NCI Drug Dictionary

398 results found for: F

F 18 fluorodeoxygalactose: A radioconjugate containing the D-galactose analogue 2-deoxy-2-fluoro-D-glucose (FDGal) labeled with the positron-emitting radioactive isotope fluorine F18, used for imaging upon positron emitting tomography (PET). With cell uptake much higher in tumor cells compared to normal cells, the F18 moiety of fluorodeoxygalactose F-18 can be visualized upon PET imaging and this agent can be used as a tracer for the evaluation of galactose tumor uptake and metabolism.
F-18 16 alpha-fluoroestradiol: A radiopharmaceutical consisting of an estradiol analogue radiolabeled with the positron-emitting isotope fluorine F 18. F-18 16 alpha-fluoroestradiol is actively taken up in tumor cells expressing the estrogen receptor (ER), allowing visualization of ER-positive tumor cells with positron emiision tomography (PET). Uptake of this agent depends upon the ER status of target tissues.
F-18 fluoroethyltyrosine: An amino acid analog radiolabeled with fluorine F 18, a positron emitting isotope, used as a tracer in positron emission tomography (PET). Reflecting the increased amino acid transport capacity of tumor cells, F-18 fluroethyltyrosine (F-18 FET) is actively taken up in tumor cells via amino acid transport system L, but is neither incorporated into proteins nor readily degraded, resulting in high intracellular concentrations of this imaging agent. Radiolableled amino acid-based agents are useful in PET brain tumor imaging because F-18 fluoro-deoxyglucose (F-18 FDG), commonly used in PET tumor imaging, is relatively insensitive for detecting tumors in the brain due the high levels of glycolytic metabolism in the normal cortex and to a lesser extent in white matter.
F16-IL2 fusion protein: An immunocytokine of the human monoclonal antibody fragment F16 (scFv) against the extra-domain A1 of tenascin-C fused, via a short 5-amino acid linker, to a recombinant form of the human cytokine interleukin-2 (IL-2) with potential immunostimulating and antineoplastic activities. The monoclonal antibody portion of the F16-IL2 fusion protein binds to tumor cells expressing the tumor associated antigen (TAA) tenascin-C. In turn, the IL-2 moiety of the fusion protein stimulates natural killer (NK) cells, macrophages and neutrophils and induces T-cell antitumor cellular immune responses thereby selectively killing tenascin-C-expressing tumor cells. In addition, F16-IL2 may potentiate the cytotoxicity of other chemotherapeutic agents. Tenascin-C, a glycoprotein of the extracellular matrix, is expressed in many cancer cell types.
FACT complex-targeting curaxin CBL0137: An orally available curaxin-based agent targeting the Facilitates Chromatin Transcription (FACT) complex, with potential antineoplastic activity. Upon administration, CBL0137 binds to FACT and sequesters the FACT complex on chromatin, which inhibits its activity. This prevents transcription of certain genes involved in cancer-associated signaling pathways; it specifically inhibits the transcription of both NF-kappa B and heat shock transcription factor 1 (HSF1) and simultaneously activates p53. This causes an increase in tumor cell apoptosis and a decrease in tumor cell proliferation, in FACT-positive cancers. In addition, this agent is able to sensitize FACT-positive tumor cells to the cytotoxic effects of other chemotherapeutic agents. FACT, a transcription and replication factor composed of the Structure Specific Recognition Protein (SSRP1) and suppressor of Ty 16 (Spt16) proteins, is expressed in a variety of tumor cells while almost absent in normal cells; its expression is associated with increased tumor aggressiveness and poor prognosis.
factor VII-targeting immunoconjugate protein ICON-1: A human immunoconjugate (ICON) fusion protein composed of a modified version of human factor VII (FVII) which targets tissue factor (TF) that is fused to the Fc domain of the human immunoglobulin G1, with potential antithrombotic and antineoplastic activities. Acting in a similar manner as plasma FVII, the natural ligand of TF, ICON-1 targets and binds to TF expressed on neovascular endothelia, thereby preventing TF-mediated signaling pathways, and leading to the initiation of an immune response and the destruction of neovascular tissue. This prevents angiogenesis, inflammation and blood coagulation. Upon intravitreal administration, ICON-1 may block TF-induced angiogenesis and treat wet age-related macular degeneration (AMD) and ocular melanoma. TF, a naturally occurring glycoprotein in humans, regulates blood clotting, angiogenesis, and inflammation.
factor VIIa inhibitor PCI-27483: A reversible small-molecule inhibitor of activated factor VII (factor VIIa) with potential antineoplastic and antithrombotic activities. FVII, a serine protease, becomes activated (FVIIa) upon binding with TF forming the FVIIa/TF complex, which induces intracellular signaling pathways by activating protease activated receptor 2 (PAR-2). Upon subcutaneous administration, factor VIIa inhibitor PCI-27483 selectively inhibits factor FVIIa in the VIIa/TF complex, which may prevent PAR-2 activation and PAR2-mediated signal transduction pathways, thereby inhibiting tumor cell proliferation, angiogenesis, and metastasis of TF-overexpressing tumor cells. In addition, this agent inhibits both the extrinsic and intrinsic coagulation cascades, preventing blood clot formation. TF, a blood protein overexpressed on the cell surface of a variety of tumor cell types, may correlate with poor prognosis; PAR-2 (also known as thrombin receptor-like 1) is a G protein-coupled receptor (GPCR) and a protease-activated receptor.
fadraciclib: An orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9), with potential antineoplastic and chemoprotective activities. Upon oral administration, fadraciclib selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow. CDKs are serine/threonine kinases involved in the regulation of the cell cycle and may be overexpressed in certain cancer cell types; they play key roles in tumor cell proliferation, the regulation of transcription, and DNA damage repair.
fadrozole hydrochloride: The hydrochloride salt of the nonsteroidal aromatase inhibitor fadrozole with potential antineoplastic activity. Fadrozole specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively, the final step in estrogen biosynthesis; the reduction in estrogen levels may inhibit growth in estrogen-dependent cancers. Aromatase, a member of the cytochrome P-450 superfamily, is found in many tissues; overexpression has been linked to the development of preneoplastic and neoplastic changes in breast tissue.
FAK inhibitor GSK2256098: A focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor GSK2256098 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thereby inhibiting tumor cell migration, proliferation and survival, and tumor angiogenesis. The tyrosine kinase FAK is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types.
FAK inhibitor PF-00562271: An orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. FAK inhibitor PF-00562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by this agent may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.
FAK inhibitor VS-4718: An orally bioavailable focal adhesion kinase (FAK) inhibitor with potential antineoplastic activity. Upon administration, VS-4718 inhibits FAK, blocks fibronectin-stimulated FAK autophosphorylation of Tyr397, and may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt. This results in the reduction of the number of cancer stem cells (CSCs) and inhibits tumor cell migration, proliferation and survival. The cytoplasmic tyrosine kinase FAK is a signal transducer for integrins and is constitutively activated in various tumor cell types; it is involved in tumor cell invasion, migration and proliferation and plays a key role in the development, function and survival of CSCs.
FAK/ALK/ROS1 inhibitor APG-2449: An orally available kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK), focal adhesion kinase (FAK) and the receptor tyrosine kinase C-ros oncogene 1 (ROS1), with potential antineoplastic activity. Upon administration, ALK/FAK/ROS1 inhibitor APG-2449 selectively binds to and inhibits ALK, FAK and ROS1 kinases. The inhibition leads to disruption of ALK-, FAK- and ROS1-mediated signal transduction pathways and eventually inhibits tumor cell growth in ALK-, FAK- and ROS1-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; its dysregulation and gene rearrangements are associated with a variety of tumors. The cytoplasmic tyrosine kinase FAK, a signal transducer for integrins, is upregulated and constitutively activated in various tumor types; it plays a key role in tumor cell migration, proliferation, survival, and tumor angiogenesis. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells.
falbikitug: A humanized immunoglobulin G1 (IgG1) monoclonal antibody against leukemia inhibitory factor (LIF), with potential immunomodulating and antineoplastic activities. Upon intravenous administration, falbikitug binds to LIF and inhibits LIF signaling by blocking the recruitment of glycoprotein 130 (gp130) to the LIF-LIF receptor (LIFR)-gp130 signaling complex. This inhibits signal transducer and activator of transcription 3 (STAT3) signaling and inhibits tumor cell growth. In addition, the inhibition of LIF signaling abrogates the immunosuppressive tumor microenvironment (TME) by decreasing immunosuppressive M2 macrophages and allows for the activation of natural killer (NK) cells and cytotoxic T lymphocytes (CTLs) against tumor cells. LIF, a member of the interleukin-6 (IL-6) family of cytokines, is involved in many physiological and pathological processes and plays an important role in both creating the TME and promoting the activity of cancer-initiating cells (CICs). LIF is overexpressed in many tumor cell types and its expression correlates with poor prognosis.
falimarev: A cancer vaccine comprised of a recombinant fowlpox viral vector encoding the carcinoembryonic antigen (CEA), MUC-1, a transmembrane glycoprotein secreted by glandular epithelial tissues, and TRICOM, comprised of three co-stimulatory molecule transgenes (B7-1, ICAM-1 and LFA-3). This agent may enhance CEA and MUC-1 presentation to antigen-presenting cells (APC) and may activate a cytotoxic T-cell response against CEA- and MUC-1-expressing tumor cells.
falnidamol: A pyrimido-pyrimidine with antitumor activity. BIBX 1382 inhibits the intracellular tyrosine kinase domain of the Epidermal Growth Factor Receptor (EGFR) thus specifically reversing the aberrant enzymatic activity from overexpressed and constitutively activated EGFR, and subsequently inhibiting cell proliferation and inducing cell differentiation.
fam-trastuzumab deruxtecan-nxki: An antibody-drug conjugate (ADC) composed of trastuzumab, a monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2; EGFR2; HER2) conjugated to deruxtecan, a derivative of the camptothecin analog exatecan (DXd; DX-8951 derivative), a DNA topoisomerase 1 (topoisomerase I; Top1) inhibitor, with antineoplastic activity. Upon administration of fam-trastuzumab deruxtecan-nxki, trastuzumab targets and binds to HER2 on tumor cells. Upon antibody/antigen binding and internalization, deruxtecan binds to and inhibits Top1-DNA complexes, which results in an inhibition of DNA replication, cell cycle arrest and tumor cell apoptosis. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. In addition, trastuzumab deruxtecan induces antibody-dependent cell-mediated cytotoxicity (ADCC) and causes a bystander killing effect.
famitinib: An orally bioavailable receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Famitinib binds to and inhibits several RTKs, dysregulated in a variety of tumors, including stem cell factor receptor (c-Kit; SCFR), vascular endothelial growth factor receptor (VEGFR) 2 and 3, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinases Flt1 and Flt3. Inhibition of these RTKs may result in an inhibition of tumor growth and angiogenesis, and eventually tumor regression in tumor cells overexpressing these RTKs.
famotidine: A propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli.
FAP-specific CD8-positive T cells: A preparation of CD8-positive T cells specific for human fibroblast activating protein (FAP) with potential immunopotentiating activity. T cells have been genetically modified to express a chimeric antigen receptor specific for FAP. Upon infusion, the FAP-specific CD8-positive T cells bind to FAP-expressing tumor cells and exhibit a selective toxicity to tumor cells. This may result in both tumor cell lysis and inhibition of tumor cell growth. FAP, a cell surface glycoprotein, is overexpressed on tumor-associated fibroblasts but minimally expressed on normal, healthy cells.
FAP/4-1BB-targeting DARPin MP0310: A designed ankyrin repeat proteins (DARPin)-based agent targeting the tumor-associated protein fibroblast activation protein (FAP) and the T-cell co-stimulatory immune receptor 4-1BB (CD137; tumor necrosis factor receptor superfamily member 9; TNFRSF9), with potential immunomodulating and antineoplastic activities. Upon administration, the FAP/4-1BB-targeting DARPin MP0310 targets and binds to both FAP, localized on tumor stromal cells, and 4-1BB, expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer (NK) cells. The simultaneous binding of FAP and 4-1BB results in local clustering of FAP-expressing tumor stromal cells and 4-1BB-expressing T cells, and local immune cell activation through the promotion of T-cell activation, cytokine release and T-cell-mediated anti-tumor immune responses. 4-1BB, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. FAP is abundantly expressed by cancer associated fibroblasts in the majority of solid tumors. Compared to antibodies, DARPins are small in size, have favorable pharmacokinetics and allow for both high affinity binding and efficacy.
FAP/4-1BB-targeting fusion protein RO7122290: A bispecific antibody-like fusion protein consisting of a trimeric ligand for the T-cell co-stimulatory immune receptor 4-1BB (CD137; tumor necrosis factor receptor superfamily member 9; TNFRSF9) and an antigen-binding fragment (Fab) moiety targeting the tumor-associated protein fibroblast activation protein (FAP), with potential immunomodulating and antineoplastic activities. Upon administration, the FAP/4-1BB-targeting fusion protein RO7122290 targets and binds to both FAP, localized on tumor stromal cells, and 4-1BB, expressed on a variety of leukocyte subsets including activated T lymphocytes and natural killer (NK) cells. The simultaneous binding of FAP and 4-1BB results in local clustering of FAP-expressing tumor stromal cells and 4-1BB-expressing T cells, and local immune cell activation through the promotion of T-cell activation, cytokine release and T-cell-mediated anti-tumor immune responses. 4-1BB, a surface glycoprotein of the tumor necrosis factor receptor superfamily, is an inducible costimulatory receptor that plays a key role in T-cell proliferation, survival and cytolytic activity. FAP is abundantly expressed by cancer-associated fibroblasts in the majority of solid tumors.
FAP/CD40-targeting agent SHR-7367: An agent targeting both the tumor-associated antigen (TAA) fibroblast activation protein (FAP) and CD40, with potential immunostimulatory and antineoplastic activities. Upon administration, FAP/CD40-targeting agent SHR-7367 targets and binds to both FAP, localized predominantly on cancer-associated fibroblasts (CAFs) in the tumor stroma, and CD40, a cell surface stimulatory receptor expressed on various immune cells including B lymphocytes, monocytes and dendritic cells (DCs). The simultaneous binding to FAP and CD40 results in local clustering of FAP-expressing tumor stromal cells and CD40-expressing immune cells. Activation of CD40 induces proliferation and activation of B lymphocytes, shifts the induction of suppressive macrophages towards immunostimulatory macrophages, activates monocyte-derived DCs (moDCs), and leads to the secretion of inflammatory cytokines, which activates the immune system to induce the proliferation and activation of cytotoxic T lymphocytes (CTLs) against tumor cells. CD40, a member of the tumor necrosis factor receptor superfamily (TNFRSF), plays a key role in the activation of the immune system. FAP is abundantly expressed by CAFs in many solid tumors.
FAP/CD40-targeting DARPin MP0317: A tri-specific, designed ankyrin repeat proteins (DARPin)-based agent targeting the tumor-associated protein fibroblast activation protein (FAP), CD40 receptor and human serum albumin (HSA), with potential immunostimulatory and antineoplastic activities. Upon administration, FAP/CD40-targeting DARPin MP0317 targets and binds to both FAP, localized predominantly on cancer-associated fibroblasts (CAFs) in the tumor stroma, and CD40, a cell surface stimulatory receptor expressed on various immune cells including B lymphocytes, monocytes and dendritic cells (DCs). The simultaneous binding to FAP and CD40 results in local clustering of FAP-expressing tumor stromal cells and CD40-expressing immune cells. Activation of CD40 induces proliferation and activation of B lymphocytes, shifts the induction of suppressive macrophages towards immunostimulatory macrophages, activates monocyte-derived DCs (moDCs), and leads to the secretion of inflammatory cytokines, which activates the immune system to induce the proliferation and activation of cytotoxic T lymphocytes (CTLs) against tumor cells. CD40, a member of the tumor necrosis factor receptor superfamily (TNFRSF), plays a key role in the activation of the immune system. FAP is abundantly expressed by CAFs in the majority of solid tumors. HSA binding prolongs the half-life of MP0317. Compared to antibodies, DARPins are small in size, have favorable pharmacokinetics and allow for both high affinity binding and efficacy.
