichDMH intracellularly; the CalichDMH moiety binds to the minor groove of DNA in a sequence-specific manner, resulting in double-strand DNA breaks and apoptosis. CalichDMH is a derivative of gamma calicheamicin, a cytotoxic antibiotic produced by the bacterium Micromonospora echinospora.
Inqovi
(Other name for: decitabine and cedazuridine)
Inrebic
(Other name for: fedratinib hydrochloride)
INS316
A short-acting, aerosolized uridine 5-triphosphate (UTP) solution used as a diagnostic aid for lung cancer. INS316 appears to improve sputum expectoration mediated through the P2Y2 receptor, a nucleotide receptor expressed in human airway epithelial cells and some other tissues. UTP binding to the P2Y2 receptor triggers signal transduction that leads to chloride ion secretion, thereby resulting in mucociliary clearance of airway.
Insegia
(Other name for: gastrin immunotoxin)
Inspra
(Other name for: eplerenone)
insulin lispro
A recombinant therapeutic agent which is chemically identical to or similar to endogenous human insulin. In lispro insulin, the amino acid proline at B-28 and the amino acid lysine at B-29 are reversed, resulting in the rapid dissolution of this insulin to a monomer that is absorbed rapidly after subcutaneous administration. Lispro insulin is equipotent to human insulin on a molar basis but its effects are faster and of shorter duration. Endogenous insulin, a pancreatic hormone composed of two polypeptide chains, is important in the normal metabolism of carbohydrates, proteins and fats, promoting glucose utilization and protein synthesis; it has anabolic effects on many types of tissues.
insulin sensitizer S-707106
An orally available protein and insulin sensitizer with anti-hyperglycemic activity. Upon oral administration, S-707106 increases the sensitivity of target organs to insulin, through an as of yet not fully elucidated mechanism. This agent may lower blood glucose levels.
insulin, NPH
An intermediate-acting insulin used in the treatment of diabetes mellitus. Administered once or twice daily, NPH (neutral protamine hagedorn) insulin lowers blood glucose within 1 to 2 hours after administration and exerts a peak effect at 6 to 10 hours. Endogenous insulin, a pancreatic hormone composed of two polypeptide chains, is important in the normal metabolism of carbohydrates, proteins and fats, promoting glucose utilization and protein synthesis; it has anabolic effects on many types of tissues.
insulin, regular
A recombinant form of the naturally occurring human pancreatic hormone insulin. Upon administration, regular insulin mimics the action of endogenous human insulin and binds to insulin receptors located on muscle and fat cells. This both facilitates the cellular uptake of glucose and lowers blood glucose levels. In addition, insulin inhibits the liver's conversion of stored glycogen into glucose, which also decreases blood glucose levels. Insulin also inhibits lipolysis in adipose tissue, inhibits proteolysis, and enhances protein synthesis.
integrin alpha-2 inhibitor E7820
A small molecule and aromatic sulfonamide derivative with potential antiangiogenic and antitumor activities. E7820 inhibits angiogenesis by suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. Inhibition of integrin alpha 2 leads to an inhibition of cell-cell interactions, endothelial cell-matrix interactions, vascular endothelial cell proliferation and angiogenesis.
integrin alphaVbeta3-targeted small molecule-drug conjugate VIP236
A small molecule-drug conjugate (SMDC) composed of an integrin alphaVbeta3 binder conjugated, via a cleavable linker, to a camptothecin-based topoisomerase I inhibitor, with potential antineoplastic activity. Upon administration of integrin alphaVbeta3-targeted SMDC VIP236, the integrin alphaVbeta3 binder targets and binds to integrin alphaVbeta3 expressed on tumor cells and tumor vessel endothelial cells. Upon binding and linker cleavage by neutrophil elastase in the tumor microenvironment (TME), the camptothecin-based topoisomerase I inhibitor is released. The topoisomerase I inhibitor inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and generating DNA single- and double-strand breaks, and leading to cell cycle arrest and apoptosis. This inhibits the proliferation of integrin alphaVbeta3-expressing tumor cells, angiogenesis and metastasis. Integrin alphaVbeta3, 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.
integrin receptor antagonist GLPG0187
A small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity. Upon administration, GLPG0187 binds to and blocks the activity of 5 RGD-integrin receptor subtypes, including alphavbeta1, alphavbeta3, alphavbeta5, alphavbeta6 and alpha5beta1. This may result in the inhibition of endothelial cell-cell interactions and endothelial cell-matrix interactions, and the prevention of angiogenesis and metastasis in tumor cells expressing these integrin receptors. Integrin receptors are transmembrane glycoproteins expressed on the surface of tumor vessel endothelial cells and some types of cancer cells, and play a crucial role in endothelial cell adhesion and migration.
Intercoat
(Other name for: absorbable adhesion barrier gel)
interferon alfacon-1
An analogue of consensus interferon which contains an additional methionyl amino acid residue. Consensus interferon (also known as interferon alfacon-1, rCon-IFN, and CIFN) is a genetically engineered synthetic interferon created from the most common amino acid sequences from the naturally occurring alpha interferons. Alpha interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects.
interferon beta-secreting mesenchymal stem cells
Human autologous mesenchymal stem cells (MSCs) harvested from the bone marrow of healthy individuals and transduced with a retroviral vector encoding the human cytokine interferon beta (IFNb), with potential immunomodulating and antineoplastic activities. Upon administration of IFNb-secreting MSCs, the cells are attracted and specifically migrate to tumor sites and become part of the tumor microenvironment. Since the MSCs express IFNb, these cells selectively deliver high levels of IFNb to the tumor site. In turn, IFNb binds to IFN-specific cell surface receptors and modulates the transcription and translation of certain genes whose protein products are involved in tumor cell proliferation. This decreases tumor cell growth.
interferon gamma-1b
A recombinant form of the endogenous cytokine interferon-gamma (IFN-gamma; IFNg), with a peptide length of 140 amino acids and modified with an N-terminal methionyl group, with potential immunomodulating and antineoplastic activities. Upon administration, IFNg-1b binds to IFNg cell surface receptors (IFNGRs), activates IFNg-stimulated signaling pathways, including the JAK-STAT pathway, and leads to the transcription of multiple IFNg-controlled genes, the expression of which may activate certain components of the immune system. IFNg activates natural killer (NK) cells, macrophages, and cytotoxic T lymphocytes (CTLs), stimulates antibody-dependent cellular cytotoxicity (ADCC) and induces the expression of major histocompatibility complex (MHC) molecules, which leads to an increase in antigen presentation, including tumor-associated antigens (TAAs), to the immune system, and modulates the expression of certain pro-inflammatory cytokines by antigen-presenting cells (APCs). Altogether, this increases tumor cell killing. IFNg-1b, a cell-signaling protein, plays a key role in the regulation and activation of the immune system.
interferon gamma-primed human bone marrow-derived mesenchymal stromal cells
Human bone marrow-derived mesenchymal stromal cells (MSCs) primed with interferon gamma (IFN-g), with potential immunomodulatory activity. Upon priming with IFN-g and the administration of IFN-g-primed human bone marrow-derived MSCs, IFN-g activates the IFN-g-Janus kinase (JAK)-signal transducer and activator of transcription 1 (STAT1) signaling pathway and induces indoleamine 2,3-dioxygenase (IDO) expression in MSCs. This promotes IDO activity and enhances the inhibition of T-cell proliferation mediated by MSCs. This may enhance MSC-mediated immunosuppression and prevent graft-versus-host disease (GvHD).
interferon-gamma-expressing adenovirus vaccine ASN-002
A replication-defective adenoviral serotype 5 vector encoding a recombinant form of the human cytokine interferon-gamma (IFN-g), with potential antineoplastic and immunoregulatory activities. Upon intratumoral administration, the sustained expression of IFN-g by IFN-g-expressing adenovirus vaccine ASN-002 promotes a T-helper type 1 (Th1) immune response and inhibits the Th2-mediated cytokine production observed in many cutaneous lymphomas. IFN-g also mediates interleukin-12 (IL-12) production by antigen-presenting cells (APCs); activates macrophages, cytotoxic T-cells, and natural killer (NK) cells; upregulates major histocompatibility complex (MHC) molecules; and stimulates antibody-dependent cellular cytotoxicity (ADCC). Altogether, these IFN-g-mediated effects may result in both an inhibition of tumor cell proliferation and tumor cell death. Compared to IFN-g injections, the prolonged local production of IFN-g at the tumor site allows for higher efficacy and a reduction of systemic toxicity.
interleukin-12 gene
The DNA sequence that encodes the protein cytokine interleukin-12 (IL-12). When introduced as the complementary DNA (cDNA) form into tumor cells by, for example, a genetically engineered adenovirus vector, the transfected IL-12 cDNA expresses IL-12 which activates antitumoral natural killer (NK) cells and CD8+ T-cells and stimulates the secretion of interferon-gamma (IFN-gamma), potentially inhibiting tumor cell metastasis. This gene therapy may also result in IL-12-mediated inhibition of vascular endothelial growth factor (VEGF) and enhancement of matrix metalloproteinases (MMPs).
interleukin-12-Fc fusion protein DF6002
A fusion protein composed of human Interleukin-12 (IL-12) fused to a Fc fragment, with potential immunomodulatory and antineoplastic activities. Although the exact mechanism of action has not been completely characterized, upon administration, the IL-12 moiety binds to the IL-12 receptor. This may activate the immune system by promoting the secretion of interferon-gamma, activating natural killer cells (NKs), and inducing cytotoxic T-lymphocyte (CTL) responses, which may result in both decreased tumor cell proliferation and enhanced immune-mediated destruction of tumor cells.
interleukin-15 agonist fusion protein SHR1501
A human Fc fusion protein composed of the cytokine interleukin (IL)-15 cross-linked with the high-affinity binding sushi domain of IL-15 receptor alpha (IL-15Ra), with potential antineoplastic activity. Upon administration, SHR-1501 activates and increases the levels of natural killer (NK) cells and memory CD8+ T cells without stimulating regulatory T cells (Tregs). The memory T cells enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. This may increase tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T- and NK-cell development, activation and proliferation. SHR1501 is more potent than unmodified IL-15 and does not require endogenous IL-15Ra for its action. The Fc moiety allows for an extended half-life of SHR-1501 while cross linking IL-15 with IL-15Ra sushi domain improves stability.
interleukin-15 fusion protein BJ-001
A human fusion protein composed of the cytokine interleukin (IL)-15 linked with an integrins-targeting moiety, with potential antineoplastic activity. Upon subcutaneous administration, the integrins-targeting moiety of BJ-001 targets tumor cells that overexpress integrins such as alpha v beta 3 (avb3), alpha v beta 5 (avb5) and alpha v beta 6 (avb6) and the IL-15 moiety binds to the IL-2/IL-15 receptor beta-common gamma chain (IL-2Rbetagamma) receptor on natural killer (NK) cells and CD8+ T lymphocytes. This activates and increases the levels of NK cells and memory CD8+ T cells. The memory T cells enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. This may increase tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T- and NK cell development, activation and proliferation. Integrins are involved in tumor growth, angiogenesis, and metastasis and they are overexpressed in a variety of tumor cell types. The linkage of the two moieties may limit the effects of IL-15 to the local tumor microenvironment (TME), increasing efficacy while reducing systemic toxicities.
interleukin-15/interleukin-15 receptor alpha complex-Fc fusion protein XmAb24306
An interleukin (IL)-15/IL-15-receptor alpha (IL-15Ra) complex fused to a bispecific Fc domain, with potential antineoplastic activity. Upon administration, XmAb24306 stimulates the proliferation of natural killer (NK) cells and memory CD8+ T cells. The memory T cells enhance the secretion of the cytokine interferon-gamma (IFN-g), which further potentiates the immune response against tumor cells. This may increase tumor cell killing and decrease tumor cell proliferation. IL-15 regulates CD8+ T and NK cell development, activation and proliferation. XmAb24306 does not require endogenous IL-15Ra for its activation.
interleukin-2 gene
The DNA sequence that encodes the protein cytokine interleukin-2 (IL-2). When introduced as the complementary DNA (cDNA) form into tumor cells by, for example, a genetically engineered adenovirus vector, the transfected IL-2 cDNA expresses IL-2 which may activate antitumoral natural killer cells and elicit an antitumoral cytotoxic T-cell response, resulting in an inhibition of tumor progression.
interleukin-2/interleukin-15 receptor agonist NL-201
An interleukin-2 (IL-2) and interleukin-15 (IL-15) receptor agonist with high binding affinity for the common heterodimeric receptor IL-2Rbeta-gamma, which is composed of the IL-2 receptor subunit beta (IL-2Rbeta; CD122) and IL-2 receptor subunit gamma (IL-2Rgamma; common gamma; CD132), and no binding affinity for the IL-2 receptor subunit alpha (IL-2Ralpha; CD25), with potential immunoregulatory and antineoplastic activities. Upon administration, IL-2/IL-15 receptor agonist NL-201 targets and binds to IL-2Rbeta-gamma on natural killer (NK) and T cells and activates IL-2Rbeta-gamma-mediated signaling. This induces the selective proliferation of CD8+ T cells and NK cells, enhances tumor cell killing and decreases tumor cell proliferation. NL-201 does not bind to IL-2Ralpha, thereby circumventing both the activation of immunosuppressive regulatory T cells (Tregs) and the exacerbation of vascular leak syndrome associated with recombinant human IL-2. IL-2 and IL-15 receptors are cytokine receptors that play key roles in the immune response.