FAPa-targeted CD40 agonist RO7300490: A CD40 agonist that targets the inducible tumor stromal antigen fibroblast activation protein-alpha (FAP-alpha; FAPa), with potential immunostimulatory and antineoplastic activities. Upon administration, FAPa-targeted CD40 agonist RO7300490 targets and binds to cell surface glycoprotein FAP which is broadly expressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment (TME) of a variety of tumors. RO7300490 also binds to and activates CD40, a cell surface stimulatory receptor that belongs to the tumor necrosis factor (TNF) receptor family and is expressed on various immune cells, such as B lymphocytes, monocytes, and dendritic cells (DCs). This crosslinks FAP-expressing CAFs and CD40-expressing immune cells. Activation of CD40 induces proliferation and activation of B lymphocytes, shifts the induction of suppressive macrophages towards immunostimulatory macrophages, activates monocyte-derived DCs (moDCs), and leads to the secretion of inflammatory cytokines, which activates the immune system to induce the proliferation and activation of cytotoxic T lymphocytes (CTLs) against tumor cells.
Fareston: (Other name for: toremifene citrate)
faricimab: A humanized bispecific antibody targeting both vascular endothelial growth factor A (VEGF-A) and angiopoietin-2 (Ang-2; Ang2; ANGPT2), that is used for the treatment of neovascular (wet) age-related macular degeneration and diabetic macular edema. Upon intravitreal administration, faricimab targets and binds to both VEGF-A and Ang-2, and prevents VEGF-A- and Ang-2-mediated signaling. The inhibition of VEGF-A-mediated signaling decreases endothelial cell proliferation, neovascularization and vascular permeability. The inhibition of Ang-2-mediated signaling improves vascular stability and desensitizes blood vessels to the effects of VEGF-A. VEGF and Ang-2, upregulated in some eye diseases, play important roles in pathological neovascularization and increased vascular permeability and inflammation, which may lead to vision loss.
farletuzumab: A humanized, immunoglobulin G1 monoclonal antibody with potential antitumor activity. Farletuzumab specifically targets at glycoprotein 3 (GP-3), a cell surface antigen that is overexpressed on many epithelial-derived cancer cells. Upon binding to the GP-3 antigen, farletuzumab triggers a host immune response against GP-3 expressing cells resulting in cell lysis.
farletuzumab ecteribulin: An antibody drug conjugate (ADC) composed of farletuzumab, a humanized immunoglobulin G1 (IgG1) monoclonal antibody directed against the folate receptor alpha (FRA; FolRa; FOLR1), and conjugated, via a cathepsin B-cleavable linker, to the microtubule-targeting agent (MTA) eribulin, a derivative of the macrocyclic polyether natural product halichondrin B, with potential antineoplastic activity. Upon administration of farletuzumab ecteribulin, the farletuzumab moiety targets and binds to FRA expressed on certain tumor cells. Upon binding, internalization, and enzymatic cleavage, eribulin binds to the vinca domain of tubulin and inhibits the polymerization of tubulin and the assembly of microtubules, resulting in inhibition of mitotic spindle assembly, induction of cell cycle arrest at G2/M phase, and the induction of tumor cell death in FRA-expressing cells. FRA is a glycosylphosphatidylinositol linked cell-surface glycoprotein that is widely expressed in certain cancers while its expression is limited in normal tissues.
Farxiga: (Other name for: dapagliflozin propanediol)
Farydak: (Other name for: panobinostat lactate)
Fas ligand-treated allogeneic mobilized peripheral blood cells: A donor graft derived from allogeneic filgrastim (granulocyte-colony stimulating factor; G-CSF)-mobilized peripheral blood cells (MPBC) that have been incubated with the recombinant human Fas ligand (FasL) APO010 ex vivo, and that can potentially be used for immune reconstitution purposes. The incubation of the hematopoietic stem cell graft with the apoptotic mediator Fas ligand (FasL) selectively induces apoptosis of mature T cells which express high levels of Fas receptor, such as T stem cell memory (TSCM), T central memory (TCM), and T effector memory (TEM) cells and the pro-inflammatory T-helper cells (Th) Th1 and Th17 subsets while sparing CD34-positive stem and progenitor cells. Upon washing and further ex vivo preparations, and upon allogeneic hematopoietic stem cell transplantation (HSCT) with the FasL-treated allogeneic MPBCs, these cells provide hematopoietic cell recovery, preserve the graft-versus-leukemia (GvL) effects, and may prevent graft-versus-host disease (GvHD).
Fas receptor agonist APO010: A recombinant, soluble, hexameric fusion protein consisting of three human Fas ligand (FasL) extracellular domains fused to the dimer-forming collagen domain of human adiponectin with potential pro-apoptotic and antineoplastic activities. Assembled into a soluble hexameric structure mimicking the ligand clustering of endogenous active FasL, Fas receptor agonist APO010 activates the Fas receptor, resulting in caspase-dependent apoptosis in susceptible tumor cell populations. FasL is a transmembrane protein of the tumor necrosis factor (TNF) superfamily and a pro-apoptotic ligand for the death receptor Fas.
fascin Inhibitor NP-G2-044: An orally available inhibitor of the protein fascin, with potential antineoplastic activity. Upon oral administration, NP-G2-044 targets and binds to fascin, thereby preventing the interaction of fascin with actin filaments, thereby preventing actin bundling and filopodia formation. By preventing actin cytoskeletal reorganization, the dynamic changes in cell shape that are necessary for tumor cell migration and invasion to occur are impaired, and tumor cell migration and metastasis are inhibited. Fascin, the main actin cross-linker protein in filopodia, is upregulated in many types of metastatic tumor cells while its expression is low or absent in normal adult epithelial cells; its expression is correlated with aggressive phenotypes, poor prognosis, and shorter survival. Filopodia, finger-like plasma membrane protrusions that are formed upon remodeling of the actin cytoskeleton, are found at a high frequency in metastatic tumor cells and their presence is correlated with tumor cell invasiveness.
Fasenra: (Other name for: benralizumab)
Fasigyn: (Other name for: tinidazole)
Faslodex: (Other name for: fulvestrant)
fat emulsion: A liquid composed of two immiscible substances, typically some form of fat and water. In parenteral nutrition, a fat emulsion may contain phospholipids, triglycerides and essential fatty acids.
favezelimab: A humanized, immunoglobulin G4 (IgG4) monoclonal antibody (MAb) directed against the inhibitory receptor lymphocyte activation gene-3 protein (LAG3), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, favezelimab binds to LAG3 expressed on tumor-infiltrating lymphocytes (TILs) and blocks its binding with major histocompatibility complex (MHC) class II molecules expressed on tumor cells. This activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG3, a member of the immunoglobulin superfamily (IgSF), is expressed on various immune cells, and negatively regulates both proliferation and activation of T cells. Its expression on TILs is associated with tumor-mediated immune suppression.
favezelimab/pembrolizumab formulation: A coformulation containing favezelimab, a humanized, immunoglobulin G4 (IgG4) monoclonal antibody (MAb) directed against the inhibitory receptor lymphocyte activation gene-3 protein (LAG3), and pembrolizumab, a humanized monoclonal IgG4 antibody directed against human cell surface receptor PD-1 (programmed death-1 or programmed cell death-1), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration of the favezelimab/pembrolizumab formulation, favezelimab binds to LAG3 expressed on tumor-infiltrating lymphocytes (TILs) and blocks its binding with major histocompatibility complex (MHC) class II molecules expressed on tumor cells. This activates antigen-specific T lymphocytes and enhances cytotoxic T-cell-mediated tumor cell lysis, which leads to a reduction in tumor growth. Pembrolizumab binds to PD-1, an inhibitory signaling receptor expressed on the surface of activated T cells, and blocks the binding to and activation of PD-1 by its ligands, which results in the activation of T-cell-mediated immune responses against tumor cells LAG3, a member of the immunoglobulin superfamily (IgSF) expressed on various immune cells, negatively regulates both proliferation and activation of T cells. Its expression on TILs is associated with tumor-mediated immune suppression. The ligands for PD-1 include programmed cell death ligand 1 (PD-L1), overexpressed on certain cancer cells, and programmed cell death ligand 2 (PD-L2), which is primarily expressed on antigen presenting cells (APCs). Activated PD-1 negatively regulates T-cell activation and plays a key role in tumor evasion from host immunity.
fazarabine: An orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug.
Fc fusion IL-7 mimetic MDK-703: A fusion protein composed of MDK-1472, a structurally unrelated engineered mimetic peptide of endogenous human cytokine interleukin-7 (hIL-7), fused to an immunoglobulin G2 (IgG2) Fc-domain, with hematopoietic and immunopotentiating activities. Upon administration, Fc fusion IL-7 mimetic MDK-703 mimics endogenous cytokine IL-7 and binds to the IL-7 receptor (IL7R) on immune cells. The binding of IL-7 to IL7R activates IL7/IL7R-mediated signaling, which leads to the expansion of various subsets of T-lymphocytes, including memory T cells, especially CD8 and CD4 stem cell memory T cells (Tscm), central memory T cells (Tcm) and effector memory T cells (Tem). This may improve immune recovery and activation and may enhance T-cell-mediated anti-tumor immune responses. Fusion to the Fc domain enhances the half-life of the IL-7 mimetic. As MDK-703 is unrelated in sequence to the natural cytokine, it is unlikely to generate anti-drug antibodies (ADAs) that neutralize the endogenous IL-7 cytokine. IL-7 is a cytokine critical for the development, maintenance and survival of T-cell subpopulations.
Fc-engineered anti-CD40 agonist antibody 2141-V11: A Fc-engineered agonistic antibody targeting the human B-cell surface antigen CD40, with potential immunostimulatory and antineoplastic activities. Upon intratumoral administration, 2141-V11 targets and binds to CD40 on a variety of immune cell types. This induces CD40-dependent signaling pathways, triggers the proliferation and activation of antigen-presenting cells (APCs) and activates T cells. This results in an enhanced cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. CD40, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on various immune cells, such as dendritic cells (DCs), macrophages and B cells, and plays a key role in the activation of the immune system.
Fc-IL-15 prodrug fusion molecule ASKG315: An engineered, prodrug form of the human endogenous cytokine interleukin-15 (IL-15), composed of a mutated form of IL-15 fused to a Fc fragment and linked to a masking moiety via a tumor protease-cleavable linker, with potential antineoplastic activity. Upon administration of Fc-IL-15 prodrug fusion molecule ASKG315, IL-15 is bound to the masking moiety and pharmacologically inactive. Upon proteolytic cleavage in the tumor microenvironment (TME), active IL-15 is released. IL-15 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. The selective activation in the TME enhances the IL-15-mediated cytolytic responses against tumor cells while sparing the unwanted effects of systemic, peripheral immune activation.
Fc-VEGFR1 fusion protein PB101: A glycosylated decoy receptor fusion protein that is composed of the vascular endothelial growth factor receptor-1 (VEGFR1; VEGFR-1) backbone and fused to fragments of Fc region, with potential anti-angiogenic, immunomodulating and antineoplastic activities. Upon administration, Fc-VEGFR1 fusion protein PB101 targets, binds to and neutralizes placental growth factor (PlGF; PGF) and VEGF-A and VEGF-B, thereby inhibiting the binding of PlGF and VEGF-A and -B to VEGFR-1 and prevents subsequent VEGFR-1 phosphorylation and VEGFR1-mediated signaling. This may result in the inhibition of tumor angiogenesis and, by blocking blood flow, inhibits tumor cell proliferation. By simultaneously inhibiting both VEGF and PlGF signaling within the tumor microenvironment (TME), PB101 modulates the immunosuppressive TME and enhances CD8-positive T-cell infiltration into the tumor. Both PGF, a member of the VEGF sub-family, and VEGF play key roles in angiogenesis, and are upregulated in many cancers. Tumor vasculature plays an important role in promoting tumor progression and immune evasion.
febuxostat: An orally available, non-purine inhibitor of xanthine oxidase with uric acid lowering activity. Upon oral administration, febuxostat selectively and noncompetitively inhibits the activity of xanthine oxidase, an enzyme that converts oxypurines, including hypoxanthine and xanthine, into uric acid. By inhibiting xanthine oxidase, uric acid production is reduced and serum uric acid levels are lowered. Febuxostat may provide protection against acute renal failure caused by the excessive release of uric acid that occurs upon massive tumor cell lysis resulting from the treatment of some malignancies.
FEC Regimen: A regimen consisting of fluorouracil, epirubicin and cyclophosphamide used in the adjuvant setting and also for the treatment of recurrent and metastatic breast cancer.
fecal microbiota preparation MTP-101P: An oral preparation composed of purified, freeze-dried fecal microbiota prepared from the stool of healthy donors and containing live bacteria, with potential gut microbiome restoring and immunomodulatory activities. Upon oral administration of the fecal microbiota preparation MTP-101P, the donor fecal transplant may restore the unhealthy, altered gut microbiome, enhance the microbial diversity and function in the gastrointestinal (GI) tract and may re-establish a healthy microbiome in the GI tract. This may relieve GI disorders and may enhance the patients' immunological activity.
fecal microbiota transplantation capsule: An oral capsule formulation composed of frozen ready-to-use human fecal microbiota from screened, healthy donors with healthy gut microbiota, for the potential treatment of recurrent Clostridium difficile (C. difficile) infections. Upon oral administration of the fecal microbiota transplantation (FMT) capsule, the microbiota in the capsule populate the gastrointestinal (GI) tract. The transplanted microbiota allows re-population of the patient's microbiome with diverse protective microorganisms that competitively exclude C. difficile. This prevents recurrent C. difficile infections.
fedratinib: An orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration, fedratinib competes with wild-type JAK2 as well as mutated forms for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, inhibition of tumor cell proliferation and induction of tumor cell apoptosis. JAK2 is the most commonly mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs). In addition, fedratinib targets, binds to and inhibits the activity of FLT3. This inhibits uncontrolled FLT3 signaling and results in the inhibition of proliferation in tumor cells overexpressing FLT3. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias and plays a key role in tumor cell proliferation.
fedratinib hydrochloride: The monohydrate dihydrochloride salt form of fedratinib, an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration, fedratinib competes with wild-type JAK2 as well as mutated forms for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, inhibition of tumor cell proliferation and induction of tumor cell apoptosis. JAK2 is the most commonly mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs). In addition, fedratinib targets, binds to and inhibits the activity of FLT3. This inhibits uncontrolled FLT3 signaling and results in the inhibition of proliferation in tumor cells overexpressing FLT3. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias and plays a key role in tumor cell proliferation.
feladilimab: An agonistic antibody for the inducible T-cell co-stimulator (ICOS; CD278), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, feladilimab targets and binds to ICOS expressed on tumor infiltrating CD4-positive T cells. This stimulates ICOS-positive T-cell proliferation, enhances cytotoxic T-lymphocyte (CTL) survival and increases CTL-mediated immune responses against tumor cells. ICOS, a T-cell specific, CD28-superfamily costimulatory molecule and immune checkpoint protein, is normally expressed on certain activated T cells and plays a key role in the proliferation and activation of T cells.
felcisetrag: A serotonin (5-HT) type 4 receptor agonist with potential gastrointestinal (GI) prokinetic activity. Upon administration, felcisetrag targets and binds to 5-HT4, thereby enhancing its activity. This may enhance GI motility, decrease GI tract and colonic transit time and improve constipation.
Feldene: (Other name for: piroxicam)
felezonexor: An orally bioavailable inhibitor of the nuclear export protein exportin-1 (XPO1; chromosome region maintenance 1 protein homolog; CRM1), with potential antineoplastic and pro-apoptotic activities. Upon administration, felezonexor reversibly binds to the cargo binding site of XPO1, and prevents the XPO1-mediated nuclear export of cargo proteins, including tumor suppressor proteins (TSPs), such as p53, FOXO, p21, and p27, and leads to their selective accumulation in the nuclei of tumor cells. As a selective inhibitor of nuclear export (SINE), SL-801 restores the nuclear localization and function of TSPs, which leads to the induction of apoptosis in tumor cells. XPO1, the major export factor that transports proteins and RNA from the nucleus to the cytoplasm, is overexpressed in a variety of cancer cell types while minimally expressed in normal, healthy cells. The dysregulated export of TSPs into the cytoplasm prevents TSP-initiated apoptosis. XPO1 overexpression leads to uncontrolled tumor cell proliferation and is associated with poor prognosis.
felmetatug vedotin: An antibody-drug conjugate (ADC) composed of a human immunoglobulin (Ig) G1 monoclonal antibody directed against the T-cell checkpoint ligand B7-H4 (V-set domain-containing T-cell activation inhibitor 1; VTCN1; B7x; B7S1) linked to the microtubule-disrupting cytotoxic agent monomethyl auristatin E (MMAE), via a protease-cleavable peptide linker, with potential antineoplastic activity. Upon administration of anti-B7-H4 ADC SGN-B7H4V, the anti-B7-H4 monoclonal antibody moiety targets and binds to B7-H4 expressed on tumor cells. Upon binding, internalization and linker cleavage, MMAE binds to tubulin and inhibits tubulin polymerization, which results in G2/M phase arrest and apoptosis specifically in B7-H4-expressing tumor cells. B7-H4, a member of the B7 family of immune modulators, is upregulated in a variety of tumor cell types and tumor-associated macrophages (TAMs). It negatively regulates T-cell immune responses. In addition, SGN-B7H4V may also kill B7-H4-expressing tumor cells through antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP).
Femara: (Other name for: letrozole)
Femest: (Other name for: conjugated estrogens)
Feminone: (Other name for: ethinyl estradiol)
fenofibrate: A synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity. Fenofibrate is hydrolyzed in vivo to its active metabolite fenofibric acid that binds to and activates peroxisome proliferator activated receptor alpha (PPARalpha), resulting in the activation of lipoprotein lipase and reduction of the production of apoprotein C-III, an inhibitor of lipoprotein lipase activity. Increased lipolysis and a fall in plasma triglycerides, in turn, leads to the modification of the small, dense low density lipoporotein (LDL) particles into larger particles that are catabolized more rapidly due to a greater affinity for cholesterol receptors. In addition, activation of PPARalpha also increases the synthesis of apoproteins A-I, A-II, and high density lipoprotein (HDL)-cholesterol. Overall, fenofibrate reduces total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) while increasing HDL cholesterol.
fenofibric acid: The active form of fenofibrate, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity.
fenretinide: An orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types. This agent also inhibits tumor growth by modulating angiogenesis-associated growth factors and their receptors and exhibits retinoid receptor-independent apoptotic properties.
fenretinide lipid matrix: An orally bioavailable powder formulation of a synthetic phenylretinamide analogue of retinol with potential chemopreventive and antineoplastic activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types, including those of the colon, breast, prostate, and neuroblastoma. Independent of RAR activation, this agent also modulates gene expression that leads to ceramide-induced, caspase-independent programmed cell death (PCD) via effectors such as ganglioside GD3 and reactive oxygen species (ROS). Compared to the capsule form, the powder contains a mixture of wheat flour, fats, and sugar that may contribute to the enhanced bioavailability of fenretinide.
Fenretinide Lym-X-Sorb: (Other name for: fenretinide lipid matrix)
fenretinide phospholipid suspension ST-001: An intravenous formulation composed of a phospholipid suspension of nanoparticles containing the synthetic retinoid derivative fenretinide, with potential antineoplastic activity. Upon intravenous administration, fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in susceptible tumor cell types. Fenretinide also binds to and inhibits the activity of mammalian target of rapamycin (mTOR), which may result in both the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Independent of RAR activation and mTOR inhibition, this agent may also modulate gene expression that leads to ceramide-induced, caspase-independent programmed cell death (PCD) via effectors such as ganglioside GD3 and reactive oxygen species (ROS).
fentanyl buccal soluble film: A transmucosal formulation consisting of a small, mucoadhesive, bioerodible polymer disc formulated with the citrate salt of fentanyl, a synthetic anilidopiperidine opioid with analgesic activity. Upon application, fentanyl buccal soluble film rapidly releases fentanyl which is quickly absorbed into the systemic circulation. Fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates.
fentanyl citrate: The citrate salt of fentanyl, a synthetic opioid related to the phenylpiperidines with analgesic and anesthetic properties. Fentanyl exerts its analgesic effect by selectively binding to the mu-opioid receptor in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. Additional pharmacological effects of fentanyl include anxiolysis, euphoria, feelings of relaxation, respiratory depression, constipation, miosis, and cough suppression.
fentanyl citrate buccal tablet: A tablet formulation containing the citrate salt of the synthetic anilidopiperidine opiate fentanyl with analgesic activity. Upon contact with the buccal mucosa, fentanyl citrate buccal tablet rapidly releases fentanyl which is quickly absorbed into the systemic circulation. Fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opioids.
fentanyl citrate pectin-based nasal spray: A pectin-based, aqueous nasal spray containing the citrate salt of fentanyl, a synthetic lipophilic phenylpiperidine opioid, with analgesic activity. Fentanyl binds to and stimulates mu-opioid receptors in the central nervous system (CNS), mimicking the analgesic effect of endogenous opiates. Upon intranasal administration of this agent and contact with the nasal mucosa, pectin in low-viscosity aqueous solution gels in the presence of mucosal calcium ions; from this intranasal gel delivery platform, fentanyl is released into the systemic circulation in a relatively rapid but controlled and sustained manner.
fentanyl citrate-containing nasal spray: A nasal spray containing a phosphate-buffered solution of the citrate salt form of fentanyl, a short-acting, synthetic, lipophilic anilidopiperidine opioid, with analgesic activity. Upon applying one puff in the nostril, the fentanyl is rapidly absorbed through the nasal mucosa and selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opiates. Due to its quick onset and short duration of action, the administration of fentanyl nasal spray may relieve breakthrough pain in adults already receiving maintenance opioid therapy for chronic pain.
fentanyl matrix transdermal patch: A transdermal formulation containing the synthetic phenylpiperidine opioid agonist fentanyl, with analgesic activity. Upon topical administration, fentanyl diffuses from the transdermal patch through the skin, is transported via the systemic circulation, and selectively binds to the mu-receptor in the central nervous system (CNS), mimicking the effects of endogenous opiates. Stimulation of the mu-receptor inhibits adenyl cyclase activity, induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels, and blocks the opening of N-type voltage-gated calcium channels, resulting in hyperpolarization and reduced neuronal excitability; in addition, neuronal release of neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline may decrease.
fentanyl sublingual spray: A sublingual preparation of a short-acting, synthetic anilidopiperidine opioid with analgesic activity. After rapid sublingual transmucosal absorption, the active ingredient fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opiates.
Fentora: (Other name for: fentanyl citrate buccal tablet)
Feraheme: (Other name for: ferumoxytol non-stoichiometric magnetite)
Feridex: (Other name for: ferumoxides injectable solution)
fermented prebiotic dietary supplement AferBio: A powder-based nutritional supplement composed of Brazilian fermented non-digestible food composed of soy, wheat, and organic wheat germ, and containing a mixture of non-soluble and fermentable fibers rich in oligosaccharides, with potential immunomodulating and prebiotic activities. Upon oral administration of the fermented prebiotic dietary supplement, the high concentrations of beta-glucans are able to stimulate the proliferation of beneficial bacteria in the gastrointestinal (GI) tract. This modulates the GI flora ecosystem, improves the functions of the intestinal barrier and protects against harmful viruses and bacteria. In addition, this prebiotic modulates the immune system and may inhibit inflammation.
fermented soybean extract: A nutritional supplement composed of an organic fermented soybean extract, with potential antioxidant, chemoprotective, anti-inflammatory, and immunostimulatory activities. During the microbial fermentation process, the nutrients in the soybean are broken down in many different substances, such as fatty acids, various amino acids and isoflavones, such as genistein and daidzein. The extract also contains other beneficial dietary nutrients, including certain trace elements and vitamins. Upon oral administration of the fermented soybean extract, the active ingredients in the extract provide essential nutrients to the body and may have immunostimulatory, pro-apoptotic, anti-proliferative, and anti-inflammatory activities and may scavenge free radicals. In addition, many ingredients in the soy extract may modulate key estrogen and androgen signaling pathways, which may further induce apoptosis and reduce proliferation in tumor cells in which these hormones are overactivated. The fermentation process allows for enhanced bioavailability of the soy nutrients.
fermented soybean MS-20: A dietary supplement composed of an organic fermented soybean extract, with potential antioxidant, chemoprotective, anti-inflammatory, immunostimulatory and anti-cachexia activities. During the microbial fermentation process, the nutrients in soybean are broken down into many different substances, including isoflavones. Upon oral administration of the fermented soybean extract MS-20, the active ingredients in the extract provide essential nutrients to the body and may have anti-cachexia, immunostimulatory, pro-apoptotic, anti-proliferative, and anti-inflammatory activities and may scavenge free radicals.
fermented soybean protein beverage: A fermented soybean-derived phytochemical beverage with potential antineoplastic activity. Fermented soybean protein beverage is reported to exhibit immunostimulatory, anti-viral, pro-apoptotic, anti-angiogenic, anti-proliferative, and anti-inflammatory activities and to enhance the cytotoxic effects of natural killer (NK) cells. The fermentation process is reported to hydrolyze many soybean proteins into amino acids and nitrogen-rich compounds and to protect and enhance the activities of isoflavones such as genistein, protease inhibitors, saponins, phytosterols, inositol hexaphosphate, and other beneficial dietary nutrients and micronutrients found in soybeans.
fermented wheat germ extract: An extract of fermented wheat germ containing a concentrated, standardized amount of methoxy-substituted benzoquinones with immunomodulatory and potential antineoplastic activities. Fermented wheat germ extract (FWGE) inhibits the activities of several enzymes involved in de novo nucleic acid synthesis and in supplying the dNTP pool required for DNA replication. This agent also induces caspase-3- mediated inactivation of poly(ADP)ribose polymerase (PARP), a key enzyme in DNA repair that is overexpressed in many cancers; cleavage of PARP prevents DNA repair and induces apoptosis. The benzoquinones may contribute to the immunomodulatory effects of FWGE, down-regulating major histocompatibility complex class I (MHC-1) protein on the surface of cancer cells, allowing natural killer (NK) cell surveillance; and up-regulating the expression of intracellular adhesion molecule 1 (ICAM-1) on tumor endothelial cells.
Ferndex: (Other name for: dextroamphetamine sulfate)
ferric carboxymaltose solution: A parenteral iron solution containing ferric iron complexed with carboxymaltose polymers, used in parenteral iron-replacement therapy. Upon administration, ferric carboxymaltose is removed from plasma by the reticuloendothelial system. Subsequently, ferric iron binds to transferrin or is stored as ferritin. Transferrin-bound iron is transported in the plasma to the liver, spleen and bone marrow, where it is incorporated into hemoglobin, and to muscle, where it is incorporated into myoglobin.
ferric derisomaltose: An iron carbohydrate complex composed of ferric hydroxide and the carbohydrate derisomaltose, that may be used for the treatment of iron deficiency anemia. Upon intravenous administration of ferric derisomaltose, ferric iron is released and binds to transferrin. Transferrin-bound iron is transported to erythroid precursor cells and incorporated into hemoglobin.
Ferriprox: (Other name for: deferiprone)
Ferrlecit: (Other name for: sodium ferric gluconate complex in sucrose)
ferrous fumarate: The fumarate salt form of the mineral iron. Administration of ferrous fumarate results in elevation of serum iron concentration, which is then assimilated into hemoglobin, required for the transport of oxygen, or trapped in the reticuloendothelial cells for storage. This agent is used as a dietary supplement, and to prevent or treat iron deficiency related syndromes.
ferrous sulfate: A sulfate salt of mineral iron formulated for oral administration and used as a dietary supplement, ferrous sulfate is absorbed in the stomach and small intestine and combines with apoferritin to form ferritin, which is stored in the liver, spleen, red bone marrow, and intestinal mucosa. Important in transport of oxygen by hemoglobin to the tissues, iron is also found in myoglobin, transferrin, and ferritin, and is a component of many enzymes such as catalase, peroxidase, and cytochromes.
ferumoxides injectable solution: An injectable, aqueous colloid solution containing a non-stoichiometric magnetite core of superparamagnetic iron oxide (SPIO) coated with dextran administered as a magnetic resonance imaging (MRI) contrast media. Upon intravenous administration, ferumoxides accumulates in phagocytic reticuloendothelial system (RES) cells of the liver (Kupffer cells). When exposed to a strong external magnetic field, ferumoxides exhibits enhanced T2 relaxation, resulting in signal loss in normal tissues (image darkening) on mid T1/T2 or strongly T2-weighted images. Tissues with decreased RES function such as metastases, primary liver cancer, cysts and various benign tumors, adenomas, and hyperplasia, retain their native signal intensity, consequently the contrast between normal tissue (with image darkening) and abnormal tissue is increased.
ferumoxides non-stoichiometric magnetite: A non-stoichiometric magnetite core of superparamagnetic iron oxide (SPIO) that can be used as part of contrast media to enhance magnetic resonance imaging (MRI). Upon administration, ferumoxides non-stoichiometric magnetite is taken up by and accumulates in phagocytic reticuloendothelial system (RES) cells of the liver (Kupffer cells). When exposed to a strong external magnetic field, ferumoxides non-stoichiometric magnetite exhibits enhanced T2 relaxation, resulting in signal loss in normal tissues (image darkening) on mid T1/T2 or strongly T2-weighted images. Tissues with decreased RES function such as metastases, primary liver cancer, cysts, various benign tumors and hyperplasia, retain their native signal intensity, consequently the contrast between normal tissue (with image darkening) and abnormal tissue is increased.
ferumoxsil oral suspension: An orally administered aqueous suspension of silicone-coated, superparamagnetic iron oxide used as a magnetic resonance imaging (MRI) contrast agent. After oral administration, ferumoxsil fills the stomach and intestines. Upon exposure to the strong external magnetic field during MRI, ferumoxsil exhibits strong T1 relaxation properties and a strongly varying local magnetic field; T2 relaxation is enhanced, thereby darkening the contrast agent-containing portion of the gastrointestinal tract. Delineation of the bowel is thus enhanced, distinguishing bowel from organs and tissues adjacent to the upper regions of the gastrointestinal tract.
ferumoxtran-10: A synthetic ultrasmall superparamagnetic iron oxide composed of dextran-coated iron oxide nanoparticles (also known as 'ultrasmall particulate iron oxides' or USPIO). Ferumoxtran-10, which accumulates in non-cancerous lymphatic tissue, is used as a molecular resonance imaging (MRI) contrast agent.
ferumoxytol non-stoichiometric magnetite: A superparamagnetic iron oxide nanoparticle coated with a low molecular weight semi-synthetic carbohydrate, polyglucose sorbitol carboxymethyl ether, with potential anti-anemic and imaging properties. After intravenous administration, ferumoxytol replaces iron stores with fewer side effects compared to the use of oral iron. In addition, this agent generates T1 relaxation, producing a magnetic field and enhancing T2 relaxation, thereby darkening contrast media-containing structures in magnetic resonance imaging (MRI). Due to small particle size, ferumoxytol remains in the intravasculature for a prolonged period and so may be used as a blood pool agent.
fesoterodine fumarate: The fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyltolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine. This results in the relaxation of bladder smooth muscle and greater bladder capacity, in addition to a reduction in involuntary muscle contractions and involuntary loss of urine. The active metabolite does not interact with alpha-adrenergic, serotonergic, histaminergic and excitatory amino acid receptors and is eliminated via renal excretion.
fexagratinib: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. fexagratinib binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways, and, so, the inhibition of tumor cell proliferation and tumor cell death. FGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cellular proliferation, differentiation and survival.
fexofenadine hydrochloride: The hydrochloride salt form of fexofenadine, a carboxylated metabolic derivative of terfenadine and third generation selective histamine H1-receptor antagonist with antihistaminic and non-sedative effects. Fexofenadine competitively binds peripheral H1-receptors, thereby stabilizing an inactive conformation of the receptor. Consequently histamine binding and activity as a result of mast-cell degranulation followed by the release of multiple inflammatory mediators, such as interleukins, prostaglandin and leukotriene precursors, is blocked, thereby preventing the triggering of pro-inflammatory pathways.
fezolinetant: An orally bioavailable, neurokinin/tachykinin 3 receptor (NK1-receptor; NK3R; NK-3R) antagonist, that can be used to treat vasomotor symptoms (VMS) in menopausal woman. Upon oral administration, fezolinetant targets, competitively binds to and blocks the activity of NK3R in the central nervous system (CNS). Specifically, this blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDgamma) neuron in the thermoregulatory center and inhibits NK3R-mediated signal transduction. This prevents VMS. Neurokinin-mediated signaling may increase during hormone deficiency and may cause VMS.