internalized-arginylglycylaspartic acid cyclic peptide
A 9 amino acid-based cyclic, tumor specific homing, arginine-glycine-aspartic acid (RGD)-based peptide (CRGDKRGPDC), with tumor penetrating activity. The iRGD contains the RGD motif as well as the C-terminal end binding (CendR) motif that increases internalization. Upon administration, the RGD motif of the iRGD peptide is able to specifically target tumors by binding to alphavbeta3/alphavbeta5 integrins on tumor endothelium. In turn, iRGD is cleaved by specific tumor proteases, which exposes the positively charged CendR motif. This motif binds to neuropilin-1 (NRP-1), a receptor overexpressed on certain tumor cells. This increases vascular permeability of tumor blood vessels and promotes tumor penetration. Compared to other RGD peptides, this agent is able to both improve delivery and increase the accumulation of co-administered or conjugated chemotherapeutic agents in the tumor.
intetumumab
A pan alpha-v human monoclonal antibody that recognizes alpha-v beta-1, alpha-v beta-3, alpha-v beta-5, and alpha-v beta-6 integrins with antiangiogenic and antitumor activities. Intetumumab competitively binds to and blocks both alpha-v beta-3 and alpha-v beta-5 integrins, resulting in inhibition of integrin-mediated tumor angiogenesis and tumor growth. Integrins facilitate the adhesion of stimulated endothelial cells to the extracellular matrix (ECM); trigger the secretion of ECM-rearranging proteases; and propagate signaling events that promote the survival and differentiation of cells in newly formed vasculature.
IntraDose
(Other name for: cisplatin-E therapeutic implant)
Intralipid
(Other name for: fat emulsion)
intranasal ketamine
An intranasal formualtion of the synthetic cyclohexanone ketamine with analgesic and anesthetic activities. Although its mechanism of action is not well understood, ketamine appears to non-competitively block N-methyl-D-aspartate (NMDA) receptors and agonistically bind to and activate opiod mu and sigma receptors, thereby reducing pain perception, inducing sedation, and producing dissociative anesthesia.
intrathecal deferoxamine
An intrathecal (IT) formulation of deferoxamine (DFO), an iron-chelating agent that can be used to deplete free iron and lower iron levels, and with potential antineoplastic activity. Upon IT administration via Ommaya reservoir, DFO chelates free iron within the cerebrospinal fluid (CSF) by forming the iron complex ferrioxamine. This lowers the amount of iron available for cancer cell growth and survival. Cancer cells show increased iron uptake as iron is needed for rapid tumor cell proliferation.
Intron A
(Other name for: recombinant interferon alfa-2b)
Intuvax
(Other name for: ilixadencel)
inulin
A naturally occurring, indigestible and non-absorbable oligosaccharide produced by certain plants with prebiotic and potential anticancer activity. Inulin stimulates the growth of beneficial bacteria in the colon, including Bifidobacteria and Lactobacilli, thereby modulating the composition of microflora. This creates an environment that protects against pathogens, toxins and carcinogens, which can cause inflammation and cancer. In addition, fermentation of inulin leads to an increase in short-chain fatty acids and lactic acid production, thereby reducing colonic pH, which may further control pathogenic bacteria growth and may contribute to inulin's cancer protective properties.
inupadenant
An orally bioavailable immune checkpoint inhibitor and antagonist of the adenosine A2A receptor (A2AR; ADORA2A), with potential immunomodulating and antineoplastic activities. Upon administration, inupadenant selectively binds to and inhibits A2AR expressed on T lymphocytes. This prevents tumor-released adenosine from interacting with the A2A receptors, thereby blocking the adenosine/A2AR-mediated inhibition of T lymphocytes. This results in the proliferation and activation of T lymphocytes, and stimulates a T-cell-mediated immune response against tumor cells. A2AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of T cells and, upon activation by adenosine, inhibits their proliferation and activation. Adenosine is often overproduced by cancer cells and plays a key role in immunosuppression.
Invanz
(Other name for: ertapenem sodium)
invariant natural killer T cells
A natural killer T-cell subtype bearing an invariant T-cell receptor. Invariant natural killer T cells recognize a small variety of glycolipid antigens presented in the context of CD1d. These cells play a regulatory role during an immune response by producing cytokines.
Invirase
(Other name for: saquinavir mesylate)
INxin
(Other name for: bizaxofusp)
iobenguane
A synthetic, aralkylguanidine analogue of the adrenergic neurotransmitter norepinephrine (NE) and adrenergic neuron blocking agent with potential diagnostic imaging or antineoplastic activity when radiolabeled. Iobenguane, also known as metaiodobenzylguanidine (MIBG), is taken up and accumulates in the granules of adrenal medullary chromaffin cells and in the pre-synaptic granules of adrenergic neurons in a manner almost identical with that of NE. In radiolabeled forms, iobenguane may be used to image or eradicate neuroendocrine tissues and tumor cells.
Iobenguane I-131
An I 131 radioiodinated synthetic analogue of the neurotransmitter norepinephrine. Iobenguane localizes to adrenergic tissue and, in radioiodinated forms, may be used to image or eradicate tumor cells that take up and metabolize norepinephrine.
iobitridol
A water-soluble, tri-iodinated, non-ionic monomeric benzoate derivative and contrast medium used in diagnostic radiography. Upon administration, iobitridol is distributed through the vascular system and interstitial space. Like other organic iodine compounds, this agent blocks x-rays and appears opaque on x-ray film thus, enhancing the visibility of body parts containing this agent. Iobitridol is rapidly removed by the kidneys in an unchanged form, and in cases of renal failure, heterotropic excretion occurs via the biliary route.
iodinated contrast agent
A contrast agent containing an iodine-based dye used in many diagnostic imaging examinations, including computed tomography, angiography, and myelography.
iodinated polyethylene glycol-based hydrogel tissue marker
A radiopaque hydrogel containing cross-linked, iodinated polyethylene glycol (PEG) particles in a viscous carrier, with potential use as a contrast agent to enhance marking of soft tissue during a surgical procedure and concomitant radiotherapy upon computed tomography (CT), magnetic resonance (MR) and ultrasound imaging. Upon intratumoral injection, iodinated PEG-based hydrogel tissue marker localizes to and is maintained in soft tissue. Upon MR, ultrasound and/or CT imaging, the visualization of the tumor tissue is enhanced, which can facilitate tumor removal and image-guided radiotherapeutic treatment. The hydrogel particles are stable and visible through 3 months, after which they liquefy, and are absorbed by the body and cleared in the urine.
iodine 131-6-beta-iodomethyl-19-norcholesterol
A radioiodine-labeled cholesterol analogue with radioisotopic activity. Iodine 131-l-6-beta-iodomethyl-19-norcholesterol accumulates in tissues where steroid hormones are produced, including the adrenal cortex and, to a lesser extent, the ovaries and the testes. After binding to low-density lipoprotein (LDL) receptors in the adrenal cortex, this agent is internalized, permitting scintigraphic localization of areas of adrenocortical glucocorticoid, mineralocorticoid and androgen secretion, and the scintigraphic assessment of adrenocortical function.
iodine I 123
A radioactive isotope of iodine, a nonmetallic element of the halogen group with an atomic mass of 123 and a half-life of 13.2 hours with radioisotopic activity. Selectively accumulating in the thyroid tissue, iodine I 123 emits gamma rays that can be detected with gamma scintigraphy, allowing localization of thyroid tissue. This agent may be used as a tracer in whole body scintigraphy (WBS) to localize thyroid carcinoma metastases.
iodine I 123 ADAM
A radiopharmaceutical containing the serotonin transporter (SERT) ligand ADAM [2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine] labeled with the radioisotope iodine I 123, with SERT-binding and radioisotope activities. Upon administration, iodine I 123 ADAM selectively binds to SERT-expressing cells; subsequently, SERT-expressing tissues may be visualized using single photon emission computed tomography (SPECT). SERT is a monamine transporter protein found in the membranes of neurons and platelets; in neurons it transports the neurotransmitter serotonin from synaptic spaces into presynaptic neurons, terminating serotonin's function.
iodine I 123 anti-CEA recombinant diabody T84.66
A radioimmunoconjugate comprised of a recombinant scFv dimer diabody of a monoclonal antibody against human carcinoembryonic antigen (CEA) labeled with iodine I 123 (I-123) with potential radioimmunolocalization applications. The antibody moiety of iodine I 123 anti-CEA recombinant diabody T84.66 binds to cells expressing CEA, selectively delivering I-123 upon cellular internalization and allowing the scintigraphic imaging of CEA-expressing tumor cells. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. Compared to whole monoclonal antibodies, diabody fragments offer the advantages of rapid tumor targeting, rapid blood clearance, more uniform tumor distribution, and a lower potential for eliciting an immune response.
iodine I 123 iodometomidate
An iodine I-123 conjugate of metomidate (MTO) with potential application in adrenal imaging. Metomidate is a potent and selective inhibitor of the cytochrome P-450 enzymes, especially CYP11B1 (11 beta-hydroxylase) and CYP11B2 (aldosterone synthase). Because both CYP11B1 and CYP11B2 are expressed exclusively in the adrenal cortex, I-123 iodometomidate can be used as a radiotracer for adrenal scintigraphy.
iodine I 124
A radioactive isotope of iodine, a nonmetallic element of the halogen group, with an atomic mass of 124 and a half-life of 4.18 days with radioisotopic activity. Selectively accumulating in thyroid tissue, iodine I 124 emits positrons that can be detected by positron emission tomography (PET), allowing localization of thyroid tissue. This radiosiotope also emits gamma rays.
iodine I 124 18B10(10L)
A radioconjugate composed of an antibody directed against the tumor-associated antigen (TAA) Claudin18.2 (CLDN18.2; A2 isoform of claudin-18), and conjugated with the radioisotope iodine I 124, that can potentially be used as an imaging agent for positron emission tomography (PET)/computed tomography (CT). Upon administration, the antibody moiety of iodine I 124 18B10(10L) selectively targets and binds to CLDN18.2. The CLDN18.2-expressing tumor cells can then be visualized using PET/CT. CLDN18.2, a tight junction protein and stomach-specific isoform of claudin-18, is expressed on a variety of tumor cells. Its expression in healthy tissues is strictly confined to short-lived differentiated epithelial cells of the gastric mucosa.
iodine I 124 CPD-1028
A radioconjugate composed of the insulin-like growth factor 1 receptor (IGF-1R) binding agent CPD-1028 and conjugated to the radionuclide iodine I 124, with potential tumor imaging properties upon positron emission tomography/computed tomography (PET/CT). Upon administration, iodine I 124 CPD-1028 targets and binds to IGF-1R-expressing tumor cells. Upon PET/CT imaging, the iodine I 124 moiety can be visualized and the quantity of IGF-1R-expressing tumor cells can be assessed. IGF-1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a significant role in the stimulation of cellular proliferation, oncogenic transformation, and the suppression of apoptosis.
iodine I 124 FIAU
A radioconjugate containing the nucleoside analog 2'-fluoro-2'-deoxy-1beta-D-arabinofuranosyl-5-iodouracil (FIAU) labeled with the radioisotope iodine I 124 with positron-emitting activity. Chemotherapeutic agents such as bortezomib may induce viral thymidine kinase expression in EBV- and Kaposi's sarcoma herpesvirus (KSHV)-associated tumors. Subsequent to chemotherapy induction of viral TK in these tumors, administered iodine I 124 FIAU is phosphorylated by expressed viral TK, becoming selectively trapped within TK-expressing tumor cells; these cells can then be visualized with positron emission tomography (PET). Viral TK is either not expressed or is expressed at very low levels in EBV- and Kaposi's sarcoma herpesvirus (KSHV)-associated tumors and may be activated by certain chemotherapeutic agents.
iodine I 124 hJAA-F11
A radioimmunoconjugate composed of a humanized form of the mouse monoclonal antibody JAA-F11 (hJAA-F11) directed against the alpha-O-linked galactose disaccharide and tumor-associated antigen (TAA) Thomsen-Friedenreich (TF) antigen (TF-Ag) labeled with the radioisotope iodine I 124, with potential imaging activity upon positron-emission tomography (PET). Upon administration of iodine I 124 hJAA-F11, the antibody moiety specifically targets and binds to alpha-linked TF-Ag expressed on tumor cells, thereby allowing for the visualization of TF-Ag-expressing tumors upon PET. This may facilitate the assessment of the effectiveness of hJAA-F11. In tumor cells, TF-Ag appears as the disaccharide D-galactose-beta-(1-3)-N-acetyl galactosamine (Gal-beta-(1-3)-GalNAc) that is specifically alpha linked to a serine or a threonine residue on proteins. It is overexpressed on a variety of tumor cells and its expression is associated with tumor cell adhesion, tissue invasion and aggressiveness.