FGF/FGFR pathway inhibitor E7090: An inhibitor of the fibroblast growth factor (FGF)/fibroblast growth factor receptor (FGFR) pathway, with potential antineoplastic activity. Upon administration, the FGF/FGFR pathway inhibitor E7090 selectively interferes with the binding of FGF to FGFR through an as of yet not fully elucidated mechanism. This inhibits FGFR-mediated signaling and leads to both cell proliferation inhibition and cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation, and survival; its expression is upregulated in many tumor cell types.
FGF401 inhibitor FGF401: An inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, FGF401 binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival.
FGFR inhibitor ASP5878: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR), with potential antineoplastic activity. Upon oral administration, FGFR inhibitor ASP5878 binds to and inhibits FGFR, which results in the inhibition of FGFR-mediated signal transduction pathways. This inhibits proliferation in FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, plays a key role in cellular proliferation and survival.
FGFR inhibitor CPL304110: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR), with potential antineoplastic activity. Upon oral administration, FGFR inhibitor CPL304110 binds to and inhibits FGFR, which results in the inhibition of FGFR-mediated signal transduction pathways. This inhibits proliferation in FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, plays a key role in cellular proliferation and survival.
FGFR inhibitor ET0111: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR), with potential antineoplastic activity. Upon oral administration, FGFR inhibitor ET0111 binds to and inhibits FGFR, which results in the inhibition of FGFR-mediated signal transduction pathways. This inhibits proliferation in FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, plays a key role in cellular proliferation and survival.
FGFR inhibitor1/2/3 HMPL-453: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) types 1, 2, and 3 (FGFR1/2/3), with potential antineoplastic activity. Upon administration, FGFR inhibitor HMPL-453 binds to and inhibits FGFR1/2/3, which may result in the inhibition of FGFR1/2/3-related signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases (RTKs) upregulated in many tumor cell types, plays a key role in cellular proliferation, migration and survival.
FGFR/VEGFR/PDGFR/FLT3/SRC inhibitor XL999: A small molecule inhibitor of numerous tyrosine kinases (TKs) including fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), FMS-related tyrosine kinase 3 (FLT3), and SRC, with potential antineoplastic activity. Upon administration, XL999 binds to and inhibits the activity of these TKs, thereby preventing both the activation of downstream signaling pathways and the proliferation of tumor cells overexpressing these TKs. FGFR, VEGFR, PDGFR, FLT-3, and SRC are upregulated in a variety of cancer cell types and play key roles in tumor cell proliferation, angiogenesis, and metastasis.
FGFR1 receptor antagonist HGS1036: A soluble fusion protein consisting of the extracellular domain of human fibroblast growth factor receptor 1 (FGFR1) fused to the Fc portion of human immunoglobulin G1 (IgG1) with potential antineoplastic and anti-angiogenic activities. FGFR1 receptor antagonist FP-1039 prevents FGFR ligands, such as FGF1, FGF2, FGF4, from binding to their cognate receptors, thereby inhibiting the activation of the related FGFR tyrosine kinases. Inhibition of FGFR1 by this agent may retard tumor cell proliferation and induce tumor cell death. FP-1039 may also inhibit vascular endothelial growth factor (VEGF)-induced angiogenesis. FGFR1 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cellular proliferation, differentiation, angiogenesis, and survival; most ligands that bind to FGFR1 also bind to the related receptors FGFR3 and FGFR4.
FGFR1/2/3 inhibitor TYRA-200: An orally bioavailable inhibitor of the tyrosine kinase fibroblast growth factor receptor (FGFR) types 1, 2, and 3 (FGFR1/2/3), with potential antineoplastic activity. Upon oral administration, FGFR1/2/3 inhibitor TYRA-200 targets, binds to and inhibits FGFR1/2/3, and is specifically active against certain FGFR2 fusions, molecular brake and gatekeeper resistance mutations. This may result in the inhibition of FGFR1/2/3-related signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases (RTKs), is upregulated in many tumor cell types.
FGFR2 inhibitor 3HP-2827: An orally bioavailable small molecule inhibitor of fibroblast growth factor receptor 2 (FGFR2), with potential antineoplastic activity. Upon oral administration, FGFR2 inhibitor 3HP-2827 targets, binds to and inhibits FGFR2, which results in the inhibition of FGFR2-mediated signal transduction pathways. This may inhibit the proliferation of tumor cells that harbor FGFR2 alterations, including amplifications, mutations and fusions. FGFR2, a receptor tyrosine kinase upregulated and mutated in many tumor cell types, plays a key role in cellular proliferation, migration and survival.
FGFR2 inhibitor RLY-4008: An orally bioavailable inhibitor of the fibroblast growth factor receptor 2 (FGFR2), with potential antineoplastic activity. Upon oral administration, FGFR2 inhibitor RLY-4008 binds to and inhibits FGFR2, which results in the inhibition of FGFR2-mediated signal transduction pathways. This inhibits the proliferation of FGFR2-overexpressing tumor cells. FGFR2, a receptor tyrosine kinase upregulated in many tumor cell types, plays a key role in cellular proliferation, migration and survival.
FGFR2/3 inhibitor CGT4859: An orally bioavailable reversible inhibitor of fibroblast growth factor receptor (FGFR) types 2 and 3 (FGFR2/3), with potential antineoplastic activity. Upon oral administration, FGFR2/3 inhibitor CGT4859 targets, reversibly binds to and inhibits FGFR2/3, and is specifically active against FGFR2 molecular brake and gatekeeper resistance mutations. This blocks FGFR2/3-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR2/3-overexpressing cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, plays a key role in cellular proliferation, cell survival and angiogenesis.
FGFR3 inhibitor LOXO-435: An orally bioavailable, selective inhibitor of human fibroblast growth factor receptor 3 (FGFR3), with potential antineoplastic activity. Upon oral administration, FGFR3 inhibitor LOXO-435 specifically targets and binds to FGFR3, including FGFR3 gatekeeper resistance mutations. This blocks FGFR3-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR3-overexpressing cells. FGFR3, a receptor tyrosine kinase, is involved in angiogenesis and in the proliferation, differentiation, and survival of tumor cells. FGFR3 expression is associated with poor prognosis. It is overexpressed and/or mutated by certain tumor cell types.
FGFR4 antagonist INCB062079: An orally bioavailable, selective inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, FGFR4 antagonist INCB062079 specifically and irreversibly binds to the cysteine residue at position 552 (Cys 552) that is within the active site of FGFR4. This blocks FGFR4 autophosphorylation and activation of receptor tyrosine kinase activity that would normally occur after binding to its ligand fibroblast growth factor 19 (FGF19), which both inhibits FGFR4-mediated signaling and leads to an inhibition of tumor cell proliferation in FGF19- and FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase, is involved in angiogenesis and in the proliferation, differentiation, and survival of tumor cells. FGFR4 expression is associated with poor prognosis. FGF19 is overexpressed by certain tumor cell types.
FGFR4 inhibitor ABSK-011: An orally bioavailable, selective inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, FGFR4 inhibitor ABSK-011 specifically and irreversibly binds to the cysteine residue at position 552 (Cys 552) that is within the active site of FGFR4. This blocks FGFR4 autophosphorylation and activation of receptor tyrosine kinase activity that would normally occur after binding to its ligand, fibroblast growth factor 19 (FGF19), which both inhibits FGFR4-mediated signaling and leads to the inhibition of tumor cell proliferation in FGF19- and FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase, is involved in angiogenesis and in the proliferation, differentiation, and survival of tumor cells. FGFR4 expression is associated with poor prognosis. FGF19 is overexpressed by certain tumor cell types.
FGFR4 inhibitor H3B-6527: An orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon administration, H3B-6527 specifically binds to and blocks FGFR4. This prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of cell proliferation in FGFR4-overexpressing tumor cells. FGFR4, a receptor tyrosine kinase overexpressed by certain tumor cell types, is involved in tumor cell proliferation, differentiation, angiogenesis, and survival; FGFR4 expression is associated with poor prognosis.
FGFR4 inhibitor ICP-105: An orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, ICP-105 specifically targets, binds to and blocks the binding of the ligand FGF19 to FGFR4. This prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase overexpressed on a variety of cancer cell types, is involved in tumor cell proliferation, differentiation, angiogenesis, and survival. FGF19 is overexpressed by certain tumor cell types.
FGFR4 inhibitor SY-4798: An orally bioavailable, selective inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, FGFR4 inhibitor SY-4798 specifically targets and binds to FGFR4. This blocks FGFR4 autophosphorylation and activation of receptor tyrosine kinase activity that would normally occur after binding to its ligand, fibroblast growth factor 19 (FGF19). This inhibits FGFR4-mediated signaling and leads to the inhibition of tumor cell proliferation in FGF19- and FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase, is involved in angiogenesis and in the proliferation, differentiation, and survival of tumor cells. FGFR4 expression is associated with poor prognosis. FGF19 is overexpressed by certain tumor cell types.
FGFR4 inhibitor SYHX2005: An orally bioavailable, selective inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, FGFR4 inhibitor SYHX2005 specifically targets and binds to FGFR4. This blocks FGFR4 autophosphorylation and activation of receptor tyrosine kinase activity that would normally occur after binding to its ligand, fibroblast growth factor 19 (FGF19). This inhibits FGFR4-mediated signaling and leads to the inhibition of tumor cell proliferation in FGF19- and FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase, is involved in angiogenesis and in the proliferation, differentiation, and survival of tumor cells. FGFR4 expression is associated with poor prognosis. FGF19 is overexpressed by certain tumor cell types.
fianlimab: A monoclonal antibody directed against the inhibitory receptor lymphocyte activation gene-3 protein (LAG-3; LAG3; CD223), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, fianlimab binds to LAG-3 expressed by tumor infiltrating lymphocytes (TILs) and blocks LAG-3 binding to tumor cells expressing major histocompatibility complex (MHC) class II molecules. This may activate antigen-specific T lymphocytes and enhance cytotoxic T-lymphocyte (CTL)-mediated tumor cell lysis, which leads to a reduction in tumor growth. LAG-3, a member of the immunoglobulin superfamily (IgSF), is expressed on various immune cells; its expression on TILs is associated with tumor-mediated immune suppression and the negative regulation of both cellular proliferation and T-cell activation.
Fibricor: (Other name for: fenofibric acid)
fibrin sealant: A plasma-derived fibrin biomatrix preparation consisting of two separate solutions that are combined on application. The sealer protein solution contains clottable human fibrinogen and bovine aprotinin, a fibrinolysis inhibitor; the thrombin solution contains human thrombin and calcium chloride. When the solutions are combined, a clot is formed, reproducing the final stages of the coagulation cascade.
fibroblast activation protein alpha-activated doxorubicin prodrug AVA6000: A prodrug of the anthracycline antineoplastic antibiotic doxorubicin composed of doxorubicin covalently bonded to the dipeptide N-(pyridine-4-carbonyl)-D-Ala-L-Pro, with potential antineoplastic activity. Upon administration, fibroblast activation protein alpha (FAP)-activated doxorubicin prodrug AVA6000 is hydrolyzed by FAP, which is overexpressed on cancer-associated fibroblasts (CAFs) in the tumor microenvironment (TME). Doxorubicin is released in the TME, and intercalates into DNA and interacts with topoisomerase II. This leads to an inhibition of DNA replication and repair, and prevents RNA and protein synthesis. By targeting the delivery of doxorubicin directly to the tumor, AVA6000 may result in less systemic toxicities. FAP, a membrane-bound protease, is overexpressed on CAFs in various tumors but minimally expressed on normal, healthy cells.
fibroblast-activation protein inhibitor: Any small molecule inhibitor of fibroblast activation protein (FAP).
Fibrocaps: (Other name for: fibrin sealant)
ficlatuzumab: A monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. Ficlatuzumab binds to the soluble ligand HGF, preventing the binding of HGF to its receptor c-Met and activation of the HGF/c-Met signaling pathway, which may result in cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.
ficonalkib: An orally bioavailable, third-generation inhibitor of the receptor tyrosine kinase (RTK) anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon oral administration, ficonalkib binds to and inhibits ALK wild-type tyrosine kinase and numerous ALK mutations, including acquired resistance mutations. 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 dysregulation and gene rearrangements are associated with a variety of tumor cell types.
Ficus septica leaf-based supplement FADA: A supplement composed of the active fraction of Ficus septica (Awar-Awar) leaf, with potential antineoplastic activity. Upon oral administration of Ficus septica leaf-based supplement FADA, the phytochemicals may kill tumor cells, although the exact mechanism of its cytotoxic action has yet to be fully elucidated.
fidaxomicin: A narrow-spectrum, 18-membered macrolide antibiotic isolated from the actinomycete Dactylosporangium aurantiacum subsp. hamdenensis with potential antibacterial activity. Although the exact mechanism of action has yet to be fully elucidated, fidaxomicin may bind to and inhibit bacterial DNA-dependent RNA polymerase, thereby inhibiting the initiation of bacterial RNA synthesis. When orally administered, this agent is minimally absorbed into the systemic circulation, acting locally in the gastrointestinal tract. Tiacumicin B appears to be active against pathogenic Gram-positive bacteria, such as clostridia, enterococci, and staphylococci, but does not appear to be active against other beneficial intestinal bacteria.
Fidelin: (Other name for: prasterone)
figitumumab: A human monoclonal antibody directed against the insulin-like growth factor type I receptor (IGF1R) with potential antineoplastic activity. Figitumumab selectively binds to IGF1R, preventing insulin-like growth factor type 1 (IGF1) from binding to the receptor and subsequent receptor autophosphorylation. Inhibition of IGF1R autophosphorylation may result in a reduction in receptor expression on tumor cells that express IGF1R, a reduction in the anti-apoptotic effect of IGF, and inhibition of tumor growth. IGF1R is a receptor tyrosine kinase expressed on most tumor cells and is involved in mitogenesis, angiogenesis, and tumor cell survival.
filgrastim: A recombinant, non-glycosylated cytokine which is chemically identical to or similar to the endogenous cytokine human granulocyte colony-stimulating factor (G-CSF) isoform B, with immunomodulating activity. Filgrastim binds to and activates G-CSF receptors with the same biological activity and stability as the endogenous cytokine, thereby controlling the production, differentiation, and function of neutrophilic granulocyte progenitors.
filgrastim-primed peripheral blood progenitor cells: Peripheral blood progenitor cells (PBPC) primed with a recombinant form of the human granulocyte colony-stimulating factor (filgrastim). As a hematopoietic growth factor, filgrastim is able to mobilize hematopoietic progenitor cells (HPCs) into the peripheral blood which allows for an increased number of HPCs upon collection by leukapheresis. Administration of filgrastim-primed PBPCs following hematopoietic stem cell transplantation provides increased numbers of progenitor cells which may prevent pancytopenia and relapse.
Filsuvez: (Other name for: oleogel-S10)
fimaporfin: A synthetic light-activated compound composed of three benzenesulfonic acid isomers: fimaporfin A (TPCS2a; tetraphenyl chlorin disulfonate), fimaporfin B, and fimaporfin C, with potential photosensitizing activity upon photodynamic therapy (PDT) . Upon intradermal administration, fimaporfin is incorporated into the tumor cells’ endosome and lysosome membranes. Subsequently, cytotoxic agents are administered and accumulate in the endosomal and lysosomal compartments; upon local activation by light, fimaporfin produces reactive oxygen species (ROS), such as singlet oxygen, damaging endo/lysosomal membranes and accumulated cytotoxic agents are released into the tumor cell cytosol. This photochemical internalization (PCI) method can enhance the efficacy and selectivity of cytotoxic agents.
fimepinostat: An orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, fimepinostat inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types. This may prevent growth of PI3K and/or HDAC-expressing tumor cells. CUDC-907 shows an increased inhibition of tumor cell growth and induction of apoptosis when compared to inhibitors that target either PI3K or HDAC.
finasteride: A synthetic 4-azasteroid compound. Finasteride competitively binds to and inhibits steroid type II 5-alpha-reductase in the prostate gland, liver, and skin, thereby interfering with the enzymatic conversion of testosterone to 5-dihydrotestosterone (DHT) and reducing serum DHT levels. The reduction in serum DHT levels results in diminished stimulation of androgen receptors in the nuclei of prostate cells and, so, diminished prostate cell proliferation.
firastotug: A human monoclonal antibody directed against the human T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4), with potential immune checkpoint inhibitory and antineoplastic activities. Upon intravenous administration, firastotug targets and binds to CTLA-4 expressed on T cells and inhibits the CTLA-4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells, thereby killing cancer cells. CTLA-4, an inhibitory receptor and member of the immunoglobulin superfamily (IgSF), plays a key role in the downregulation of the immune system.
Firmagon: (Other name for: degarelix)
firmonertinib: An orally available selective inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, firmonertinib specifically binds to and inhibits the tyrosine kinase activity of EGFR T790M, a secondarily acquired resistance mutation. This prevents EGFR T790M-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. EGFR, a receptor tyrosine kinase that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. Compared to some other EGFR inhibitors, alflutinib may have therapeutic benefits in tumors with T790M-mediated drug resistance.
fisetin: An orally bioavailable naturally occurring polyphenol found in many fruits and vegetables, with potential antioxidant, neuroprotective, anti-inflammatory, antineoplastic, senolytic, and longevity promoting activities. Upon administration, fisetin, as an antioxidant, scavenges free radicals, protect cells from oxidative stress, and is able to upregulate glutathione. It inhibits pro-inflammatory mediators, such as tumor necrosis factor alpha (TNF-a), interleukin-6 (IL-6), and nuclear factor kappa B (NF-kB). Fisetin promotes cellular metabolism, reduces senescence, regulates sirtuin function and may promote longevity. Fisetin also exerts anti-cancer activity by inhibiting certain signaling pathways. It also inhibits certain anti-apoptotic proteins and induces apoptosis in susceptible cells.
fish oil: An oil derived from the tissues of oily fish. Fish oil is considered valuable due to its high content of omega-3 fatty acids eicosapentanoic acid and docosahexaenoic acid. Such fatty acids are not actually produced in fish, but are accumulated from phytoplankton which produce omega-3 fatty acids.
fish oil/glycerol/egg lecithin-based emulsion: An injectable, nutritional lipid emulsion composed of 10% fish oil and high amounts of the fish oil-derived polyunsaturated omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). Additionally, the fish oil/glycerol/egg lecithin-based emulsion contains myristic acid, palmitic acid, palmitoleic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, octadecatetraenoic acid, eicosaenoic acid, arachidonic acid, docosaenoic acid, and docosapentaenoic acid. This agent supplies essential fatty acids that can be incorporated into cell membranes. The fatty acids may decrease the production of certain pro-inflammatory cytokines, including interleukin 1 (IL-1), IL-6 and tumor necrosis factor (TNF). In addition to fish oil, this lipid emulsion contains egg phospholipids to maintain membrane integrity; glycerol to provide energy through glycolysis; and the antioxidant alpha-tocopherol (vitamin E).
fisogatinib: An orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, fisogatinib specifically binds to and blocks the binding of the ligand FGF19 to FGFR4. This prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase and is involved in tumor cell proliferation, differentiation, angiogenesis, and survival. FGF19 is overexpressed by certain tumor cell types.
Flagyl I.V.: (Other name for: metronidazole hydrochloride)
flanvotumab: A monoclonal antibody directed against the melanosomal membrane protein gp75 (or Tyrosinase-Related Protein 1 [TRP1]) with potential immunostimulatory and antineoplastic activities. Flanvotumab targets and binds to gp75. This may lead to the induction of cytotoxic T cell immune and antibody-mediated immune responses against melanoma cells expressing gp75. gp75, a pigmentation-associated antigen, is expressed in melanosomes of human melanocytes and melanomas.
flavone acetic acid: A synthetic flavonoid with vascular targeting properties. Flavone acetic acid exhibits an antiproliferative effect on endothelial cells as a result of a superoxide-dependent mechanism, which induces changes in permeability of the vasculature of the tumor. This agent may stimulate tumor necrosis and promote shunting of blood flow to viable regions of the tumor, increasing their oxygenation and rendering them more susceptible to the antitumor effects of hyperthermia and ionizing radiation.
flavonoid tablet: A tablet formulation of flavonoids with antioxidant and potential chemopreventive activities. Polyphenolic, soluble plant pigment flavonoids inactivate oxygen radicals, prevent lipid peroxidation, and inhibit DNA oxidation. In vitro, these agents have been shown to increase the rate of apoptosis, and inhibit cell proliferation and angiogenesis. Furthermore, flavonoids can induce conjugating enzymes, such as glutathione transferases and glucuronosyltransferases.
flaxseed: Seed isolated from one of several species of the plant genus Linum. Flaxseed-derived foods, lignans, and essential fatty acids such as alpha-linolenic acid, possess anti-inflammatory, lipid-lowering, antioxidant, and antineoplastic properties.
flaxseed lignan: A group of bioactive polyphenolic phytoestrogens derived from the seed of the flax plant (Linum usitatissimum) with potential antioxidant and chemopreventive activities. Flaxseed lignan is primarily comprised of secoisolariciresinol diglucoside (SDG), isolariciresinol, matairesinol, pinoresinol and lariciresinol. SDG is converted to the enterolignans enterolactone (EL) and enterodiol (ED) by the intestinal microflora in the proximal colon. EL and ED have both weakly estrogenic and anti-estrogenic activities depending upon the tissue. The anti-estrogenic effects in reproductive tissue may help reduce the risk of hormone-associated cancers, while the estrogenic effects in bone may help maintain bone density. Flaxseed is the richest dietary source of lignans.
Flebogamma DIF: (Other name for: human immunoglobulin G)
Flector Patch: (Other name for: diclofenac epolamine patch)
Fleet Phospho-soda: (Other name for: sodium biphosphate/sodium phosphate oral laxative)
Flexeril: (Other name for: cyclobenzaprine hydrochloride)
Flexiban: (Other name for: cyclobenzaprine hydrochloride)
flexible heteroarotinoid sulfur heteroarotinoid A2: An orally bioavailable, synthetic flexible heteroarotinoid (Flex-Het), with antineoplastic activity. Upon oral administration, Flex-Het sulfur heteroarotinoid A2 (SHetA2) binds to the three related heat shock protein A (HSPA) chaperone proteins HSPA5 (78-kDa glucose-regulated protein; Grp78; BiP), HSPA8 (Hsc70) and HSPA9 (mortalin), and disrupts their binding to client proteins. This may induce G1 cell cycle arrest and apoptosis, and inhibit tumor cell growth, migration and invasion. Grp78, hsc70, and mortalin play important roles in ensuring the proper folding, function, and cellular localization of their client proteins, which are important for cell survival; they are mutated in certain cancer types.
flibanserin: An orally bioavailable, non-hormonal, multifunctional serotonin agonist and antagonist (MSAA) that may improve sexual desire and arousal in women. Upon oral administration, flibanserin selectively binds to serotonin receptors in the central nervous system, acting as an agonist on 5-HT1A receptors and an antagonist on 5-HT2A receptors. Agonist activity at 5-HT1A postsynaptic receptors may enhance the release of dopamine and other monoamines. Combined with 5-HT2A antagonism, flibanserin boosts levels of dopamine in the mesocortical area of the prefrontal cortex and produces a net increase of norepinephrine selectively in the prefrontal cortex through disinhibition of locus coeruleus noradrenergic neurons. In addition, flibanserin reduces concentrations of serotonin in the prefrontal cortex with chronic administration. Reducing serotonin, which modulates sexual activity in an inhibitory fashion through downstream decreases in dopamine release, while enhancing the release of norepinephrine and dopamine in the prefrontal cortex may improve sexual desire and interest.
flizasertib: An orally available inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1; receptor-interacting protein 1; RIP1) with potential immunomodulatory and anti-inflammatory activities. Upon oral administration, flizasertib inhibits RIP1-mediated signaling, which may preserve intestinal stem cells (ISCs) and prevent RIP1-mediated gastrointestinal (GI) damage in acute graft-versus-host disease (GvHD). RIP1 plays a key role in inflammation and cell death in response to tissue damage and pathogen recognition.
Flomax: (Other name for: tamsulosin hydrochloride)
Flonase: (Other name for: fluticasone propionate)
flonoltinib maleate: The maleate salt form of flonoltinib, an orally bioavailable dual inhibitor of both Janus-associated kinase 2 (JAK2) and of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon oral administration, flonoltinib targets, binds to and inhibits the activity of both JAK2 and FLT3. This prevents the activation of the JAK/signal transducer and activator of transcription (STAT) signaling pathway and the activation of STAT3 and STAT5 as well as FLT3-mediated signaling. This may lead to an induction of apoptosis and a decrease in proliferation of tumor cells in which JAK2 and FLT3 are overexpressed. In addition, as JAK2 and FLT3 play a key role in the regulation of the inflammatory response and dendritic cell (DC) proliferation, differentiation and function, inhibition of JAK2- and FLT3-mediated signaling may suppress the generation and differentiation of DCs, and may regulate inflammatory and immune responses. JAK2, often upregulated or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key role in tumor cell proliferation and survival. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.
Florafur: (Other name for: tegafur)
florbenazine F-18: A radioconjugate composed of the vesicular monoamine transporter 2 (VMAT2) targeting agent florbenazine , a dihydrotetrabenazine analog, labeled with the positron-emitting isotope fluorine F 18, that can potentially be used as a tracer using positron emitting tomography (PET) imaging. Upon administration , florbenazine F-18 binds to VMATs expressed on monoamine neurons and pancreatic beta-cells within the islets of Langerhans. Upon PET imaging, VMAT2-expressing cells can be detected and the level of functional monoamine neurons can be assessed, which can be used in the diagnosis of neurodegenerative diseases. In addition, this radiotracer can be used to assess the function of pancreatic beta-cells. VMAT2, a transporter that loads monoamine neurotransmitters into secretory vesicles, is expressed on biogenic amine-containing neurons in the central nervous system (CNS) and pancreatic beta cells.
florbetaben (18F): A stilbene derivative labeled with the positron-emitting isotope fluorine F 18, that may be used for positron emission tomography (PET) detection of beta-amyloid neuritic plaques and other amyloid protein deposits. Upon administration, F 18-florbetaben exhibits differential retention in regions that contain certain amyloid deposits. Differences in signal intensity between tissues showing specific and non-specific uptake of F 18-florbetaben allows for the detection of amyloid neuritic plaques in patients being evaluated for Alzheimer's disease, and potentially the detection of amyloid deposits in amyloidosis.
Florinef: (Other name for: fludrocortisone acetate)
flortaucipir F-18: A radioconjugate composed of the paired helical filament (PHF) tau binding agent flortaucipir, a benzimidazole pyrimidine derivative, conjugated to the radioisotope fluorine F 18, with potential tau positron emission tomography (PET) imaging activity. Upon administration, flortaucipir F-18 targets and binds to PHF-tau in the brain, which allows PET imaging of PHF-tau and analysis of phosphorylated PHF-tau aggregates (neurofibrillary tangles). Increased levels of PHF-tau and neurofibrillary tangles are correlated with the cognitive decline seen in neurodegenerative diseases, such as dementia, Alzheimer disease (AD) and chemotherapy-induced cognitive impairment (CICI).
flotetuzumab: An anti-CD123/anti-CD3 bispecific humanized monoclonal antibody with potential immunostimulatory and antineoplastic activities. Flotetuzumab possesses two antigen-recognition and binding sites, one for the CD3 complex, a group of T-cell surface glycoproteins that complex with the T-cell receptor (TCR), and one for CD123, a tumor-associated antigen (TAA) overexpressed on the surface of certain tumor cells. Upon administration of flotetuzumab, this bispecific antibody simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This may result in potent CTL-mediated cell lysis of CD123-expressing tumor cells. CD123, the interleukin-3 receptor alpha chain, is overexpressed in a variety of hematological malignancies; its expression is low or absent in normal hematopoietic progenitors and stem cells.
flouride F 18 fluoropivalate: A radioconjugate composed of fluoropivalate, a non-natural short-chain fatty acid (SCFA), labeled with the positron-emitting radioisotope fluorine F 18, with potential use as an imaging agent for tracing SCFA metabolism upon positron emitting tomography (PET)/computed tomography (CT). Upon administration, fluorine F 18 FPIA is rapidly taken up by tumor cells. This may allow for the visualization of tumor cells upon PET/CT. SCFA is used as an energy source for cell growth and proliferation; tumor cells take up SCFAs at a much higher rate than normal, healthy cells due to their increased energy demand to allow for rapid tumor cell proliferation.
Flovent: (Other name for: fluticasone propionate)
floxuridine: A fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP) with antineoplastic activity. As an antimetabolite, floxuridine inhibits thymidylate synthetase, 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.
FLT3 agonist-Fc fusion protein GS-3583: A fusion protein composed of fms-related tyrosine kinase 3 ligand (FLT3L) and agonist fused to an immunoglobulin (Ig) fragment crystallizable region (Fc region), with potential immunostimulating activity. Upon administration of the FLT3 agonist-Fc fusion protein GS-3583, the FLT3 agonist moiety specifically targets, binds to, and activates FLT3 and, synergistically with other growth factors, stimulates the proliferation and mobilization of bone marrow precursor cells, including CD34+ cells, and dendritic cells (DCs). FLT3 agonist-Fc fusion protein GS-3583 has a longer serum half-life compared with soluble FLT3L.
FLT3 inhibitor BMF-500: An orally bioavailable, covalent and selective inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration, FLT3 inhibitor BMF-500 selectively targets and irreversibly binds to a reactive cysteine in the active site of FLT3. This inhibits the activity of FLT3 and prevents FLT3-mediated downstream signaling. This inhibits the proliferation of FLT3-expressing cancer cells. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.
FLT3 inhibitor FF-10101 succinate: The succinate salt form of FF-10101, a FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) inhibitor, with potential antineoplastic activity. Upon administration of FLT3 inhibitor FF-10101 succinate (FF-10101-01), FF-10101 irreversibly binds to and inhibits the activity of FLT3. This inhibits the proliferation of FLT3-expressing cancer cells. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.