iodine I 124 iobenguane
A radioconjugate composed of the positron-emitting radioisotope iodine I 124 labeled to iobenguane, the synthetic aralkylguanidine analogue of the neurotransmitter norepinephrine (NE), with potential diagnostic imaging applications upon positron emitting tomography (PET) or computed tomography (CT). Upon administration, iodine I 124 iobenguane is taken up and accumulates in the granules of adrenal medullary chromaffin cells and in the pre-synaptic granules of adrenergic neurons in a manner almost identical with that of NE. In turn, tumor cells can be imaged upon PET or CT.
iodine I 124 iodo-azomycin galactopyranoside
A diagnostic radiopharmaceutical comprised of iodo-azomycin galactopyranoside (IAZGP) labeled with the positron-emitting radioisotope iodine I 124 and used as an imaging agent. Iodine I 124 iodo-azomycin galactopyranoside (I-124 IAZGP) is reduced under hypoxic conditions, covalently binding to macromolecules in hypoxic cells. After incorporation into hypoxic tumor cell DNA, I-124 IAZGP can be localized and quantified using positron emission tomography (PET), allowing a quantitative assessment of hypoxic tumor burden. IAZGP appears to have a higher water solubility and faster clearance from normal tissue than traditional imidazole tracers.
iodine I 124 iododeoxyuridine
A radiopharmaceutical comprised of the thymidine analog, 5-iodo-2-deoxyuridine (idoxuridine), labeled with the positron emitter iodine I 124. After incorporation into tumor cell DNA, positron emission tomography (PET) is used to image iodine I 124 localized to tumor cells for determining and monitoring tumor burden.
iodine I 124 monoclonal antibody 3F8
A radioimmunoconjugate consisting of 3F8, a murine anti-GD2 ganglioside monoclonal antibody labeled with iodine I 124 (I-124), with radioimaging activity using positron emission tomography (PET). Upon intravenous administration of iodine I 124 monoclonal antibody 3F8, the 3F8 moiety binds to GD2 expressed on tumor cells. This binding enables both PET imaging via iodine I 124 and the visualization of GD2-expressing tumor cells. GD2 is a ganglioside overexpressed in a variety of cancer cells, including neuroblastoma cells.
iodine I 124 monoclonal antibody A33
A radioimmunoconjugate of a humanized monoclonal antibody (MoAb) A33 labelled with iodine 124 (I-124). MoAb A33 recognizes A33 antigen, a 43 KDa transmembrane glycoprotein of the immunoglobulin superfamily, highly and homogenously expressed in 95% of colorectal cancer metastases, with only restricted expression in normal colonic mucosa. I-124 MoAb A33 delivers beta particle emitting I-124 nuclide directly to metastatic colorectal tissues, thereby this agent could be used in kinetics studies or radioimmunotherapy.
iodine I 124 monoclonal antibody M5A
A radioimmunoconjugate comprised of M5A, a humanized monoclonal antibody directed against carcinoembryonic antigen-related cell adhesion molecule 5 (CEA or CEACAM5), labeled with iodine I 124 (I-124) with potential radiolocalization applications. Upon administration, the antibody moiety of iodine I 124 monoclonal antibody M5A specifically binds to cells expressing CEA. Upon binding, the radioisotope moiety can be detected using positron-emission tomography (PET), thereby allowing the imaging and quantification of CEA-expressing tumor cells. CEA, a tumor associated antigen and a member of the CEA family of proteins, plays a key role in cell migration, cell invasion, and cell adhesion and is overexpressed by a variety of cancer types.
iodine I 124 NM404
A phospholipid ether analog labeled with iodine I 124, with a potential imaging property upon positron emission tomography (PET). Upon administration, iodine I 124 NM404 selectively accumulates in and is retained within tumor cells for a prolonged period of time due to the decreased activity of a phospholipase D (PLD), most likely isoform 1 of PLD, in tumor cells compared to normal cells. As tumor cells are unable to metabolize and eliminate MN404, tumor cells can be visualized upon PET imaging. In addition, iodine I 124 NM404 may provide a more accurate image of the tumor than imaging with the current standard. PLD is an enzyme found in the cell membrane of normal cells that degrades phospholipids.
iodine I 124 omburtamab
A radioimmunoconjugate consisting of the iodine I 124-radiolabeled murine IgG1 monoclonal antibody omburtamab directed against the cell surface glycoprotein CD276 (4Ig-B7-H3) with potential for radioimaging using positron emission tomography (PET). Through convection enhanced delivery of iodine I 124 omburtamab, the antibody moiety binds to the 4Ig domain of CD276, and in turn CD276-expressing tumor cells may be visualized upon PET imaging of the iodine I 124 moiety. CD276, a tumor-associated antigen (TAA) and member of the B7 family of co-stimulatory proteins, suppresses natural killer (NK) cell and cytotoxic T-lymphocyte activation; it is expressed on the cell membranes of a wide variety of tumors of neuroectodermal, mesenchymal and epithelial origin and its expression is associated with increased aggressiveness, poor prognosis and resistance.
iodine I 124 phospholipid ether analogue CLR1404
A small molecule radiopharmaceutical composed of the radioisotope iodine I 124 covalently attached to a proprietary alkylphospholipid ether (PLE) analogue, with potential imaging activity upon positron emission tomography (PET). Iodine I 124 phospholipid ether analogue CLR1404 is selectively taken up by tumor cells via membrane lipid rafts and accumulates in tumor cells. The accummulation of this agent is due to a decreased ability of tumor cells to metabolize PLEs because certain tumor cells have lower levels of the enzyme phospholipase-D, in comparison to normal cells. This facilitates imaging of cancer cells by PET. Lipid rafts, specialized microdomains of plasma membrane, are overexpressed in cancer cells compared to normal cells. In addition, the radioiodine moiety of this agent is resistant to de-iodination.
iodine I 124 PU-AD
A radioconjugate composed of PU-AD, a synthetic purine-scaffold inhibitor of the molecular chaperone heat shock protein 90 (Hsp90), conjugated to the radioisotope iodine I 124, with potential imaging activity upon positron emission tomography (PET). Upon administration of iodine I 124 PU-AD, the PU-AD moiety selectively binds to cancer cells expressing stress-induced Hsp90 (stress Hsp90). Upon PET, Hsp90-overexpressing cancer cells can be visualized and patients who may benefit from PU-AD therapy can be identified. This radioconjugate may also be used to determine the pharmacokinetics of the therapeutic agent PU-AD. PU-AD is able to cross the blood-brain-barrier (BBB) and specifically targets stress Hsp90, as seen in certain conditions, such as cancer and neurodegenerative diseases, while normal housekeeping Hsp90 complexes are not targeted by PU-AD at dose levels administered for imaging. Additionally, housekeeping Hsp90 complexes are only targeted at doses that are much larger than that are needed to exert an anticancer effect.
iodine I 124-cRGDY-PEG-C dots
An imaging agent composed of silica-based nanoparticles labeled with a near-infrared (NIR) fluorophore, Cyanine 5.5 (Cy5.5) and surrounded by polyethylene glycol (PEG) chains attached to cyclo-[Arg-Gly-Asp-Tyr] (cRGDY) peptides labeled with the positron-emitting radioisotope iodine I 124 via a tyrosine linker, with potential use in positron emission tomography (PET)/spiral computed tomography (CT) imaging. Upon intravenous administration of the radiolabeled iodine I 124-cRGDY-PEG-C dots, the cRGD moiety selectively binds to alphaVbeta3 integrin expressed on tumor cells. Upon PET/CT imaging, alphaVbeta3 integrin-expressing tumor cells can be visualized and the degree of both tumor metastasis and sentinel lymph node (SLN) trafficking can be assessed. Integrins are transmembrane glycoproteins upregulated on proliferating tumor vessel endothelial cells and various cancer cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells, metastasis and an overall poor prognosis.
iodine I 124-labeled anti-phosphatidylserine monoclonal antibody PGN650
A radioimmunoconjugate composed of the F(ab')2 fragment of human monoclonal antibody PGN650 against phosphatidylserine (PS) labeled with the radioisotope iodine I 124, with potential imaging activity upon positron-emission tomography (PET). Upon administration, the MoAb moiety of PGN650 binds to exposed PS on tumor cells, thereby allowing for the visualization of tumors upon PET. This may facilitate the assessment of the effectiveness of antitumor agents. The phospholipid PS is normally located on the inner leaflet of the plasma membrane of healthy cells but is flipped to the outer leaflet in the endothelial lining of the tumor vasculature and other tumor cells in response to chemo- or radio- treatments in addition to oxidative stress.
iodine I 124-labeled anti-PSCA A11 minibody
A radioconjugate composed of an affinity-matured antibody fragment, the A11 minibody, directed against human prostate stem cell antigen (PSCA), and conjugated with the radioisotope iodine I 124, that can potentially be used as an imaging agent for positron emission tomography (PET)/computed tomography (CT). The minibody moiety of iodine I 124-labeled anti-PSCA A11 minibody selectively targets and binds to PSCA. The PSCA-expressing tumor cells can then be visualized using PET/CT. PSCA, a cell surface antigen expressed in normal human prostate and bladder, is overexpressed in a variety of cancers, including bladder, pancreatic, and prostate cancer. The A11 minibody is formed by the fusion of a single chain Fv fragment with the immunoglobulin G1 CH3 domain.
iodine I 124-labeled HSP90 inhibitor PUH71
A radioconjugate containing the purine scaffold heat shock protein 90 (Hsp90) inhibitor PUH71 labeled with the radioisotope iodine I 124, with positron emitting activity. Hsp90 inhibitor PUH71 is thought to bind to cytosolic Hsp90 and the endoplasmic reticulum paralogue gp96 (HSP90B1), thereby inhibiting its molecular chaperone function and promoting the degradation of the oncogenic signaling proteins. This induces caspase-dependent apoptosis. The iodine I 124 moiety can be visualized using positron emission tomography (PET) imaging, thereby allowing an assessment of the accumulation of PUH71 in vivo, particularly in tumors. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.
iodine I 125
A radioactive isotope of iodine, a nonmetallic element of the halogen group. With a half-life of 60 days, iodine 125 occurs naturally and can be produced artificially. This agent has both therapeutic and diagnostic uses, particularly in thyroid disease.
iodine I 125 anti-EGFR-425 monoclonal antibody
A radioimmunoconjugate consisting of a murine IgG2a monoclonal antibody directed against the human epidermal growth factor receptor (EGFR) labeled with iodine I 125 with potential antineoplastic activity. Iodine I 125 anti-EGFR-425 monoclonal antibody binds specifically to the epidermal growth factor receptor (EGFR). Upon binding to EGFR-expressing tumor cells, this agent is internalized, selectively delivering a potentially cytotoxic dose of gamma radiation. EGFR is a receptor tyrosine kinase that may be overexpressed on the cell surfaces of various solid tumors.
iodine I 131 anti-fibronectin antibody fragment L19-SIP
An iodine 131 radioimmunoconjugate of a small immunoprotein (SIP), derived from the variable region fragment of human monoclonal antibody L19, that is directed against the extra-domain B (ED-B) of fibronectin, with potential radioimmunotherapeutic activity. The SIP moiety of iodine I 131 anti-fibronectin antibody fragment L19-SIP binds to the ED-B domain of fibronectin on tumor cells in the tumor neovasculature. Upon internalization, the I 131 radionuclide may selectively detect or deliver cytotoxic radiation to fibronectin-expressing tumor cells. ED-B of fibronectin, a naturally occurring marker of tissue remodeling and angiogenesis, is expressed in the majority of aggressive solid human tumors, whereas it is not detectable in normal vessels and tissues.
iodine I 131 apamistamab
A radioimmunoconjugate consisting of BC8, a murine IgG1 anti-CD45 monoclonal antibody labeled with iodine 131 (I-131), with radioimmunotherapeutic properties. Using monoclonal antibody BC8 as a carrier for I-131 results in the targeted destruction of cells expressing CD45. CD45 is tyrosine phosphatase expressed on virtually all leukocytes, including myeloid and lymphoid precursors in bone marrow and mature lymphocytes in lymph nodes; it is also expressed on most myeloid and lymphoid leukemic cells, but not on mature erythrocytes or platelets.
iodine I 131 chimeric monoclonal antibody G-250
A radioimmunoconjugate comprised of the chimeric monoclonal antibody G-250 conjugated with iodine I 131 with potential antineoplastic activity. The antibody moiety of iodine I 131 chimeric monoclonal antibody G-250 binds to G-250, a renal-cell carcinoma-associated antigen, delivering cytotoxic iodine I 131 specifically to renal cell carcinoma cells that express G-250.
iodine I 131 ethiodized oil
A cytotoxic radioconjugate consisting of ethiodized oil, an iodinated ethyl ester derived from poppy seed oil, labeled with iodine 131 (I-131). Iodine I 131 ethiodized oil accumulates in hepatocellular carcinoma and hepatoblastoma tumor cells, resulting in targeted cytotoxicity to tumor cells while sparing surrounding normal cells and tissues.
iodine I 131 iodocholesterol
A radioiodine-labeled cholesterol analogue with diagnostic imaging activity upon scintigraphy. Upon administration, iodine I 131 iodocholesterol accumulates in tissues where steroid hormones are produced, including the adrenal glands and, to a lesser extent, the ovaries and the testes. After binding to low-density lipoprotein (LDL) receptors on adrenocortical cells, this agent is internalized. As cholesterol is the precursor for all adrenocortical steroid hormones, areas of hormonal hypersecretion, can be visualized using scintigraphy and the adrenocortical function can be assessed.
iodine I 131 iopofosine
A radioconjugate composed of iopofosine, a phospholipid ether analog, labeled with the radioactive isotope iodine I 131, with potential antineoplastic activity. Upon administration, iodine I 131 iopofosine selectively accumulates in and retains within tumor cells for a prolonged period of time due to the decreased activity of a phospholipase D (PLD) in tumor cells compared to normal cells, thereby delivering cytotoxic radiation specifically to tumor cells. PLD is an enzyme found in the cell membrane of normal cells that degrades phospholipids.
iodine I 131 IPA
A radioconjugate consisting of the tumor-specific amino acid derivative 4-iodo-L-phenylalanine labeled with iodine I 131, a beta emitting radionuclide, with potential antineoplastic activity. Upon administration, iodine I 131 IPA actively crosses the blood-brain barrier and accumulates specifically in gliomas, via the amino acid transport system l-amino acid transporter 1 (LAT1) over-expressed in malignant glioma cells. where it delivers a cytotoxic dose of beta radiation. Cells that are exposed to radiation may also release potent toxins into the intracellular environment, leading to radiation-induced biological bystander effects (RIBBE) and killing cells not directly exposed to the radiation. Iodine I 131 IPA may also act synergistically with external irradiation due to its radiosensitizing property.
Iodine I 131 Lipiodol
(Other name for: iodine I 131 ethiodized oil)
iodine I 131 MIP-1095
A radioconjugate composed of MIP-1095, a urea-based ligand for the tumor-associated antigen (TAA) prostate-specific membrane antigen (PSMA), radiolabeled with iodine I 131 (I131), with potential antineoplastic activity. Upon administration of iodine I 131 MIP-1095, the MIP-1095 moiety selectively targets and binds to the extracellular domain of PSMA, thereby delivering cytotoxic iodine I 131 specifically to PSMA-expressing cancer cells. PSMA is a transmembrane glycoprotein that is highly expressed by malignant prostate epithelial cells and certain other tumor cells.
iodine I 131 monoclonal antibody 3F8
A radioimmunoconjugate consisting of 3F8, a murine anti-GD2 ganglioside monoclonal antibody labeled with iodine 131 (I-131), with radioimaging and radioimmunotherapeutic properties. Using monoclonal antibody 3F8 as a carrier for I-131 results in the targeted imaging and/or destruction of cells expressing GD2. GD2 is a ganglioside which is overexpressed in malignant melanoma, neuroblastoma, and small cell carcinoma of the lung.
iodine I 131 monoclonal antibody 81C6
A radioimmunoconjugate consisting of 81C6, a murine IgG2 anti-tenascin monoclonal antibody labeled with iodine 131 (I-131), with radioimaging and radioimmunotherapeutic activities. Using monoclonal antibody 81C6 as a carrier for I-131 results in the targeted imaging and/or destruction of cells expressing tenascin. Tenascin is an extracellular matrix protein which is overexpressed in gliomas and other cancers.
iodine I 131 monoclonal antibody CC49-deltaCH2
A radioimmunoconjugate consisting of the humanized CH2 domain-deleted monoclonal antibody CC49 and iodine I 131 with antineoplastic activity. Monoclonal antibody CC49-deltaCH2 targets the tumor-associated glycoprotein 72 (TAG-72) that is expressed by a wide range of human neoplasms including colorectal, gastric, pancreatic, ovarian, endometrial, breast, non-small cell lung, and prostate cancers. Iodine I 131 monoclonal antibody CC49-deltaCH2 binds to tumor cells expressing TAG-72, selectively delivering a cytotoxic dose of beta and gamma radiation.
iodine I 131 monoclonal antibody F16SIP
A fully human monoclonal antibody (MoAb) against human A1 domain of tenascin-C, in small immunoprotein (SIP) format conjugated with iodine 131 with potential antineoplastic activity. Iodine I 131 MoAb F16SIP binds to tenascin-C on the vascular tissues and delivers cytotoxic radiation to the tumors, thereby minimizing systemic radiotoxicity. Tenascin-C is a glycoprotein of the extracellular matrix, and the large isoform of this matrix protein is expressed and restricted around vascular structures in the tumor stroma of a variety of different tumors.
iodine I 131 monoclonal antibody muJ591
A radioimmunoconjugate of a mouse monoclonal antibody (MoAb) J591 labeled with Iodine 131 (I-131). MoAb muJ591 recognizes the extracellular domain of the prostate-specific membrane antigen (PSMA) and reacts with tumor vascular endothelium. Using MoAb muJ591 as a carrier for I-131 results in the targeted imaging and/or destruction of cells overexpressed PSM.
iodine I 131 monoclonal antibody TNT-1/B
An iodine 131 labeled radioimmunoconjugate of monoclonal antibody (MOAB) TNT-1/B with radioimaging and antineoplastic properties. MOAB TNT-1/B was developed for radioimmunotherapy of solid tumors, designated as Tumor Necrosis Treatment (TNT). TNT exploits the presence of degenerating and necrotic cells within tumors by utilizing MOAbs directed against universal, intracellular nucleosomal determinants consisting of histone H1 and DNA. This MOAB was conjugated with biotin (B) molecules, which increase pharmacokinetic performance of the monoclonal antibody. MOAB TNT-1/B delivers I 131 to tumor cells and results in the targeted imaging and/or destruction of cells with exposed necrotic antigens.
iodine I 131 NM404
A phospholipid ether analog labeled with iodine I 131, with potential radiotherapeutic and radioimaging potential upon positron emission tomography (PET). Upon administration, iodine I 131 NM404 selectively accumulates in and is retained within tumor cells for a prolonged period of time due to the decreased activity of a phospholipase D (PLD), most likely isoform 1 of PLD, in tumor cells compared to normal cells. As tumor cells are unable to metabolize and eliminate MN404, tumor cells can be visualized upon PET imaging. In addition, iodine I 131 NM404 selectively delivers a cytotoxic dose of iodine I 131 to the tumor cells. PLD is an enzyme found in the cell membrane of normal cells that degrades phospholipids.
iodine I 131 omburtamab
A radioimmunoconjugate consisting of the iodine 131-radiolabeled murine IgG1 monoclonal antibody 8H9 directed against the surface immunomodulatory glycoprotein 4Ig-B7-H3 with potential radioimaging and radioimmunotherapeutic uses. Iodine I 131 monoclonal antibody 8H9 binds to 4Ig-B7-H3 (human B7-H3 with 4 Ig-like domains) and may be used to radioimage and/or destroy tumor cells that express tenascin. 4Ig-B7-H3 inhibits T-cell activation and the production of effector cytokines such as interferon-gamma and interleukin-4; it is expressed on the cell membranes of a wide variety of tumors of neuroectodermal, mesenchymal and epithelial origin and is highly expressed on monocyte-derived dendritic cells (mdDCs). In vitro, it has been shown that monoclonal antibody-mediated masking of 4Ig-B7-H3 on neuroblastoma cells resulted in the enhancement of natural killer (NK)-mediated lysis of target cells.
iodine I 131 rituximab
A radioimmunoconjugate comprised of rituximab, a recombinant chimeric monoclonal antibody directed against the CD20 antigen, and labeled with iodine I 131 with potential antineoplastic activity. The antibody moiety of iodine I 131 rituximab binds to the CD20 antigen thereby delivering cytotoxic iodine I 131 specifically to cancer cells expressing CD20. The CD20 antigen, a hydrophobic transmembrane protein, is expressed on normal pre-B and mature B lymphocytes.
iodine I 131 SGMIB-anti-HER2 VHH1
A monoclonal antibody (MoAb) directed against the human epidermal growth factor receptor 2 (HER2; ERBB2) labeled with iodine I 131 using the residualizing radio-iodinating reagent N-succinimidyl 4-guanidinomethyl 3-iodobenzoate (SGMIB), with potential radiotherapeutic and radioimaging activities upon positron emission tomography (PET). Upon administration of iodine I 131 SGMIB-anti-HER2 VHH1, the HER2 MoAb moiety selectively targets and binds to HER2-expressing tumor cells. Upon PET imaging, tumor cells can be visualized. In addition, the iodine I 131 moiety of VHH1 selectively delivers a cytotoxic dose of iodine I 131 to the tumor cells. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. SGMIB improves tumor retention of radioactivity and decreases exocytosis.
iodine I 131 tenatumomab
A radioimmunoconjugate of tenatumomab, a murine monoclonal antibody targeting the tumor-associated antigen (TAA) tenascin-C (TNC), labeled with iodine I 131, with potential antineoplastic activity. The antibody moiety of iodine I 131 tenatumomab binds to TNC, thereby delivering a cytotoxic dose of iodine I 131 specifically to tumors expressing TNC. TNC, an extracellular matrix protein, is upregulated in a variety of tumor cell types; it plays a key role in invasion, tumor cell proliferation and immune evasion.
iodine I 131 TM-601
An iodine 131 (I 131) radioconjugate of the synthetic chlorotoxin (CTX) TM-601 with potential antiangiogenic and antineoplastic activities. CTX is a 36 amino acid neurotoxin found in the venom of the giant yellow scorpion Leiurus quinquestriatus that preferentially binds malignant cells of neuroectodermal origin. The recombinant version of this peptide, TM-601, is expressed in and purified from E. coli and then covalently linked to I 131 to produce 131I-TM-601. 131I-TM-601 binds to tumor cells of neuroectodermal origin and is internalized; administered once, it may be used as a radioimaging agent; repeated administration may result in a tumor-specific, cumulative radiocytotoxic dose of I 131. In addition, TM-601 alone, similar to native CTX, may inhibit angiogenesis due to its ability to bind to and inhibit matrix metalloproteinase 2 (MMP-2), an endopeptidase involved in tissue remodeling processes such as angiogenesis.
iodine I 131 tositumomab
A monoclonal antibody directed against the CD20 protein expressed on the surface of B-lymphocytes and radiolabeled with the radioisotope iodine I 131 with potential antineoplastic activity. Iodine I 131 tositumomab binds to and selectively delivers cyctotoxic radiation to CD20-expressing B-lymphocytes, thereby minimizing systemic radiotoxicity.
iodine I 131-labeled anti-CEA/anti-HSG bispecific monoclonal antibody TF2
A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten radiolabeled with iodine I 131 (I131) with antigen-binding and radioisotopic activities. Iodine I 131-labeled anti-CEA/anti-HSG bispecific monoclonal antibody TF2 binds to the tumor-associated antigen (TAA) CEA on CEA-expressing tumor cells; these cells may then be radioimaged scintigraphically.
iodine I-124 girentuximab
A radioimmunoconjugate comprised of the chimeric monoclonal antibody G250 conjugated with the positron emitter iodine I 124. The antibody moiety of iodine I 124 girentuximab may bind to renal cell carcinoma (RCC) cells that express the RCC-associated antigen G250, allowing detection of tumor-localized iodine I 124 with positron emission tomography (PET). G250 is a cell surface tumor-associated antigen (TAA) that is found in the majority of renal cell carcinomas.
iodine I-131
A radioactive isotope of iodine with an atomic mass of 131, a half life of eight days, and potential antineoplastic activity. Selectively accumulating in the thyroid gland, iodine I 131 emits beta and gamma particles, thereby killing thyroid cells and decreasing thyroid hormone production.
iodine-123 metaiodobenzylguanidine
The neurotransmitter analogue 3-nitrobenzylguanidine conjugated to iodine I 123 and used as a gamma-emitting imaging agent. The adrenergic tissue uptake and storage of I-123 metaiodobenzylguanidine (I-123 MIBG) mimics that of norepinephrine (NE). The distribution of this agent enables the scintigraphic imaging of neural crest tumors, such as neuroblastoma and pheochromocytoma.
iodixanol
A dimeric iso-osmolar, non-ionic, hydrophilic iodinated radiocontrast agent used in diagnostic imaging. Upon intravascular administration and during computed tomography (CT) imaging, iodixanol blocks x-rays and appears opaque on x-ray images. This allows body structures that absorb iodine to be visualized. The degree of opacity produced by iodixanol is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of iodixanol. Compared to other iodinated contrast agents, iodixanol appears to exhibit less nephrotoxicity.