FLT3 inhibitor HM43239: A selective, reversible type I inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) with potential antineoplastic activity. Upon administration of FLT3 inhibitor HM43239, it reversibly binds to and inhibits the activity of FLT3. This inhibits the proliferation of FLT3-expressing cancer cells. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.
FLT3 inhibitor XY0206: A selective inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) with potential antineoplastic activity. Upon administration, FLT3 inhibitor XY0206 targets, binds to and inhibits the activity of FLT3. This inhibits the proliferation of FLT3-expressing cancer cells. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias.
Flt3 ligand/anti-CTLA-4 antibody/IL-12 engineered oncolytic Vaccinia virus RIVAL-01: An oncolytic vaccinia virus (VV; VACV) genetically engineered to express an Fms-like tyrosine kinase 3 (Flt3) ligand, an antibody directed against the human T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) and the human pro-inflammatory cytokine interleukin-12 (IL-12), with potential immunomodulating and antineoplastic activities. Upon administration of the Flt3 ligand/anti-CTLA-4 antibody/IL-12 engineered oncolytic VV RIVAL-01, the virus preferentially targets, infects and replicates in tumor cells, causing oncolysis. In turn, the lysed tumor cells release various tumor-associated antigens (TAAs), which induce an immune response against the tumor cells. In addition, the Flt3 ligand, the anti-ctla-4 antibody and IL-12 are expressed by the VV in the cancer cells and may activate the immune system within the tumor microenvironment (TME), thereby stimulating both innate and adaptive immune responses. The anti-CTLA-4 antibody 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. Flt3 ligand binds to the Flt3 tyrosine kinase receptor and promotes Flt3 signaling which plays an important role in expanding the population of antigen-presenting dendritic cells (DCs). IL-12 activates natural killer cells (NKs), induces the secretion of interferon-gamma and promotes CD8 cytotoxic T-cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation.
FLT3 tyrosine kinase inhibitor TTT-3002: An orally bioavailable indolocarbazole derivative and inhibitor of constitutively active mutant forms of FMS-like tyrosine kinase 3 (FLT3) with potential antineoplastic activity. Following administration, FLT3 tyrosine kinase inhibitor TTT-3002 binds to and inhibits ligand-dependent dimerization and autophosphorylation of mutant forms of FLT3 with constitutively activating mutations, including FLT3 internal tandem duplication (FLT3/ITD) and the activating point mutation D835Y. Prevention of autophosphorylation inhibits uncontrolled FLT3 signaling and may result in the inhibition of proliferation in tumor cells expressing constitutively active mutant forms of FLT3. The ability of TTT-3002 to inhibit FLT3 proteins with activating point mutations may result in increased efficacy because the activity of these mutants are resistant to other FLT3 kinase inhibitors. FLT3, a tyrosine kinase receptor, plays a role in the regulation of hematopoietic progenitor cell proliferation, and in leukemic cell proliferation and survival. Constitutively activating mutations of FLT3 are the most frequent genetic alterations in acute myeloid leukemia.
FLT3/ABL/Aurora kinase inhibitor KW-2449: An orally available inhibitor of FMS-related tyrosine kinase 3 (FLT3, STK1, or FLK2), the tyrosine kinase ABL, and aurora kinases, with potential antineoplastic activity. Upon administration, FLT3/ABL/Aurora kinase inhibitor KW-2449 specifically binds to and inhibits both wild-type and mutated forms of FLT3, ABL and aurora kinases, which both interferes with the activation of signal transduction pathways mediated by these kinases and reduces the proliferation of susceptible cancer cells. FLT3 and ABL kinases are upregulated in certain tumor cells and play important roles in tumor cell proliferation and metastasis. Aurora kinases, serine-threonine kinases overexpressed by a wide variety of cancer cell types, play essential roles in mitotic checkpoint control.
FLT3/CDK4/6 inhibitor FLX925: An orally available inhibitor of FMS-related tyrosine kinase 3 (FLT3, STK1, or FLK2) and the cyclin-dependent kinases 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon administration, FLT3/CDK4/6 inhibitor FLX925 specifically binds to and inhibits FLT3, which interferes with the activation of FLT3-mediated signal transduction pathways and reduces cell proliferation in cancer cells that overexpress FLT3. In addition FLX925 inhibits CDK4 and 6 and prevents the phosphorylation of retinoblastoma (Rb) protein in early G1 phase. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, which causes G1 phase cell cycle arrest, suppresses DNA synthesis and inhibits cancer cell growth. FLT3, a class III tyrosine kinase receptor, is overexpressed in a variety of cancers. Overexpression of CDK4/6, which is seen in certain types of cancer, causes cell cycle deregulation.
FLT3/FGFR dual kinase inhibitor MAX-40279: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) and FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon oral administration of FLT3/FGFR dual kinase inhibitor MAX-40279, this agent binds to and inhibits both FGFR and FLT3, including FLT3 mutant forms, which results in the inhibition of FGFR/FLT3-mediated signal transduction pathways. This inhibits proliferation in FGFR/FLT3-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases, is upregulated in many tumor cell types. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. They both play key roles in cellular proliferation and survival.
FLT3/KIT kinase inhibitor AKN-028: An orally bioavailable protein tyrosine kinase inhibitor for FMS-related tyrosine kinase 3 (FLT3; STK1) and stem cell factor receptor (SCFR; KIT), with potential antineoplastic activity. FLT3/KIT kinase inhibitor AKN-028 binds to and inhibits both the wild-type and mutated forms of FLT3 and SCFR. This may result in an inhibition of tumor cell proliferation in cancer cell types that overexpress these receptor tyrosine kinases.
FLT3/KIT/CSF1R inhibitor NMS-03592088: An orally bioavailable inhibitor of the receptor tyrosine kinases FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), the mast/stem cell factor receptor c-Kit (SCFR; KIT) and colony stimulating factor 1 receptor (CSF1R; CSF-1R; C-FMS; CD115; M-CSFR), with potential antineoplastic and immunomodulating activities Upon administration, FLT3/KIT/CSF1R inhibitor NMS-03592088 binds to and inhibits the activity of FLT3, KIT and CSF1R. This prevents FLT3, KIT and CSF1R-mediated signaling and results in the inhibition of proliferation in tumor cells overexpressing FLT3, KIT and CSF1R. In addition, NMS-03592088 binds to CSF1R expressed on monocytes, macrophages, and osteoclasts and inhibits the binding of the CSF1R ligands colony-stimulating factor-1 (CSF-1) and interleukin-34 (IL-34), to CSF1R. This prevents CSF1R activation and CSF1R-mediated signaling in these cells. This blocks the production of inflammatory mediators by macrophages and monocytes and reduces inflammation. By blocking the recruitment to the tumor microenvironment and activity of CSF1R-dependent tumor-associated macrophages (TAMs), NMS-03592088 inhibits the immunomodulating activity by macrophages and enhances T-cell infiltration and antitumor T-cell immune responses, which inhibits the proliferation of tumor cells. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B lineage neoplasms and in acute myeloid leukemia (AML), and plays a key role in tumor cell proliferation. c-Kit, a transmembrane protein and receptor tyrosine kinase, is overexpressed in solid tumors and hematological malignancies; it plays a key role in the regulation of cell differentiation and proliferation. CSF1R, also known as macrophage colony-stimulating factor receptor (M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface receptor for its ligand colony stimulating factor 1 (CSF1) and plays major roles in tumor cell proliferation and metastasis.
FLT3/KIT/VEGFR2/PDGFRB inhibitor ETN101: An orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), mast/stem cell factor receptor c-Kit (SCFR; KIT), vascular endothelial growth factor receptor type 2 (VEGFR2) and platelet-derived growth factor receptor beta (PDGFRB), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, FLT3/KIT/VEGFR2/PDGFRB inhibitor ETN101 targets, binds to and inhibits the activity of FLT3, c-Kit, VEGFR2 and PDGFRB. This prevents FLT3, c-Kit, VEGFR2 and PDGFRB-mediated signaling and the activation of downstream signaling pathways. By inhibiting multiple RTKs, ETN101 may be able to inhibit angiogenesis and tumor cell invasion, normalize abnormal blood vessels, and reverse the immunosuppressive state of the tumor microenvironment (TME). This may halt tumor cell proliferation in susceptible tumor cells. FLT3, c-Kit, VEGFR2, and PDGFRB are upregulated in a variety of cancer cell types and play key roles in tumor cell proliferation, angiogenesis, and metastasis.
Flt3/MerTK inhibitor MRX-2843: An orally bioavailable inhibitor of two receptor tyrosine kinases (RTKs), FMS-like tyrosine kinase-3 (Flt3; CD135; fetal liver kinase-2; Flk2) and tyrosine-protein kinase Mer (MerTK; proto-oncogene c-Mer; Mer), with potential antineoplastic activity. Upon administration, MRX-2843 targets and binds to both Flt3 and MerTK. This prevents ligand-dependent phosphorylation and activation of Flt3 and MerTK, which inhibits the activation of their downstream signaling pathways. This induces apoptosis and inhibits proliferation of Flt3- and/or MerTK-overexpressing tumor cells. Flt3 and MerTK, are overexpressed in certain tumor cell types and play key roles in tumor cell proliferation and survival.
flu matrix peptide p58-66: A short chain synthetic antigenic peptide (GILGFVFTL) derived from the influenza virus A matrix protein and presented by HLA-A2 major histocompatibility complex (MHC) class I molecules. Flu matrix peptide p58-66 stimulates the lytic functions of cytotoxic T lymphocytes (CTLs), which may result in the eradication of virus-infected or malignant tumor cells.
Fluarix: (Other name for: trivalent influenza vaccine)
Flublok: (Other name for: trivalent influenza vaccine)
fluciclatide F 18: A radiopharmaceutical compound of a small synthetic cyclic peptide containing an RGD-sequence (Arg-Gly-Asp) labeled with the positron-emitting isotope fluorine F 18 that may be used to selectively image tumor cells and tumor vasculature by PET imaging. The RGD motif of fluciclatide F 18 selectively binds to the alphaVbeta3 integrin receptor, commonly upregulated on the surfaces of tumor cells and endothelial cells of tumor vasculature. This agent may be of use in visualizing and quantifying the development of tumor vascularity in response to antiangiogenic agents.
fluciclovine F18: A radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with potential diagnostic imaging use. Similar to most amino acids, fluciclovine F18 appears to enter cells through the energy-independent L-type amino acid transporter (LAT) system. As an amino acid analogue, this agent is preferentially accumulated by tumor cells due to their increased metabolic needs; however, unlike naturally occurring amino acids, this non-natural amino acid-analogue radiotracer is not metabolized. Accordingly, fluciclovine F18 accumulates in tumor cells and can potentially be used to image tumors using positron emission tomography (PET).
fluconazole: A synthetic triazole with antifungal activity. Fluconazole preferentially inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols, the loss of normal fungal sterols, and fungistatic activity. Mammalian cell demethylation is much less sensitive to fluconazole inhibition.
flucytosine: A pyrimidine compound and a fluorinated cytosine analog exhibiting antifungal activity. After penetration into the fungal cells, flucytosine is deaminated to its active metabolite 5-fluorouracil. 5-fluorouracil replaces uracil during fungal RNA synthesis, thereby inhibiting fungal protein synthesis. In addition, fluorouracil is further metabolized to 5-fluorodeoxyuridylic acid monophosphate, which inhibits thymidylate synthetase, thereby interrupting nucleotide metabolism, DNA synthesis and ultimately protein synthesis.
fludarabine phosphate: The phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.
Fludase: (Other name for: recombinant cell-surface anchored sialidase DAS181)
fludeoxyglucose F 18: A positron-emitting radiopharmaceutical containing radioactive 2-deoxy-2-[18F] fluoro-D-glucose. With similar cell uptake as glucose (high in tumor cells), fludeoxyglucose F 18 is not dephosphorylated and further metabolized.
fludrocortisone acetate: The acetate salt of a synthetic fluorinated corticosteroid with antiinflammatory and antiallergic activities. As a glucocorticoid-receptor agonist, fludrocortisone binds to cytoplasmic receptors, translocates to the nucleus, and subsequently initiates the transcription of glucocorticoid-responsive genes such as lipocortins to inhibit phospholipase A2 (PLA2). Inhibition of PLA2 activity prevents the release of arachidonic acid, a precursor of eicosanoids such as prostaglandins and leukotrienes; eicosanoids are important mediators in the pro-inflammatory response mechanism. As a mineralocorticoid-receptor agonist, this agent stimulates Na+ reabsorption and water retention and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney.
FluLaval: (Other name for: trivalent influenza vaccine)
flumatinib mesylate: The orally bioavailable, mesylate salt form of the tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity. Upon administration, flumatinib inhibits the wild-type forms of Bcr-Abl, platelet-derived growth factor receptor (PDGFR) and mast/stem cell growth factor receptor (SCFR; c-Kit) and forms of these proteins with certain point mutations. This results in the inhibition of both Bcr-Abl-, PDGFR- and c-Kit-mediated signal transduction pathways, and the proliferation of tumor cells in which these kinases are overexpressed. Bcr-Abl fusion protein is an abnormal, constitutively active enzyme expressed in Philadelphia chromosome positive chronic myeloid leukemia (CML), acute lymphoblastic leukemia (ALL) or acute myelogenous leukemia (AML). PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. c-kit, a receptor tyrosine kinase mutated and constitutively activated in certain tumors, plays a key role in tumor cell survival, proliferation, and differentiation.