Iodotope
(Other name for: iodine I-131)
ioflubenzamide I-131
An iodine 131-radiolabeled small-molecule benzamide compound with potential antineoplastic activity. The benzamide moiety of ioflubenzamide I-131 binds to melanin, selectively delivering a cyotoxic dose of gamma and beta radiation to melanin-expressing tumor cells. Melanin pigments, polymer derivatives of the amino acid tyrosine, are over-expressed in approximately 40% of melanomas.
iofolastat I123
An iodine 123-radiolabled small molecule that exhibits high affinity for prostate-specific membrane antigen (PSMA) with potential use in molecular imaging. Iofolastat I123, a radiolabeled glutamate-urea-lysine analogue, selectively binds PSMA, which allows imaging of PSMA-expressing prostate cancer cells with gamma scintigraph. PSMA is a transmembrane glycoprotein highly expressed by malignant prostate epithelial cells and vascular endothelial cells of various solid tumors.
iohexol
An X-ray contrast medium containing iohexol in various concentrations, from 140 to 350 milligrams of iodine per milliliter.
iolopride I-123
A radiopharmaceutical containing the dopamine D2/D3 receptor agonist iodobenzamide (IBZM) labeled with the radionuclide iodine I 123 with dopamine receptor-binding and radioisotopic activities. Upon administration, iodine I 123 iodobenzamide binds to dopamine D2/D3 receptors; subsequently, tissues expressing these receptors can be visualized using single photon emission computed tomography (SPECT). Dopamine receptors are a class of metabotropic G protein-coupled receptors found in the central nervous system (CNS) and neuroendocrine tumors such as pheochromocytoma and paraganglioma.
Iomab-B
(Other name for: iodine I 131 apamistamab)
ionic silver-impregnated sodium carboxymethyl cellulose antimicrobial dressing
A textile fiber dressing composed of ionic silver-impregnated sodium carboxymethylcellulose with potential wound-healing and antimicrobial activities. Ionic silver-impregnated sodium carboxymethylcellulose antimicrobial dressing inhibits microbial growth and promotes wound healing while protecting the wound site from external factors that may cause pain, promote infection, or slow the natural wound healing process. Ionic silver has a high affinity for negatively charged side groups on microbial cell proteins. Upon binding, ionic silver alters the molecular structure of proteins with a role in normal microbial cell functions thereby interfering with cell wall synthesis, transcription, translation, electron transport across membranes and protein folding, resulting in microbial cell death.
iopamidol
An organic iodine compound and used as a non-ionic water soluble radiographic contrast medium. Iopamidol blocks x-rays as they pass through the body, thereby allowing body structures not containing iodine to be visualized. The degree of opacity produced by iopamidol is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of iopamidol.
iopromide
A contrast medium.
ipafricept
A proprietary fusion protein comprised of the cysteine-rich domain of frizzled family receptor 8 (Fzd8) fused to the human immunoglobulin Fc domain with potential antineoplastic activity. Upon intravenous administration, ipafricept competes with the membrane-bound Fzd8 receptor for its ligand, Wnt proteins, thereby antagonizing Wnt signaling. This may result in the inhibition of Wnt-driven tumor growth. Fzd8, a member of the Frizzled family of G protein-coupled receptors, is one of the components in the Wnt/beta-catenin signaling pathway that plays key roles in embryogenesis and cancer growth.
ipamorelin
A pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) and a ghrelin mimetic with growth hormone (GH) releasing activity. Ipamorelin mimics ghrelin and binds to the ghrelin receptor (or GH secretagogue receptor, GHSR) in the brain, thereby selectively stimulating the release of GH from the pituitary gland. This results in increased plasma GH levels, which would affect many biological processes. Besides its presence in the brain, GHSR can also be found in the gastrointestinal tract, heart, lung, liver, kidney, pancreas, adipose tissue and immune cells. Unlike other GH releasing peptides, ipamorelin only stimulates GH release in a manner very similar to that of growth hormone releasing hormone.
iparomlimab/tuvonralimab
A mixture of the two engineered monoclonal antibodies iparomlimab, which is an immunoglobulin G4 (IgG4) monoclonal antibody directed against the human negative immunoregulatory checkpoint receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and tuvonralimab, which is an IgG1 monoclonal antibody directed against the cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration of iparomlimab/tuvonralimab, iparomlimab and tuvonralimab target and bind to PD-1 and CTLA4 expressed on tumor-infiltrating lymphocytes (TILs), respectively. This inhibits the PD-1- and CTLA4-mediated downregulation of T-cell activation and proliferation. This restores immune function and activates a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. Both PD-1 and CTLA4 are selectively expressed on TILs in the tumor microenvironment (TME) and negatively regulate the activation and effector functions of T cells. They play key roles in the downregulation of the immune system and tumor evasion from host immunity. Dual checkpoint blockade of PD-1 and CTLA4 enhances T-cell activation and proliferation more than the blockade of either immune checkpoint receptor alone.
ipatasertib
An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Ipatasertib binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.
ipilimumab
A recombinant human immunoglobulin (Ig) G1 monoclonal antibody directed against the human T-cell receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4), with immune checkpoint inhibitory and antineoplastic activities. Ipilimumab binds to CTLA4 expressed on T cells and inhibits the CTLA4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. CTLA4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system.
IPOL
(Other name for: inactivated poliovirus vaccine)
ipomeanol
A natural toxic furan isolated from a fungus-infected sweet potato (Ipomoea batatas) with potential antineoplastic activity. Ipomeanol is activated by mixed function oxidases in vivo to its epoxide form, an alkylating agent that covalently binds cell macromolecules. This agent causes cell death by a p53-independent mechanism.
iproplatin
A synthetic second-generation platinum-containing compound related to cisplatin. Iproplatin binds to and forms DNA crosslinks and platinum-DNA adducts, resulting in DNA replication failure and cell death. Although less prone to glutathione inactivation compared to cisplatin, resistance to this agent has been observed in vitro due to repair of platination damage by tumor cells.
iPSC-derived allogeneic anti-HER2 CAR T cells FT825
An off-the-shelf (OTS) preparation of induced pluripotent stem cell (iPSC)-derived, multiplexed-engineered alpha-beta T lymphocytes expressing a chimeric antigen receptor (CAR), using a specific H2CasMab-2 binder and Trac-mediated 1XX CAR, with a specific binding domain targeting the tumor-associated antigen (TAA) human epidermal growth factor receptor type 2 (HER2; EGFR2; ErbB2), with potential antineoplastic activity. FT825 contains seven synthetic controls in order to manipulate cellular function, including a CXC chemokine receptor 2 (CXCR2) to promote cell trafficking, a chimeric tumor growth factor-beta (TGFb) signal redirection receptor (TGFb-SRR) to redirect immunosuppressive signals, such as the immunosuppressive TGFb, in the tumor microenvironment (TME), a CD38 knock-out (CD38 null) to improve persistence, a synthetic interleukin (IL) 7/IL-7 receptor fusion protein (IL-7RF) to promote T-cell stemness, a T-cell receptor (TCR) removal to reduce the risk of graft-versus-host disease (GvHD), and a high-affinity non-cleavable CD16a receptor (hnCD16) to enable CD16-mediated antibody-dependent cellular cytotoxicity (ADCC) upon administration of a specific therapeutic antibody. Upon administration, allogeneic anti-HER2 CAR T cells FT825 target, bind to and induce selective toxicity in HER2-expressing tumors cells. This may result in the inhibition of tumor cell proliferation. HER-2 is overexpressed in various tumor cell types.
iPSC-derived anti-BCMA CAR/CD16/IL-15RF-expressing CD38-eliminated NK cells FT576
An allogeneic, off-the-shelf, natural killer (NK) cell product derived from a clonal master induced pluripotent stem cell (iPSC) line, and engineered and multiplex-edited to express a chimeric antigen receptor (CAR) specific for the tumor-associated antigen (TAA) B-cell maturation antigen (BCMA; tumor necrosis factor receptor superfamily member 17; TNFRSF17), a high-affinity, non-cleavable CD16 (hnCD16) Fc receptor and a recombinant fusion of IL-15 and IL-15 receptor alpha (IL-15RF), and to eliminate CD38 expression, with potential immunostimulatory and antineoplastic activities. Upon administration, iPSC-derived anti-BCMA CAR/CD16/IL-15RF-expressing CD38-eliminated NK cells FT576 recognize, bind to and induce selective cytotoxicity in BCMA-expressing tumor cells, leading to tumor cell lysis and the release of tumor neoantigens. Additionally, FT576 NK cells secrete inflammatory cytokines and chemokines, thereby enhancing T-cell activity and recruitment to the tumor site. BCMA, a receptor for both a proliferation-inducing ligand (APRIL) and B-cell activating factor (BAFF), is a member of the tumor necrosis factor receptor superfamily (TNFRSF). BCMA is found on the surfaces of plasma cells, is overexpressed on malignant plasma cells and plays a key role in plasma cell proliferation and survival. IL-15RF promotes the survival of NK cells and enhances the cytotoxic effect of the NK cells and the activated anti-tumor T cells. When used in combination with monoclonal antibodies, the hnCD16 Fc receptor of FT576 binds to the Fc portion of tumor cell-bound monoclonal antibodies, leading to NK cell activation, cytokine secretion and enhanced antibody-dependent cellular cytotoxicity (ADCC). CD16, also known as Fc-gamma receptor III, is normally expressed on the surface of NK cells, neutrophils, monocytes and macrophages, and plays a key role in initiating ADCC. It is often downregulated in certain cancers, thereby inhibiting the anti-tumor immune response. The lack of CD38 in FT576 NK cells prevents NK cell fratricide upon co-administration with a CD38-targeting monoclonal antibody as CD38 is normally expressed on the surface of activated NK cells. This enhances ADCC mediated by CD38-targeting monoclonal antibodies.
iPSC-derived anti-CD19 CAR/CD16/IL-15RF/ADR-expressing CD38-eliminated NK cells FT522
An allogeneic, off-the-shelf, natural killer (NK) cell product derived from a clonal master induced pluripotent stem cell (iPSC) line, and engineered and multiplex-edited to express a chimeric antigen receptor (CAR) specific for the tumor-associated antigen (TAA) CD19, a high-affinity, non-cleavable CD16 (hnCD16) Fc receptor, a recombinant fusion of IL-15 and IL-15 receptor alpha (IL-15RF), an alloimmune defense receptor (ADR) that targets the immune co-stimulatory receptor 4-1BB (CD137; tumor necrosis factor receptor superfamily member 9; TNFRSF9), and to eliminate CD38 expression, with potential immunostimulatory and antineoplastic activities. Upon administration, iPSC-derived anti-CD19 CAR/CD16/IL-15RF/ADR-expressing CD38-eliminated NK cells FT522 recognize, bind to and induce selective cytotoxicity in CD19-expressing tumor cells, leading to tumor cell lysis and the release of tumor neoantigens. Additionally, FT522 NK cells secrete inflammatory cytokines and chemokines, thereby enhancing T-cell activity and recruitment to the tumor site. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. IL-15RF promotes the survival of NK cells and enhances the cytotoxic effect of the NK cells and the activated anti-tumor T cells. The ADR targets 4-1BB-expressing alloreactive immune cells and leads to the killing of the alloreactive immune cells, further enhancing potency and extending the persistence of the FT522 NK cells. When used in combination with monoclonal antibodies, the hnCD16 Fc receptor of FT522 binds to the Fc portion of tumor cell-bound monoclonal antibodies, leading to NK cell activation, cytokine secretion and enhanced antibody-dependent cellular cytotoxicity (ADCC). CD16, also known as Fc-gamma receptor III, is normally expressed on the surface of NK cells, neutrophils, monocytes and macrophages, and plays a key role in initiating ADCC. It is often downregulated in certain cancers, thereby inhibiting the anti-tumor immune response. The lack of CD38 in FT522 NK cells prevents NK cell fratricide upon co-administration with a CD38-targeting monoclonal antibody as CD38 is normally expressed on the surface of activated NK cells. This enhances ADCC mediated by CD38-targeting monoclonal antibodies.
iPSC-derived CD16-expressing natural killer cells FT516
An allogeneic, off-the-shelf, natural killer (NK) cell product derived from a clonal master induced pluripotent stem cell (iPSC) line, and engineered to express a high-affinity, non-cleavable CD16 (hnCD16) Fc receptor, with potential antineoplastic and immunostimulatory activities. Upon administration, iPSC-derived CD16-expressing NK cells FT516 bind to the Fc portion of tumor cell-bound monoclonal antibodies and activate NK cell activation, cytokine secretion and antibody-dependent cellular cytotoxicity (ADCC). CD16, also known as Fc-gamma receptor III, is normally expressed on the surface of NK cells, neutrophils, monocytes and macrophages, and plays a key role in initiating ADCC. It is often downregulated in certain cancers, thereby inhibiting the anti-tumor immune response. FT516 NK cells' hnCD16 Fc receptor prevents downregulation and optimizes binding to tumor-targeting antibodies for enhanced ADCC.
iPSC-derived CD16/IL-15RF-expressing anti-CD19 CAR-NK cells FT596
An allogeneic, off-the-shelf, chimeric antigen receptor (CAR)-natural killer (NK) cell product derived from a clonal master induced pluripotent stem cell (iPSC) line, and engineered to express a NK cell-specific anti-CD19 CAR, a high-affinity, non-cleavable CD16 (hnCD16) Fc receptor, and a recombinant fusion of IL-15 and IL-15 receptor alpha (IL-15RF), with potential immunostimulatory and antineoplastic activities. Upon administration, iPSC-derived CD16/IL-15RF-expressing Anti-CD19 CAR-NK Cells FT596 recognize, bind to and induce selective cytotoxicity in CD19-expressing tumor cells. IL-15RF enhances the cytotoxic effect of the NK cells and the activated anti-tumor T-cells. When used in combination with monoclonal antibodies, the hnCD16 Fc receptor of FT596 binds to the Fc portion of tumor cell-bound monoclonal antibodies, leading to NK cell activation, cytokine secretion and enhanced antibody-dependent cellular cytotoxicity (ADCC). CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD16, also known as Fc-gamma receptor III, is normally expressed on the surface of NK cells, neutrophils, monocytes and macrophages, and plays a key role in initiating ADCC. It is often downregulated in certain cancers, thereby inhibiting the anti-tumor immune response.
iPSC-derived CD16/IL-15RF-expressing CD38-eliminated NK Cells FT538
An allogeneic, off-the-shelf, natural killer (NK) cell product derived from a clonal master induced pluripotent stem cell (iPSC) line, and engineered and CRISPR-edited to express a high-affinity, non-cleavable CD16 (hnCD16) Fc receptor and a recombinant fusion of IL-15 and IL-15 receptor alpha (IL-15RF), and to eliminate CD38 expression, with potential immunostimulatory and antineoplastic activities. Upon administration, iPSC-derived CD16/IL-15RF-expressing CD38-eliminated NK cells FT538 bind to stress-induced ligands on tumor cells, leading to tumor cell lysis and release of tumor neoantigens. Additionally, FT538 NK cells secrete inflammatory cytokines and chemokines, thereby enhancing T-cell activity and recruitment to the tumor site. IL-15RF promotes the survival of NK cells and enhances the cytotoxic effect of the NK cells and the activated anti-tumor T cells. When used in combination with monoclonal antibodies, the hnCD16 Fc receptor of FT538 binds to the Fc portion of tumor cell-bound monoclonal antibodies, leading to NK cell activation, cytokine secretion and enhanced antibody-dependent cellular cytotoxicity (ADCC). CD16, also known as Fc-gamma receptor III, is normally expressed on the surface of NK cells, neutrophils, monocytes and macrophages, and plays a key role in initiating ADCC. It is often downregulated in certain cancers, thereby inhibiting the anti-tumor immune response. The lack of CD38 in FT538 NK cells prevents NK cell fratricide upon co-administration with a CD38-targeting monoclonal antibody as CD38 is normally expressed on the surface of activated NK cells. This enhances ADCC mediated by CD38-targeting monoclonal antibodies.
iPSC-derived MSCs CYP-001
A preparation of allogeneic mesenchymal stem cells (MSCs) derived from induced pluripotent stem cells (iPSCs), with potential immunomodulating activity. iPSCs are derived from one healthy adult donor and are expanded and differentiated into mesenchymoangioblasts (MCAs), which are further expanded and cultured, upon which MSCs are formed and further expanded. Upon intravenous administration and following allogeneic hematopoietic stem cell transplantation (HSCT), the iPSC-derived MSCs CYP-001 may attenuate and prevent acute graft versus host disease (aGvHD).
iPSC-derived natural killer cells FT500
A preparation of off-the-shelf, natural killer (NK) cells derived from a clonal master induced pluripotent stem cell (iPSC) line, with potential antineoplastic and immunostimulatory activities. Upon administration, iPSC-derived natural killer cells FT500 bind to stress-induced ligands on tumor cells, leading to tumor cell lysis and release of tumor neoantigens. Additionally, iPSC-NK cells secrete inflammatory cytokines and chemokines including interferon-gamma (IFN-gamma), tumor necrosis factor-alpha (TNF-alpha), C-C motif chemokines 3, 4, and 22 (CCL3, CCL4, and CCL22), and C-X-C motif chemokine 10 (CXCL10), thereby enhancing T-cell activity and recruitment to the tumor site.
iptacopan
An orally available, small-molecule inhibitor of complement factor B (FB) with potential immunomodulatory activity. Upon administration, iptacopan binds to FB and prevents the formation of the alternative pathway (AP) C3-convertase (C3bBb). This limits the cleavage of C3 to the active fragment C3b and may prevent C3b-mediated extravascular hemolysis in certain complement-driven disorders such as paroxysmal nocturnal hemoglobinuria (PNH).
iratumumab
A fully human monoclonal antibody with potential antineoplastic activity. MDX-060 is a fully humanized antibody that targets CD30, a member of the tumor necrosis factor receptor superfamily found on activated lymphocytes. CD30 is over-expressed in various lymphoproliferative disorders, Hodgkin disease and other lymphomas, and other cancers.
IRDye800-labeled heterodimeric peptide KSP-QRH 919288G
A heterodimeric peptide consisting of the heptapeptide monomers KSPNPRF (KSP) and QRHKPRE (QRH) targeting human epithelial growth factor receptor type 2 (EGFR2; HER2; ErbB2) and epidermal growth factor receptor (EGFR), with an E3 spacer, labeled with the near-infrared (NIR) fluorophore IRDye800, with potential imaging activity using the scanning fiber endoscope (SFE) imaging system. Upon spraying of the esophagus with IRDye800-labeled heterodimeric peptide KSP-QRH 919288G, the heterodimeric peptide moiety targets and binds to HER2 and EGFR expressed on dysplastic cells in the pre-cancerous mucosa of the esophagus. Upon fluorescence imaging of the fluorophore IRDye800 with the SFE probe, the HER-2- and EGFR-expressing dysplastic cells can be detected. EGFR and HER2 are tyrosine kinase receptors that are overexpressed on the surfaces of various tumor cell types, and they are expressed in esophageal dysplasia.
IRDye800CW-labeled GPC3-targeted agent
A fluorescence imaging agent and an immunoconjugate comprised of a glypican 3 (GPC3)-targeting moiety conjugated to the near-infrared (NIR) fluorescent dye IRDye800CW, that can potentially be used for the imaging of GPC3-expressing tumor cells. Upon administration of the IRDye800CW-labeled GPC3-targeted agent, the GPC3-targeting moiety targets and binds to GPC3 expressed on tumor cells. Upon fluorescence imaging of the fluorophore IRDye800CW, the GPC3-expressing tumor cells can be visualized and detected. GPC3, a heparan sulfate proteoglycan and a member of the glypican family, is overexpressed on certain tumor cell types while minimally expressed on normal, healthy cells; GPC3 plays an important role in cellular proliferation and differentiation.
IRDye800CW-labeled heptapeptide KSP-910638G
An imaging agent composed of a heptapeptide targeting human epithelial growth factor receptor type 2 (EGFR2; HER2; ErbB2) conjugated, via a five-amino acid linker, to the near-infrared (NIR) fluorescent dye IRDye800CW, that can potentially be used for the imaging of HER2-expressing tumors. Upon oral administration of the IRDye800CW-labeled heptapeptide KSP-910638G, the peptide moiety targets and binds to HER2 expressed on tumor cells in the gastrointestinal (GI) tract. Upon fluorescence imaging of the fluorophore IRDye800CW, the tumor cells can be detected.
IRDye800CW-nimotuzumab
A fluorescence imaging and contrast agent and immunoconjugate comprised of nimotuzumab, a humanized monoclonal antibody directed against the epidermal growth factor receptor (EGFR), conjugated to the near-infrared (NIR) fluorescent dye IRDye 800CW, with potential imaging use. Upon administration of IRDye800CW-nimotuzumab, the nimotuzumab moiety targets and binds to the extracellular domain of EGFR. Upon binding, IRDye 800 may be detected using NIR imaging, which facilitates the visualization and detection of EGFR-expressing tumor cells. EGFR is a receptor tyrosine kinase that may be overexpressed on the cell surfaces of various tumor types.
IRE1 RNase inhibitor ORIN1001
An orally bioavailable inhibitor of the serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (inositol-requiring enzyme 1 alpha; IRE1), with potential immunoactivating, chemosensitizing and antineoplastic activities. Upon oral administration, IRE1 RNase inhibitor ORIN1001 targets and binds to the RNase domain of IRE1, thereby inhibiting the activity of IRE1. This prevents activation of the IRE1/X-Box Binding Protein 1 (XBP1) pathway, inhibits unfolded protein response (UPR) stress adaptation and prevents the production of pro-tumorigenic factors. This may inhibit tumor growth in which IRE1 is overactivated. In addition, ORIN1001 abrogates the immunosuppressive tumor microenvironment (TME) through cytotoxic T-cell infiltration and depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs) in the TME. IRE1, an endoplasmic reticulum (ER)-localized transmembrane protein containing an ER luminal stress-sensing domain and a cytoplasmic facing RNase domain, acts as a key sensor for the UPR and plays a key role in the response to and resolution of ER stress. IRE1 is involved in both protein phosphorylation and mRNA processing and degradation in response to ER stress-dependent signaling. IRE1 is frequently co-amplified with the MYC oncogene.
Iressa
(Other name for: gefitinib)
iriduim Ir 192
A radioactive isotope of iridium. Iridium-192 emits gamma rays and has a half-life of 74 days. A high dose rate of this radioisotope can be used in brachytherapy to treat tumors by selectively delivering a cytotoxic dose of radiation to the tumor site.
irinotecan hydrochloride
The hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.
irinotecan hydrochloride and floxuridine liposome LY01616
A liposomal formulation composed of a combination of two antineoplastic agents, the hydrochloride (HCl) salt form of irinotecan, a semisynthetic camptothecin analogue, and floxuridine, a fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP), with potential antineoplastic activity. Upon administration of irinotecan HCl/floxuridine liposome LY01616, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Floxuridine, as an antimetabolite, inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis. Liposome encapsulation of two antineoplastic agents at an optimal ratio can promote efficient drug delivery, improve efficacy and increase the synergistic effect.
irinotecan liposome HR070803
A liposomal formulation of the semisynthetic camptothecin analogue irinotecan, with potential antineoplastic activity. Upon administration of irinotecan liposome HR070803, irinotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell.
irinotecan sucrosofate
A liposomal dispersion formulated with the semisynthetic camptothecin analogue irinotecan, provided as the hydrochloride trihydrate form, which is encapsulated and entrapped within liposomes in a gelated or precipitated state as the irinotecan sucrose octasulfate (sucrosulfate) salt form, with potential antineoplastic activity. Upon administration of the liposomes containing irinotecan sucrosulfate, irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. During the S-phase, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Liposome encapsulation of this agent promotes efficient drug delivery into the cytosol from the endosome compartment of the cell, extends the circulation of irinotecan, and prolongs the duration of active therapy at the site of tumor to inhibit tumor growth.
irinotecan-eluting beads
Microporous hydrospheres of polyvinylalcohol (PVA) impregnated with irinotecan with potential antineoplastic activity. In transarterial chemoembolization (TACE), irinotecan-eluting beads are administered into blood vessels that feed the tumor, occluding tumor blood vessels and inducing ischemic tumor necrosis while simultaneously delivering high-dose chemotherapy locally. Irinotecan, a semisynthetic derivative of camptothecin, inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death.
irinotecan/P-glycoprotein inhibitor HM30181AK combination tablet
An orally bioavailable combination tablet containing the semisynthetic camptothecin derivative irinotecan and the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181AK, with potential antineoplastic activity. HM30181A binds to P-gp and prevents the P-gp-mediated efflux of irinotecan from tumor cells, which may result in greater intracellular concentrations of irinotecan and enhanced cytotoxicity. Retained intracellularly, the prodrug irinotecan is converted, by a carboxylesterase-converting enzyme, to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38). SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters and is overexpressed by some MDR tumors, preventing the intracellular accumulation of various cytotoxic agents.
irofulven
A semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. This agent requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. Irofulven is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and MDR1 than other alkylating agents.
iron
An element with atomic symbol Fe, atomic number 26, and atomic weight 55.85.