FluMist: (Other name for: trivalent live-attenuated influenza vaccine)
fluocinolone acetonide: The acetonide salt form of fluocinolone, a synthetic fluorinated corticosteroid with antiinflammatory, antipruritic and vasoconstrictive properties. Fluocinolone is a glucocorticoid receptor agonist that binds to cytoplasmic glucocorticoid receptors and subsequently translocates to the nucleus where it initiates the transcription of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both are potent mediators of inflammation. Fluocinolone exerts its vasoconstrictive effect through inhibition of nitric oxide synthase, thereby blocking nitric oxide production and effectively diminishing the effect of nitric oxide on vascular smooth muscles leading to reduced blood flow.
fluocinonide cream: A topical cream containing the synthetic glucocorticoid fluocinonide, with anti-inflammatory and antipruritic activities. Upon administration of the fluocinonide cream to the affected area(s), fluocinonide binds to the cytosolic glucocorticoid receptor, followed by translocation of the ligand-receptor complex to the nucleus and transcription activation of genes containing glucocorticoid-responsive elements (GREs), which increases the expression of specific target genes, such as lipocortin-1 (annexin A1). The induction of lipocortin-1 expression by fluocinonide leads to an increased interaction and inhibition of cytosolic phospholipase 2 alpha, thereby preventing phospholipase translocation to the perinuclear membrane and subsequent release and conversion of arachidonic acid to inflammatory prostaglandins and leukotrienes. This may relieve symptoms associated with skin inflammation.
fluorescein sodium injection: An injectable form of the sodium salt of the fluorophore fluorescein. Fluorescein responds to electromagnetic radiation between the wavelengths of 465-490 nm and fluoresces, emitting light at wavelengths of 520-530 nm that can be detected visually.
fluorescein-conjugated Wisteria floribunda lectin: A fluorescein conjugated to a preparation of lectin(s) extracted from the seeds of Wisteria floribunda (Japanese wisteria), with potential use as a diagnostic agent. Upon administration of fluorescein-conjugated Wisteria floribunda lectin, the lectin moiety preferentially targets and binds to carbohydrate structures containing N-acetylgalactosamine and galactose residues overexpressed on certain tumor cell surfaces. Using white and fluorescent light, tumor cells with increased lectin-binding affinity can be visualized or imaged.
fluorescence imaging agent EMI-137: A water-soluble compound composed of a 26-amino acid cyclic peptide targeting the human hepatocyte growth factor receptor (c-MET) conjugated to a cyanine-based fluorescent dye, with potential fluorescent imaging activity. Upon administration of EMI-137, the peptide moiety specifically targets and binds to the human tyrosine kinase receptor c-Met, which is often overexpressed on cancer cells. Upon imaging, the cancer cells can be visualized.
fluorescent antibody SGM-101: A near infrared-emitting fluorochrome-labeled anti-carcinoembryonic antigen (ACE; anti-CEA) monoclonal antibody, with potential diagnostic imaging activity. Upon administration, the fluorescent antibody SGM-101 binds CEA-overexpressing cancer cells. Upon fluorescence imaging, the fluorochrome can be visualized and CEA-overexpressing cancer cell can be imaged and detected. CEA, a tumor-associated antigen (TAA), is overexpressed on the surface of tumor cells.
fluorescent cRGDY PEG-Cy5.5 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, with potential use as a tumor-selective fluorescent imaging agent. Upon intradermal administration of the fluorescent cRGDY PEG-Cy5.5 C dots, the cRGD moiety selectively binds to alphaVbeta3 integrin expressed on tumor cells. Upon intraoperative fluorescence imaging, alphaVbeta3-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.
fluorescent dye LS301: A hydrophobic near-infrared (NIR) fluorescent probe composed of a NIR fluorescent dye cypate linked to an unnatural D-cysteine-containing cyclic octapeptide (D-Cys-Gly-Arg--Asp-Ser-Pro-Cys)-Lys-OH, with potential cancer-imaging activity. Upon administration during tumor resection, the peptide component of LS301 specifically targets and binds integrin receptors expressed on tumor cells, which are not expressed on normal, healthy cells. Upon receptor-mediated endocytosis and fluorescence imaging using infrared light that is visualized by the surgeon with special Cancer Vision Goggles (CVG), tumor cells can be detected, identified, and removed accordingly. This enhances the accuracy of cancer cell removal during surgery. The D-cysteine on the peptide prevents degradation by endogenous proteases.
fluorescent imaging agent cRGD-ZW800-1: An imaging agent composed of the cyclic arginine-glycine-aspartic acid (cRGD)-based peptide derivative cyclo-(RGDyK) conjugated to the near-infrared (NIR) fluorophore ZW800-1, with potential use as a tumor-selective fluorescent imaging agent. Upon administration of the fluorescent imaging agent cRGD-ZW800-1, the cRGD moiety selectively binds to integrins, including alphaVbeta3, alphaVbeta5 and alphaVbeta6, expressed on tumor cells and tumor-associated vascular endothelium. Upon intraoperative fluorescence imaging, tumor cells and tumor-associated vascular endothelium expressing these integrins can be visualized. 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.
fluorescent imaging ligand OTL38: A fluorescent imaging agent composed of a folate receptor-alpha (FRa)-targeting ligand conjugated to a fluorescent near infrared (NIR) dye, that can be used for imaging of FRa-expressing tumor cells. Upon administration, the FRa-targeting moiety of OTL38 specifically binds to FRa expressed on tumor cells thus selectively delivering the fluorescent dye to FRa-expressing tumor cells. Upon NIR imaging, tumor cells fluoresce, which allows for the visualization and identification of FRa-overexpressing tumor cells. FRa, a high-affinity folate-binding protein and a member of the folate receptor family, is overexpressed in various cancer cell types.
fluorescent protease-activated peptide AVB-620: A protease-cleavable peptide linked to a fluorescent probe, with potential imaging activity. Upon intravenous infusion of the fluorescent protease-activated peptide AVB-620 before surgery, the peptide moiety of AVB-620 can be cleaved by proteases overexpressed by tumor cells. This activates the fluorescent probe and the tumor cells expressing the proteases can be detected using a fluorescence imaging system. This allows for the visualization and removal of the tumor during surgery.
Fluorescite: (Other name for: fluorescein sodium injection)
fluorine 18 F-fludarabine: A radiopharmaceutical containing the purine analog fludarabine that is labeled with the radioisotope fluorine F18 with potential use as a tumor imaging agent upon positron emission tomography (PET). After intravenous administration, the fludarabine is selectively taken up by tumor cells. The radioisotope moiety is detected using PET, which allows imaging and quantification of both the biodistribution of fludarabine and the presence of tumor cells. This could identify tumors and select patients that will likely respond to fludarabine treatment.
fluorine F 18 3F-PHPG: A radioconjugate containing a substrate of the norepinephrine transporter (NET), chromaffin granule amine transporter (CGAT; vesicular monoamine transporter 1; VMAT1; VAT1; solute carrier family 18 member 1; SLC18A1) and synaptic vesicular amine transporter (SVAT; vesicular monoamine transporter 2; VMAT2; VAT2; solute carrier family 18 member 2; SLC18A2) labeled with the positron-emitting radioisotope fluorine F 18, with potential diagnostic imaging applications upon positron emitting tomography (PET)/computed tomography (CT). Upon administration, fluorine F 18 3F-PHPG is taken up by NET, VMAT1 and VMAT2 and accumulates in adrenergic tissues. This may allow for the visualization of tumors expressing these transporters upon PET/CT. NET, VMAT1 and/or VMAT2 are expressed in some adrenergic tumors.
fluorine F 18 4-fluoro-1-naphthol: A radioconjugate composed of a myeloperoxidase (MPO) activity tracer labeled with fluorine F 18, with potential use for imaging of MPO activity and areas of inflammation using positron emission tomography (PET). Upon administration of fluorine F 18 4-fluoro-1-naphthol, the 4-fluoro-1-naphthol moiety selectively binds to nearby proteins and cells when they are oxidized by MPO plus hydrogen peroxide, but not hydrogen peroxide alone. This allows the visualization of MPO activity using PET. MPO is one of the key effector molecules and enzymes of innate immunity.
fluorine F 18 alphaVbeta6-binding peptide: A radiotracer composed of a 20 amino acid peptide derived from the GH loop of an envelope protein (VP1) of the foot-and-mouth disease virus (FMDV), where the N-terminal lysine has been substituted with arginine, conjugated with two polyethylene glycol units and radiolabeled with fluorine 18, for potential positron emission tomography (PET) imaging of alphaVbeta6 integrin expression. Upon administration, the arginine-glycine-aspartic acid (RGD) motif within the peptide moiety of the fluorine 18 F-alphaVbeta6-binding peptide selectively binds to alphaVbeta6 integrin. During PET imaging, alphaVbeta6-expressing tumor cells can be visualized and the degree of tumor growth can be determined. AlphaVbeta6 integrin, a cell adhesion and signaling receptor, is upregulated in certain cancers and has been associated with proliferation, migration and invasion of tumor cells.
fluorine F 18 boronophenylalanine: A radioconjugate composed of boronophenylalanine (BPA) labeled with the positron-emitting isotope fluorine F 18, with potential imaging applications upon positron emission tomography (PET). Upon administration, fluorine F 18 BPA is selectively taken up by tumor cells. Upon PET, fluorine F 18 can be detected, which allows the imaging of the tumor cells.
fluorine F 18 C-SNAT4: A radiotracer composed of C-SNAT4 radiolabeled with the radioisotope fluorine F 18, with potential tumor imaging activity upon positron emission topography (PET)/computed tomography (CT). Upon administration, the C-SNAT4 moiety of fluorine F 18 C-SNAT4 selectively targets and binds to a tumor-associated antigen (TAA) on the tumor cell. During PET/CT, TAA-expressing tumor cells can be visualized.
fluorine F 18 choline: A radioconjugate composed of choline labeled with the positron-emitting isotope fluorine F 18, with potential tumor tracer activity using positron emission tomography (PET). Fluorine F 18 fluorocholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, that is integrated into the cell membrane as part of phosphatidylcholine. Since the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of fluorine F 18 fluorocholine uptake and incorporation, facilitating imaging of the tumor using PET. Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently upregulated in human tumor cells. Choline is essential for the production of phosphatidylcholine, which is an important element of phospholipids in cell membranes.
fluorine F 18 clofarabine: A radioconjugate composed of the nucleoside analog and deoxycytidine kinase (DCK)-dependent pro-drug clofarabine (Cl-F-ara-A) linked to the radioisotope fluorine F 18, with potential imaging activity using positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18 clofarabine, the clofarabine moiety is preferentially taken up by and accumulates in cells with dysregulated nucleoside metabolism, including tumor cells expressing high levels of DCK. The clofarabine moiety is phosphorylated by DCK into its active triphosphate form, Cl-F-ara-ATP. The 18F moiety can be visualized by PET imaging. As many nucleoside analog prodrugs are chemotherapeutic agents that require DCK for their phosphorylation and activation, fluorine F 18 clofarabine can potentially be used as a marker to measure DCK activity and to predict the chemotherapeutic efficacy of DCK-dependent prodrugs. DCK, a rate-limiting enzyme in the deoxyribonucleoside salvage pathway for DNA synthesis, is overexpressed in certain solid tumors, lymphoid and myeloid malignancies and certain immune cells, such as proliferating T-lymphocytes. Compared to other nucleoside analogs, clofarabine is not susceptible to deamination by cytidine deaminase (CDA).
fluorine F 18 CP18 peptide: A triazole containing pentapeptide labeled with the positron-emitting isotope fluorine F 18, used as a tracer for positron emitting tomography (PET) imaging. As a caspase-3 specific substrate, fluorine F 18 CP18 peptide is preferentially taken up by and accumulates in tumor cells with high caspase-3 activity. Upon PET imaging, apoptotic cells can be detected and apoptotic activity can be assessed. Caspase-3 is a cysteine protease that plays a key role in the induction of apoptosis.
fluorine F 18 d-FMAU: A radioconjugate comprised of the synthetic pyrimidine analogue 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)thymine (d-FMAU) labeled with the radioisotope fluorine F 18 (18F-d-FMAU), that can potentially be used as an imaging agent upon positron emission tomography (PET). Upon administration, fluorine F 18 d-FMAU is distributed and taken up by cells based on the rate of the cell’s DNA synthesis. Upon PET imaging, cell proliferation in tumors can be assessed as tumor cells have a higher rate of DNA synthesis than normal, healthy cells. This agent is not catabolized and has a long half-life compared to the radioconjugate carbon C 11 thymidine.
fluorine F 18 dabrafenib: A radioconjugate containing dabrafenib, a tyrosine kinase inhibitor of the V600 mutated version of the B-raf (BRAF) protein and labeled with the positron-emitting isotope fluorine F 18 with potential prostate tumor imaging upon positron emission tomography (PET). Upon administration, the dabrafenib moiety of fluorine F 18 dabrafenib specifically targets and binds to the BRAF V600-mutated form, expressed on tumor cells, thereby allowing the visualization of tumor cells expressing BRAF V600 upon PET. BRAF is constitutively activated in a variety of cancers due to BRAF gene mutations.
fluorine F 18 DASA-23: A radiotracer composed of DASA-23, a pyruvate kinase isoform M2 (PKM2) ligand, conjugated to the radioisotope fluorine F 18, with potential use for imaging of PKM2-expressing tumor cells upon positron emission tomography (PET). Upon administration of fluorine F 18 DASA-23, the DASA-23 moiety selectively targets and is taken up by tumor cells that express PKM2. Upon binding to PKM2 and following PET, PKM2-expressing tumor cells can be visualized and the metabolic activity of the tumor cells can be assessed through the quantitation of PKM2 expression levels. PKM2, an enzyme that plays a key role in the glycolytic reprogramming, metabolic activity and rapid proliferation of tumor cells, is selectively overexpressed in various tumor cell types. Tumor uptake of fluorine F 18 DASA-23 is positively correlated with PKM2 expression.
fluorine F 18 dasatinib: A radioconjugate composed of a derivative of the multi-targeted kinase inhibitor dasatinib conjugated to the radioisotope fluorine F 18, with potential imaging activity during positron emission tomography (PET). Upon administration of fluorine F 18 dasatinib, dasatinib targets and binds to Bcr/Abl, SRC-family protein-tyrosine kinases, c-Kit and platelet-derived growth factor receptor (PDGFR). Upon binding, the fluorine F 18 moiety allows PET imaging of tumor cells and can be used as a tracer for the biodistribution of dasatinib.
fluorine F 18 DCFBC: A radioconjugate containing a low molecular weight tracer, DCFBC, specific for prostate-specific membrane antigen (PSMA) and labeled with the positron-emitting isotope fluorine F 18 with potential prostate tumor imaging upon positron emission tomography (PET). Upon administration, the DCFBC moiety of fluorine F 18 DCFBC specifically targets and binds to the tumor associated antigen PSMA, thereby allowing the visualization of tumor cells expressing PSMA upon PET. PSMA is a transmembrane glycoprotein highly expressed on malignant prostate epithelial cells and vascular endothelial cells of various solid tumors.
fluorine F 18 EF5: A radioconjugate consisting of EF5, a fluorinated derivative of etanidazole, conjugated to fluorine F 18, a positron emitting isotope. EF5 binds to hypoxic tissue; conjugation to Fluorine F 18 allows imaging of hypoxic regions within tumors.
fluorine F 18 FAPI-74: A radioconjugate composed of FAPI-74, a quinoline-based fibroblast activation protein (FAP)-targeted tracer belonging to the group of FAP inhibitors (FAPi) conjugated to the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and labeled with the positron-emitting radioisotope fluorine F 18, with potential use as a tracer for FAP-expressing tumors and cancer-associated fibroblasts (CAFs) during positron emission tomography (PET). Upon administration of fluorine F 18 FAPI-74, the FAPI-74 moiety targets and binds to FAP-expressing tumor cells and FAP-expressing CAFs. Upon binding and internalization, FAP-expressing tumor cells and CAFs can be detected during PET imaging. FAP, a cell surface protein, is overexpressed in a variety of human cancer cell types and on CAFs in the tumor microenvironment (TME).
fluorine F 18 FDHT: A radioconjugate containing a derivative of the androgen testosterone, 16-beta-fluoro-5-alpha-dihydrotestosterone (FDHT), labeled with the radioisotope fluorine F18 (18F-FDHT), with potential use as an imaging agent for positron emission tomography (PET). Upon administration, 18F-FDHT binds to the androgen receptor (AR). Upon PET imaging, AR-expressing prostate tumor cells can be imaged and assessed.
fluorine F 18 FEQA: The anilinoquinazoline derivative FEQA radiolabeled with the positron-emitting radioisotope fluorine F 18 with epidermal growth factor receptor (EGFR) binding and radioisotopic activities. Fluorine F 18 FEQA irreversibly binds to (EGFR), allowing imaging of EGFR-positive tumor cells with positron emission tomography (PET).
fluorine F 18 florastamin: A radioconjugate composed of the human prostate-specific membrane antigen (PSMA)-targeting ligand, florastamin, labeled with the radioisotope fluorine F 18, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18 florastamin, the florastamin moiety targets and binds to PSMA-expressing tumor cells. Upon binding, PSMA-expressing tumor cells can be detected during PET/CT imaging. 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.
fluorine F 18 florbetapir: A radioconjugate composed of florbetapir, an amyloid-binding ligand, labeled with the positron-emitting isotope fluorine F 18, that may be used for positron emission tomography (PET) detection of beta-amyloid neuritic plaques. Upon administration, fluorine F 18 florbetapir targets and binds to beta-amyloid neuritic plaques. Upon PET, amyloid neuritic plaques can be visualized, and the amount of amyloid neuritic plaque present may be indicative of Alzheimer's disease (AD) or other types of neurologic conditions.