iron dextran complex
A colloidal solution containing ferric oxyhydroxide complexed with polymerized dextran, used as a form of parenteral iron-replacement therapy. Upon administration and absorption, the iron dextran complex is removed from plasma by the reticuloendothelial system which cleaves it into the components iron and dextran; ferric iron subsequently binds to transferrin or is stored as hemosiderin or ferritin. Transferrin-bound iron is transported in the plasma to the liver, spleen and bone marrow, where is it is incorporated into hemoglobin (Hgb) and to muscle where it is incorporated into myoglobin (Mb). Use of this agent circumvents the gastrointestinal adverse effects commonly encountered with the use of orally administered iron salt preparations. Because of cross-reactivity with antibodies targeted against polysaccharides similar to dextran, anaphylactic reactions may occur with this type of iron formulation.
iron isomaltoside 1000
An intravenous colloidal solution containing trivalent iron (Fe3+) chelated to isomaltosides, used as iron replacement. The iron in iron isomaltoside 1000 is strongly bound to the carbohydrate particles; each particle contains a trivalent iron core and a carbohydrate shell of isomaltosides which protects and stabilizes the iron core. This results in low levels of free iron and decreases inorganic, unbound iron-related toxicities thereby allowing for administration of higher doses of iron as compared to other iron-containing formulations. Upon parenteral administration and degradation of the carbohydrate shell, the iron in iron isomaltoside 1000 is released and replenishes iron stores.
iron sucrose injection
A sterile aqueous complex of polynuclear iron (III)-hydroxide in sucrose for intravenous use. Following intravenous administration, iron sucrose is dissociated by the reticuloendothelial system into iron and sucrose; the sucrose component is eliminated mainly by urinary excretion. Iron sucrose can be administered with or without erythropoietin to raise hemoglobin levels and may be used in cases of oral iron therapy intolerance or ineffectiveness. Hypersensitivity reactions are less common with iron sucrose compared to other parenteral iron products, such as iron dextran.
iron-conjugated polymers in saline suspension
A magnetic tracer composed of a suspension containing iron conjugated to polymers that can potentially be used as a contrast agent for detecting sentinel lymph node metastases using magnetic resonance imaging (MRI). Upon intravenous administration of the iron conjugated polymers in saline suspension, the iron conjugated polymers may collect in sentinel lymph nodes and lymph node metastases may be detected upon MRI.
irradiated allogeneic human lung cancer cells expressing OX40L-Ig vaccine HS-130
An allogeneic irradiated human lung cancer cell vaccine expressing a fusion protein composed of the OX40 ligand (OX40L) linked to an immunoglobulin (Ig) (OX40L-Ig), with potential immunomodulating and antineoplastic activities. Upon intradermal administration of irradiated allogeneic human lung cancer cells expressing OX40L-Ig vaccine HS-130, the irradiated lung cancer cells continuously express OX40L-Ig. OX40L may then target, bind to and activate its cognate receptor, tumor necrosis factor receptor superfamily member 4 (TNFRSF4; OX40; CD134), which is expressed on activated T cells. OX40L/OX40 binding promotes increased cytokine production, and induces the proliferation and activation of memory and effector T lymphocytes against the human lung cancer cells. In turn, this promotes a CTL-mediated immune response against the endogenous lung cancer cells. OX40L, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) ligand family, provides a co-stimulatory signal for the proliferation and survival of activated T cells.
IRS1/IRS2/STAT3 inhibitor NT219
An inhibitor of signal transducer and activator of transcription 3 (STAT3) and insulin receptor substrate 1 (IRS1) and 2 (IRS2), with potential antineoplastic activity. Upon administration, the IRS1/IRS2/STAT3 inhibitor NT219 specifically targets and binds to IRS1/2 and STAT3. Inhibiting IRS1/2 prevents IRS1/2-mediated signaling pathways and other tumor survival pathways. Inhibiting STAT3 prevents nuclear translocation of STAT3 and the STAT3-mediated regulation of oncogenes expression. This causes tumor cell apoptosis and inhibits tumor cell proliferation. IRS1/2 and STAT3, oncogenic drivers that are upregulated in a variety of human cancers, play key roles in uncontrolled tumor cell proliferation and tumor resistance.
iruplinalkib
An orally available, small molecule inhibitor of the receptor tyrosine kinase (RTK) anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon oral administration, iruplinalkib binds to and inhibits ALK tyrosine kinase, ALK fusion proteins, ALK point mutation variants ALK L1196M, ALK C1156Y, and EGFR L858R/T790M. Inhibition of ALK leads to the disruption of ALK-mediated signaling and the inhibition of cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK is not expressed in healthy adult human tissue but ALK dysregulation and gene rearrangements are associated with a series of tumors. Additionally, ALK mutations are associated with acquired resistance to small molecule tyrosine kinase inhibitors.
isatuximab-irfc
A humanized IgG1 monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. Isatuximab-irfc specifically binds to CD38 on CD38-positive tumor cells. This may trigger antitumoral antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC) and apoptosis eventually leading to cell lysis in CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies, and its expression has been correlated with poor prognosis.
isavuconazole
A water-soluble triazole prodrug with broad-spectrum antifungal activity. Administered intravenously or orally with high oral bioavailability, isavuconazole is hydrolyzed to the active moiety BAL4815 by plasma esterases. BAL4815 inhibits fungal cytochrome P450 lanosterol 14-alpha-demethylase (CYP51), which catalyzes the conversion of lanosterol to ergosterol, an important component of the fungal cell membrane. CYP51 inhibition by this agent leads to a decrease in ergosterol pool, thus disturbing synthesis of the fungal cell membrane; increasing fungal cell membrane permeability; promoting the loss of essential intracellular elements; and resulting in fungal cell lysis and death.
isavuconazonium sulfate
The sulfate ester form of isavuconazonium, a prodrug of the triazole antifungal agent isavuconazole, with broad-spectrum antifungal activity. Upon administration, isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of lanosterol to yield ergosterol, an important component of the fungal cell membrane. Inhibition of CYP51 leads to a decrease in fungal ergosterol production and disrupts synthesis of the fungal cell membrane, which decreases membrane integrity, increases cell membrane permeability and promotes the loss of essential intracellular elements. This results in fungal cell lysis and death.
Iscar
(Other name for: mistletoe extract)
Iscomatrix
(Other name for: saponin-cholesterol-phospholipid adjuvant)
Isentress
(Other name for: raltegravir potassium)
ISIS-STAT3rx
(Other name for: danvatirsen)
iso-fludelone
A third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells.
Isoflo
(Other name for: isoflurane)
isoflurane
A fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, inhaled isoflurane, appears to act on the lipid matrix of the neuronal cell membrane, which results in disruption of neuronal transmission. This agent enhances the release of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), thereby increasing the activity of the inhibitory neurotransmitter on synaptic transmission. Isoflurane may inhibit glutamatergic excitatory transmission by increasing glutamate re-uptake and it may potentiate glycine receptor activity, which decreases motor function. In addition, isoflurane may alter certain pro- and anti-inflammatory cytokines, including interleukin-6 and -10 (IL-6, IL-10), possibly through the activation of the nuclear factor kappa B (NF-KB) pathway, which may affect immune responses during surgery.
isoniazid
A synthetic derivative of nicotinic acid with anti-mycobacterial properties. Although its mechanism of action is still unclear, isoniazid appears to block the synthesis of mycolic acids, major components of the mycobacterial cell wall. This agent is only active against actively growing mycobacteria because, as a pro-drug, it requires activation in susceptible mycobacterial species. Isoniazid also interferes with mycobacterial metabolism of vitamin B6. Resistance occurs due to decreased bacterial wall penetration.
isopropyl alcohol
An isomer of propyl alcohol with antibacterial properties. Although the exact mechanism of isopropanol's disinfecting action is not known, it might kill cells by denaturing cell proteins and DNA, interfering with cellular metabolism, and dissolving cell lipo-protein membranes. Isopropanol is used in soaps and lotions as an antiseptic.
isoquercetin
An orally bioavailable, glucoside derivative of the flavonoid quercetin and protein disulfide isomerase (PDI) inhibitor, with antioxidant and potential antithrombotic activity. As an antioxidant, isoquercetin scavenges free radicals and inhibits oxidative damage to cells. As a PDI inhibitor, this agent blocks PDI-mediated platelet activation, and fibrin generation, which prevents thrombus formation after vascular injury. In addition, isoquercetin is an alpha-glucosidase inhibitor. PDI, an oxidoreductase secreted by activated endothelial cells and platelets, plays a key role in the initiation of the coagulation cascade. Cancer, in addition to other thrombotic disorders, increases the risk of thrombus formation.
isosulfan blue
A synthetic visual lymphatic imaging agent. Injected into the periphery of the tumor site, isosulfan blue localizes to the lymphatic system and aids in the surgical identification of tumor sentinel nodes which stain blue.
isotretinoin
A naturally-occurring retinoic acid with potential antineoplastic activity. Isotretinoin binds to and activates nuclear retinoic acid receptors (RARs); activated RARs serve as transcription factors that promote cell differentiation and apoptosis. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.
Isovue
(Other name for: iopamidol)
ispinesib
A synthetic small molecule, derived from quinazolinone, with antineoplastic properties. Ispinesib selectively inhibits the mitotic motor protein, kinesin spindle protein (KSP), resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest during the mitotic phase, and cell death in tumor cells that are actively dividing. Because KSP is not involved in nonmitotic processes, such as neuronal transport, ispinesib may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents.
ISS 1018 CpG oligodeoxynucleotide
A short, synthetic, unmethylated CpG motif-based oligodeoxynucleotide (CpG ODN) with immunostimulatory activity. As an immunostimulatory sequence (ISS) that signals through Toll-like receptor 9 (TLR9), ISS 1018 CpG ODN induces the production of immunoglobulin by B cells and interferon (IFN) -alpha, IFN-beta, interleukin (IL) -12, and tumor necrosis factor (TNF) -alpha by plasmacytoid dendritic cells (pDC). In turn, pDC, through cell-cell contact and secretion of and IFN-alpha and -beta induce natural killer (NK) cell proliferation, NK cell production of IFN-gamma, and NK cell-mediated cytotoxicity; secreted IFNs also stimulate bystander T cell activation and differentiation of naive CD4+ T cells into T-helper 1 cells on specific antigen challenge. In addition, ISS 1018 CpG ODN promotes antigen presentation and co-stimulatory molecule expression. Unmethylated CpG motifs are regions of genomic DNA containing the cytosine-guanine dinucleotide in which cytosine remains unmethylated, especially in prokaryotic DNA.
Istodax
(Other name for: romidepsin)
isunakinra
A recombinant protein resembling interleukin-1 (IL-1) receptor antagonist (IL-1Ra), with potential anti-inflammatory, immunomodulatory and antineoplastic activities. Upon administration, isunakinra targets and binds to the IL-1 receptor type 1 (IL-1-R1; IL-1R1; IL1R1), thereby blocking the binding of IL-1 alpha and beta to and activation of its receptor. Blockade of IL-1 activity and IL-1R1-mediated signaling inhibits the release of other pro-inflammatory mediators and may suppress inflammation and immunological responses. This may also abrogate the inflammatory and the immunosuppressive nature of the tumor microenvironment (TME), and may inhibit tumor growth, invasion, metastasis, and angiogenesis. IL-1/IL-1R1 signaling plays a key role in inflammation, which is present in various disease states including certain types of cancer.
isuventatug
A human immunoglobulin G1 (IgG1) monoclonal antibody directed against the natural-killer group 2, member D receptor protein (NKG2D or KLRK1) ligands MHC class I polypeptide-related sequence A (MICA) and B (MICB), with potential immunostimulating and antineoplastic activities. Upon administration, isuventatug targets and binds to the alpha3 domain of MICA and MICB, and prevents the cleavage of MICA and MICB from the cell surface of tumor cells by proteases in the tumor microenvironment (TME). This enhances the binding of NKG2D-expressing immune cells, including natural killer (NK) cells and subset of T cells, to MICA- and MICB-expressing tumor cells, which leads to the activation of NK cells and the lysis of tumor cells. CLN-619 also enhances antitumor response through antibody-dependent cell-mediated cytotoxicity (ADCC). MICA and MICB are stress-induced NKG2D ligands overexpressed on infected cells and many cancer cell types, but are not expressed on most normal, healthy cells. The shedding of MICA and MICB from tumor cell surface allows the tumor cells to evade NKG2D-expressing immune cells.
itacitinib adipate
The adipate salt form of itacitinib, an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic and immunomodulating activities. Upon oral administration, itacitinib selectively inhibits JAK-1, thereby inhibiting the phosphorylation of signal transducer and activator of transcription (STAT) proteins and the production of proinflammatory factors induced by other cytokines, including interleukin-23 (IL-23) and interleukin-6 (IL-6). The JAK-STAT pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.
itacnosertib
An orally bioavailable inhibitor of activin A receptor type 1 (activin receptor-like kinase 2; ALK2; ALK-2; ACRV1), with potential antineoplastic activity. Upon oral administration, itacnosertib targets, binds to and inhibits the activity of ALK-2. This prevents ALK-2-mediated signaling and inhibits cell growth in ALK-2-overexpressing tumor cells. In addition, in cancer and inflammatory conditions, ALK-2 is upregulated in response to increased signaling of pro-inflammatory cytokines, especially interleukin-6 (IL-6), and enhances the secretion of hepcidin, a peptide liver hormone and a key modulator of iron homeostasis. Blocking ALK-2-mediated pathways in inflammation and cancer leads to a decrease of hepcidin expression and restores plasma iron levels, thereby preventing low serum iron levels and anemia of chronic disease (ACD). ALK-2, a serine/threonine receptor kinase, is constitutively activated due to activating mutations or upregulated upstream signaling pathways in inflammatory conditions and certain types of cancer.
ITK inhibitor CPI-818
An orally available, small-molecule, irreversible inhibitor of interleukin-2 inducible T-cell kinase (ITK) with potential immunomodulatory and antineoplastic activities. Upon oral administration, ITK inhibitor CPI-818 selectively and covalently binds to the cysteine residue at position 442 (CYS-442) of ITK, thereby disrupting ITK-mediated signal transduction, while sparing tyrosine-protein kinase TXK (resting lymphocyte kinase, RLK) activity. This may abrogate T-cell receptor (TCR) signaling through ITK and inhibit TCR-induced proliferation of malignant T cells. Additionally, inhibiting ITK activation may prevent the upregulation of GATA-3, a transcription factor that drives T-helper 2 (Th2) cell differentiation and is overexpressed in certain T-cell lymphomas. Thus, selective inhibition of ITK may inhibit Th2 responses without affecting T-helper 1 (Th1)-dependent immunity. ITK, a member of the Tec family of non-receptor protein tyrosine kinases plays a significant role in the T-cell development, differentiation and production of pro-inflammatory cytokines.
Itovebi
(Other name for: inavolisib)
itraconazole
A synthetic triazole agent with antimycotic properties. Formulated for both topical and systemic use, itraconazole preferentially inhibits fungal cytochrome P450 enzymes, resulting in a decrease in fungal ergosterol synthesis. Because of its low toxicity profile, this agent can be used for long-term maintenance treatment of chronic fungal infections.
itraconazole dispersion in polymer matrix
A proprietary oral formulation composed of the poorly soluble, synthetic triazole agent, itraconazole, dispersed in a polymer matrix, with antifungal and potential anti-angiogenic activities. Upon oral administration, itraconazole inhibits the enzyme cytochrome P450 lanosterol 14 alpha-demethylase, resulting in a decrease in fungal ergosterol synthesis. Although the exact mechanism through which itraconazole inhibits angiogenesis has yet to be fully elucidated, this agent appears to inhibit the Hedgehog (Hh) signaling pathway, cholesterol synthesis and mammalian target of rapamycin (mTOR) signaling in endothelial cells. This agent may also prevent the activation of and signaling by various angiogenic growth factors. By decreasing the tumor vasculature and nutrient supply, itraconazole ultimately inhibits tumor cell growth. The solid dispersion of itraconazole in the polymer matrix enhances dissolution of itraconazole in the gastrointestinal tract and increases its bioavailability; this allows for the administration of a much lower dose compared to itraconazole alone.
ivabradine hydrochloride
The hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization. This decreases heart rate, reduces myocardial oxygen demand and allows more time for blood to flow to the myocardium without affecting cardiac contractility. HCN channels, mixed sodium (Na+) and potassium (K+) channels that carry the inward If current, play a key role in the regulation of pacemaker firing rate in the SA node. The If pacemaker current, the inward flow of positively charged Na+-K+ ions, initiates the spontaneous diastolic depolarization phase and modulating heart rate.
IVAC mutanome vaccine
An individualized, poly-neo-epitopic encoding, ribonucleic acid (RNA)-based cancer vaccine that targets a variety of patient-specific, immunogenic mutant epitopes, with potential immunostimulatory and antineoplastic activities. Upon intranodal administration, the RNA in the individualized mutanome vaccine is translated by antigen presenting cells (APCs) and the expressed protein is presented via major histocompatibility complex (MHC) molecules on the surface of the APCs. This leads to an induction of both cytotoxic T-lymphocyte (CTL) and memory T-cell immune responses against the patient-specific neoantigens.
ivaltinostat
A histone deacetylase (HDAC) inhibitor with potential antineoplastic activity. Ivaltinosta tinhibits the catalytic activity of HDAC, resulting in an accumulation of highly acetylated chromatin histones, followed by the induction of chromatin remodeling and an altered pattern of gene expression. In particular, this agent enhances the histone acetylation of the tumor suppressor gene p53. This results in an accumulation of p53, p53-dependent transactivation and apoptosis in tumor cells. HDAC, an enzyme upregulated in many tumor types, deacetylates chromatin histone proteins.
ivarmacitinib
An orally available inhibitor of Janus-associated kinase 1 (JAK1), with potential antineoplastic activity. Upon oral administration, ivarmacitinib binds to and inhibits JAK1, thereby preventing JAK-dependent signaling. This may lead to an inhibition of cellular proliferation in JAK1-overexpressing tumor cells. The JAK-STAT (signal transducer and activator of transcription) signaling pathway is a major mediator of cytokine activity and is often dysregulated in a variety of tumor cell types. Additionally, JAK1 may be a primary driver of STAT3 phosphorylation and signaling, which plays a role in neoplastic transformation, resistance to apoptosis, tumor angiogenesis, metastasis, immune evasion, and treatment resistance.
Iveegam EN
(Other name for: therapeutic immune globulin)
ivermectin
A macrocyclic lactone derived from Streptomyces avermitilis with antiparasitic activity. Ivermectin exerts its anthelmintic effect via activating glutamate-gated chloride channels expressed on nematode neurons and pharyngeal muscle cells. Distinct from the channel opening induced by endogenous glutamate transmitter, ivermectin-activated channels open very slowly but essentially irreversibly. As a result, neurons or muscle cells remain at either hyperpolarisation or depolarization state, thereby resulting in paralysis and death of the parasites. Ivermectin does not readily pass the mammal blood-brain barrier to the central nervous system where glutamate-gated chloride channels locate, hence the hosts are relatively resistant to the effects of this agent.
ivonescimab
A bispecific antibody directed against the negative immunoregulatory human cell receptor programmed cell death protein 1 (PD-1; PDCD1; CD279) and the human vascular endothelial growth factor (VEGF), with potential immune checkpoint inhibitory, anti-angiogenic and antineoplastic activities. Upon administration, ivonescimab simultaneously targets and binds to both PD-1 expressed on certain T cells and VEGF expressed on tumor cells. The binding of ivonescimab to PD-1 prevents the activation of PD-1 by its ligands, programmed cell death-1 ligand 1 (PD-L1; CD274) and/or 2 (PD-L2; CD273). This abrogates T-cell inhibition, activates antigen-specific T-lymphocytes and enhances cytotoxic T-lymphocyte (CTL)-mediated tumor cell lysis, which may lead to a reduction in tumor growth. The binding of ivonescimab to VEGF prevents binding of VEGF to its receptor VEGFR, abrogates VEGF/VEGFR-mediated signaling and may lead to the inhibition of vascular endothelial cell proliferation. The inhibition of tumor angiogenesis may further decrease tumor cell proliferation and prevent metastasis. PD-1, a transmembrane protein in the immunoglobulin superfamily (IgSF) expressed on T cells, functions as an immune checkpoint that negatively regulates T-cell activation and effector function when activated by its ligands PD-L1 and/or PD-L2; it plays an important role in tumor evasion from host immunity. VEGF is overexpressed in a variety of cancers and is associated with increased invasiveness and decreased survival.
ivosidenib
An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Upon administration, ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells. IDH1, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG.
ivuxolimab
An agonistic antibody that recognizes the co-stimulatory receptor OX40 (CD134; TNFRSF4), with potential immunostimulatory activity. Upon administration, ivuxolimab selectively binds to and activates OX40; which induces proliferation of memory and effector T lymphocytes. In the presence of tumor-associated antigens (TAAs), this may promote a T-cell-mediated immune response against TAA-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on T lymphocytes and plays an essential role in T-cell activation.
Iwilfin
(Other name for: eflornithine hydrochloride)
ixabepilone
An orally bioavailable semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines.
ixabepilone (oral)
An enteric-coated formulation of ixabepilone, a semisynthetic analogue of epothilone B and a non-taxane tubulin inhibitor, with antineoplastic activity. Ixabepilone binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in cell cycle arrest at the G2-M phase and leads to apoptosis within fast growing tumor cells. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. Compared to intravenously administered ixabepilone, the oral formulation provides a more manageable way to administer this agent.
ixazomib citrate
The citrate salt form of ixazomib, an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. Ixazomib inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome, which results in an accumulation of unwanted or misfolded proteins; disruption of various cell signaling pathways may follow, resulting in the induction of apoptosis. Compared to first generation PIs, second generation PIs may have an improved pharmacokinetic profile with increased potency and less toxicity. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquinated.
Ixempra
(Other name for: ixabepilone)
ixotatug vedotin
An antibody-drug conjugate (ADC) composed of ixotatug, a humanized monoclonal antibody directed against the tumor-associated antigen (TAA) claudin 6 (CLDN6; CLDN-6), linked to the auristatin derivative monomethyl auristatin E (MMAE) via a cleavable linker, with potential antineoplastic activity. Upon administration of ixotatug vedotin, the anti-CLDN6 antibody moiety targets and binds to CLDN6-expressing tumor cells. Upon binding, internalization, and linker cleavage, MMAE is released. MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. This induces cell death in CLDN6-expressing cancer cells. CLDN6, a transmembrane tight-junction protein and embryonic antigen, is overexpressed on a variety of tumor cells but is not expressed on normal, healthy adult cells.
Ixoten
(Other name for: trofosfamide)
izalontamab
An immunoglobulin G (IgG) bispecific antibody targeting both the epidermal growth factor receptor (EGFR; HER1; ErbB1) and the epidermal growth factor receptor 3 (HER3; ErbB3), with potential antineoplastic activity. Upon administration, izalontamab simultaneously targets and binds to EGFR and HER3 expressed on cancer cells, thereby preventing receptor phosphorylation. This prevents the activation of both EGFR- and HER3-mediated signaling pathways and results in the inhibition of tumor cell proliferation. EGFR and HER3, both upregulated and/or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation.
izalontamab brengitecan
A dual-targeted antibody-drug conjugate (ADC) consisting of a bispecific antibody directed against both the epidermal growth factor receptor (EGFR; HER1; ErbB1) and the epidermal growth factor receptor 3 (HER3; ErbB3) conjugated, via a cathepsin-B cleavable linker, to the camptothecin derivative and topoisomerase 1 inhibitor Ed-04, with potential antineoplastic activity. Upon administration of izalontamab brengitecan, the bispecific antibody moiety simultaneously targets and binds to EGFR and HER3 expressed on cancer cells. Upon binding and internalization, Ed-04 is released and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing EGFR and/or HER3. EGFR and HER3, both upregulated and/or mutated in a variety of tumor cell types, play key roles in tumor cell proliferation. Simultaneously targeting both EGFR and HER3 may enhance the anti-tumor activity of izalontamab brengitecan.
izorlisib
An orally bioavailable inhibitor of the class I phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha (PIK3CA), with potential antineoplastic activity. Upon administration, izorlisib selectively binds to and inhibits PIK3CA and its mutated forms in the PI3K/Akt (protein kinase B)/mammalian target of rapamycin (mTOR) pathway. This results in both apoptosis and growth inhibition in PIK3CA-expressing tumor cells. By specifically targeting PIK3CA, izorlisib may be more efficacious and less toxic than pan-PI3K inhibitors. In addition, izorlisib also targets mutated forms of PI3K gamma (PI3Kg). It may also stimulate the immune system to restore CD8+ T-cell activation and cytotoxicity. 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. In most solid tumors, the activation of the PI3K pathway is induced by mutations of PIK3CA.
izuralimab
A humanized, Fc-engineered bispecific monoclonal antibody directed against both the human negative immunoregulatory checkpoint receptor, programmed cell death protein 1 (PD-1; PCD-1; CD279), and inducible T-cell co-stimulator (ICOS; CD278), with potential immunomodulating and antineoplastic activities. Upon administration, izuralimab targets and binds to both PD-1 and ICOS expressed on certain T cells, including tumor-infiltrating lymphocytes (TILs). This prevents the activation of PD-1 by its ligands, programmed cell death-1 ligand 1 (PD-L1) and PD-1 ligand 2 (PD-L2), and stimulates ICOS-mediated signaling, which promotes the activation of T cells and enhances T-cell-mediated immune responses against tumor cells. Combined PD-1 blockade and ICOS stimulation may enhance T-cell activation and proliferation more than targeting each receptor individually. The engineered Fc domain increases the stability and half-life of the antibody.