fluorine F 18 florilglutamic acid: A radioconjugate composed of the radionuclide fluorine F 18 conjugated to the florilglutamic acid that targets the cystine/glutamate transporter protein (xCT or SLC7A11), which is a subunit of the transport system xc(-), with potential imaging activity upon positron emission tomography (PET). Upon intravenous administration, fluorine F 18 florilglutamic acid specifically binds to xCT and is subsequently taken up by the cell via xc(-). Upon uptake, xc(-) activity can be assessed and tumor cells can be detected and imaged by PET. System xc(-), a sodium-independent, heterodimeric transporter, mediates the cellular uptake of cystine in exchange for intracellular glutamate at the plasma membrane; although, it will take up glutamate as well. Xc(-) shows increased activity in certain tumor cells compared to normal, healthy cells due to increased metabolic activity in tumor cells; it plays a key role in tumor cell proliferation, progression and chemoresistance as well as in the management of oxidative stress.
fluorine F 18 fluoro furanyl norprogesterone: The progesterone derivative fluoro furanyl norprogesterone (FFNP), radiolabeled with fluorine F 18, with positron-emitting radioligand activity. Upon injection, fluorine F 18 fluoro furanyl norprogesterone (F18-FFNP) binds to progesterone receptors (PgR) in progesterone-responsive tissues. In PgR-positive breast cancer, positron emission tomography (PET) may then be used to quantitate hormone receptor status.
fluorine F 18 fluoro-PEG6-IPQA: A radioconjugate containing the tracer PEG6-IPQA labeled with fluorine F 18 for potential tumor imaging using positron emission tomography (PET). Upon administration, the IPQA moiety of fluorine F 18 fluoro-PEG6-IPQA selectively targets and irreversibly binds to the constitutively active mutant L858R of epidermal growth factor receptor (EGFR) kinase, thereby allowing the visualization of tumor cells expressing the active mutant L858R EGFR using PET. This can be used to select EGFR kinase inhibitors that bind in a similar manner as this tracer and may allow individualized therapy for patients that respond well to these types of EGFR kinase inhibitors. The presence of the L858R EGFR mutation in non small cell lung cancer (NSCLC) cells is correlated with a better response to EGFR kinase inhibitors compared to wild-type (WT) or L858R/T790M EGFR dual-mutant.
fluorine F 18 fluorobenzyl triphenyl phosphonium: A radioconjugate and cationic lipophilic agent consisting of fluorobenzyl triphenyl phosphonium (FBnTP), labeled with the radioisotope fluorine F 18, with potential use as a tracer for both mitochondrial membrane potential (MMP) and apoptosis, and as a tumor imaging agent using positron emission tomography (PET). Upon administration, fluorine F 18 FBnTP is taken up by cells and its uptake and accumulation within mitochondria is directly correlated with MMP. Apoptosis causes a loss of membrane potential across the inner mitochondrial membrane which decreases FBnTP mitochondrial uptake. As apoptosis is suppressed in tumor cells, the FBnTP uptake is increased as compared to normal cells. This allows, upon PET, for the imaging of cancer cells. As apoptosis-inducing chemotherapeutic agents cause a collapse of MMP, this agent can also be used to assess the response of tumor cells to those chemotherapeutic agents.
fluorine F 18 fluoroethylcholine: Ethylcholine labeled with fluorine F 18, a positron-emitting isotope. Fluorine F 18 fluoroethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, and finally is integrated into cellular phospholipids, probably primarily into a phosphatidyl derivative; concentration of this agent in tumor cells as various fluorine F 18 fluoroethylcholine derivatives enables tumor imaging using positron emission tomography (PET). Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently up-regulated in human tumor cell lines.
fluorine F 18 fluoromethylcholine: A radiotracer consisting of methylcholine labeled with the positron-emitting radioisotope fluorine F 18 (18F-FMCH) with potential imaging use. Upon administration, 18F-fluoromethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, an enzyme frequently upregulated in human tumors, yielding phosphoryl 18F-fluoromethylcholine. In turn, phosphoryl 18F-fluoromethylcholine is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. As the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of 18F-FMCH uptake and incorporation, allowing tumor imaging with positron emission tomography (PET).
fluorine F 18 fluoropaclitaxel: A radiotracer containing paclitaxel labeled with the radioisotope fluorine F 18 with potential use as an imaging agent. After cellular uptake, the paclitaxel moiety of fluorine F18 fluoropaclitaxel binds to tubulin. Upon uptake, the radioisotope moiety may be detected using positron emission tomography (PET), thereby allowing imaging and quantification of the biodistribution of paclitaxel. This could identify multidrug resistant (MDR) status of tumor cells and select patients that will likely respond to paclitaxel treatment.
fluorine F 18 fluorthanatrace: A radiotracer consisting of an analogue of the poly(ADP-ribose) polymerase 1 (PARP1) inhibitor rucaparib radiolabeled with the positron emitting isotope fluorine F 18, which can potentially be used for the imaging of PARP1 expression using positron emission tomography (PET). Upon administration, fluorine F 18 fluorthanatrace targets and binds to PARP1. Upon PET, PARP1-expressing tumor cells can be visualized. PARP1, which is overexpressed in many cancer cell types, catalyzes post-translational ADP-ribosylation of nuclear proteins and plays a key role in the repair of DNA strand breaks.
fluorine F 18 FMDHT: A radioconjugate containing a derivative of the androgen testosterone (FMDHT) and labeled with the radioisotope fluorine F 18, with potential use as an imaging agent for positron emission tomography (PET). Upon administration, fluorine F 18 FMDHT binds to the androgen receptor (AR). Upon PET imaging, AR-expressing prostate tumor cells can be imaged and assessed.
fluorine F 18 FP-R01-MG-F2: A radiotracer composed of the integrin alphaVbeta6 (aVb6) ligand and cystine knot peptide R01 variant R01-MG-F2 radiolabeled with [18F]-fluoropropionate (F 18 FP), with potential integrin aVb6 imaging activity using positron emission tomography (PET). Upon administration, the R01-MG-F2 moiety of fluorine F 18 FP-R01-MG-F2 selectively binds to integrin aVb6-positive cancer cells. During PET, aVb6-expressing tumor cells can be visualized. Integrin aVb6, a cell adhesion and signaling receptor, is upregulated in certain cancer cell types and has been associated with increased proliferation of tumor cells. The cystine knot peptide shows high stability and allows for rapid and high uptake into aVb6-expressing tumor cells.
fluorine F 18 FTC-146: A radioconjugate composed of the selective sigma-1 receptor (S1R) ligand FTC-146 labeled with the radionuclide fluorine F 18, with potential use as an imaging agent for S1R-expressing tumor cells upon positron emission tomography (PET)/computed tomography (CT). Upon administration, fluorine F 18 FTC-146 targets and selectively binds to S1R expressed on tumor cells. The S1R-expressing tumor cells can then be visualized using PET/CT. S1R, widely distributed in the central nervous system (CNS) and peripheral tissues, plays a key role in the modulation of ion channels and other neurotransmitter systems, and in restoring neuronal function. It is upregulated in inflammatory diseases and in a variety of cancers. 18F-FTC-146 shows excellent selectivity for the S1R over the sigma-2 receptor and vesicular acetylcholine transporter (VAChT).
fluorine F 18 galacto-RGD peptide: A radiotracer composed of a cyclic Arg-Gly-Asp (RGD) peptide that is conjugated with galactose and radiolabeled with fluorine 18, for potential noninvasive positron emission tomography (PET) imaging of alphaVbeta3 integrin expression. Upon administration, the RGD moiety of the fluorine 18 galacto-RGD peptide selectively binds to alphaVbeta3 integrin. During PET imaging, alphaVbeta3-expressing tumor cells can be visualized and the degree of tumor angiogenesis can be determined. Use of a hydrophilic glycopeptide-based agent may increase retention in the blood and reduce clearance by the liver. This leads to both increased uptake of fluorine 18 galacto-RGD peptide by tumor cells and enhanced PET imaging efficiency, when compared to other agents that are constructed using lipophilic conjugates. AlphaVbeta3 integrin, a cell adhesion and signaling receptor, is upregulated in tumor vessel endothelial cells and has been associated with proliferation of tumor cells, tumor angiogenesis and metastasis.
fluorine F 18 GEH121224: A radioconjugate composed of a human epidermal growth factor receptor 2 (HER2; ErbB2; HER-2)-targeting ligand labeled with the radioisotope fluorine F 18, with potential use as a tracer for HER2-expressing tumors during positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18 GEH121224, the HER2-targeting moiety targets and binds to HER2-expressing tumor cells. Upon binding, HER2-expressing tumor cells can be detected during PET/CT imaging. HER2, a tumor-associated antigen (TAA) overexpressed on a variety of tumor cell types, plays an important role in tumor cell proliferation, differentiation and survival.
fluorine F 18 integrin alpha v beta 6-targeted binding peptide: A radiotracer composed of an integrin alphaVbeta6 (aVb6) binding peptide (BP) radiolabeled with the radionuclide fluorine F 18, with potential integrin aVb6 imaging activity using positron emission tomography (PET). Upon administration, the fluorine F 18 integrin aVb6-targeted peptide selectively binds to integrin aVb6-positive cancer cells. During PET, aVb6-expressing tumor cells can be visualized and the degree of tumor growth can be determined. Integrin aVb6, a cell adhesion and signaling receptor, is upregulated in certain cancer cell types and has been associated with increased proliferation, migration and invasion of tumor cells.
Fluorine F 18 ISO-1: A radioconjugate consisting of the benzamide ligand ISO-1 labeled with the radioisotope fluorine F18 with positron-emitting radioisotope activity. Upon administration, fluorine [F18]ISO-1 binds to sigma-2 receptors, located on tumor cells, allowing visualization of sigma-2 receptor-expressing tumor cells with positron emission tomography (PET). Sigma-2 receptors, expressed in a variety of normal healthy tissues such as liver, kidneys, endocrine glands, and in the central nervous system, may be overexpressed in tumor cells.
fluorine F 18 LY3546117: A radioconjugate composed of the granzyme B-targeting agent LY3546117 labeled with the radionuclide fluorine F 18, with potential use as an imaging agent for granzyme B activity upon positron emission tomography (PET). Upon administration, fluorine F 18 LY3546117 targets and binds to granzyme B. Granzyme B activity can then be visualized using PET. Granzyme B plays a key role in cytotoxic T-lymphocyte (CTL)- and natural killer (NK) cell-mediated cytotoxicity of virus-infected cells and tumor cells.
fluorine F 18 NOS: A radiotracer composed of an analog of the reversible nitric oxide synthase (NOS) inhibitor, 2-amino 4-methylpyridine, radiolabeled with fluorine F 18, with potential imaging activity upon positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18 NOS, the NOS moiety targets and binds to inducible NOS (iNOS). Upon PET/CT imaging, iNOS expression and thus the extent of inflammation can be assessed. iNOS expression is upregulated in a variety of inflammatory diseases and certain cancers and may invoke a chronic inflammatory state in tumor cells.
fluorine F 18 ODS2004436: A radioconjugate containing the epidermal growth factor receptor (EGFR) kinase tracer ODS2004436 labeled with fluorine F 18 for potential tumor imaging using positron emission tomography (PET). Upon administration of fluorine F 18 ODS2004436, the ODS2004436 moiety selectively targets and binds to forms of EGFR that contain activating mutations. This allows the visualization of tumor cells expressing activating EGFR mutations using PET. This agent can also be utilized in the prediction of responsiveness to EGFR tyrosine kinase inhibitors (TKIs) and the selection of patients that respond well to those kinase inhibitors that specifically target forms of EGFR with activating mutations. EGFR-activating mutations play a key role in the development of certain tumors and in tumor resistance to a variety of antineoplastic agents.
fluorine F 18 para-chloro-2-fluoroethyl-etomidate: A radioconjugate composed of para-chloro-2-fluoroethyletomidate (CETO) conjugated to the radioisotope fluorine F 18 (18F), with potential application in adrenal imaging during positron emission tomography/computed tomography (PET/CT). Upon administration of [18F]CETO, the CETO moiety targets, binds to and is taken up by the adrenocortical cells located on the adrenal glands. Upon PET/CT, primary aldosteronism and adrenal tumors, such as cortisol producing adrenocortical adenoma and non-functioning adrenocortical carcinoma, can be visualized and detected during PET/CT imaging.
fluorine F 18 PARP inhibitor: A radiotracer consisting of a 1(2H)phthalazinone-based poly(ADP-ribose) polymerase 1 (PARP1) inhibitor radiolabeled with the positron emitting isotope fluorine F 18, which can potentially be used for the imaging of PARP1 expression using positron emission tomography (PET). Upon administration, fluorine F 18 PARPi targets and binds to PARP1. Upon PET, PARP1-expressing tumor cells can be visualized. PARP1, which is overexpressed in many cancer cell types, catalyzes post-translational ADP-ribosylation of nuclear proteins and plays a key role in the repair of DNA strand breaks.
fluorine F 18 piflufolastat: A urea-based radiotracer composed of the prostate specific membrane antigen (PSMA) targeting agent DCFPyL and labeled with the positron-emitting isotope, fluorine F 18, that can potentially be used for positron emitting tomography (PET) imaging. Upon administration of fluorine F piflufolastat, piflufolastat binds to PSMA expressed on tumor cells. The fluorine F 18 moiety facilitates PET imaging of PSMA-expressing tumor cells. PSMA, a cell-surface antigen, is abundantly present on the surface of prostate cancer cells and on the neovasculature of most solid tumors.
fluorine F 18 PSMA-1007: A radioconjugate containing the human prostate-specific membrane antigen (PSMA)-targeting ligand, PSMA-1007, labeled with the radioisotope fluorine F 18, with potential imaging activity using positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18 PSMA-1007, the PSMA-1007 moiety targets and binds to PSMA-expressing tumor cells. This allows for visualization of PSMA-expressing cells upon imaging. PSMA, a tumor-associated antigen (TAA) and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and strongly overexpressed in prostate cancer (PCa) cells, with its level rising with increasing tumor differentiation and in hormone-refractory cancers.
fluorine F 18 PT2385: A radioconjugate containing PT2385, a small molecule inhibitor of the hypoxia inducible factor (HIF)-2alpha, conjugated to the positron-emitting isotope fluorine F 18, with potential imaging activity upon positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18 PT2385, the PT2385 moiety specifically targets and binds to HIF-2alpha overexpressed on tumor cells, thereby allowing the visualization of tumor cells expressing HIF-2alpha upon PET/CT. HIF-2alpha, a heterodimeric transcription factor overexpressed in many cancer cell types, promotes proliferation, progression and metastasis of tumors.
fluorine F 18 RD2: A radioconjugate composed of the amyloid-beta-binding peptide RD2 labeled with the radionuclide fluorine F 18, with potential amyloid-beta peptide imaging activity upon positron emission topography (PET)/computed tomography (CT). Upon administration of fluorine F 18 RD2, RD2 targets and binds to amyloid-beta. Upon PET/CT imaging, amyloid-beta plaques can be visualized and detected. Amyloid-beta is a key component in plaque formation in Alzheimer's disease. Elevated plasma levels of amyloid-beta are also associated with some cancers.
fluorine F 18 RGD-K5: A radiotracer composed of a cyclic triazole-containing the Arg-Gly-Asp (RGD) peptide (RGD-K5) radiolabeled with fluorine F 18, with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET). Upon administration, the RGD moiety of fluorine F 18 RGD-K5 selectively binds to alphaVbeta3 integrin. During PET, alphaVbeta3-expressing tumor cells can be visualized and the degree of tumor angiogenesis can be determined. AlphaVbeta3 integrin, a cell adhesion and signaling receptor, is upregulated in tumor vessel endothelial cells and has been associated with neovascularization, differentiation, proliferation of tumor cells, and metastasis.
fluorine F 18 tetrafluoroborate: A radioconjugate composed of the sodium-iodide symporter (NIS; SLC5A5) ligand tetrafluoroborate (TFB) labeled with the radionuclide fluorine F 18, with potential use as an imaging agent for NIS-expressing cells upon positron emission tomography (PET). Upon administration, fluorine F 18 tetrafluoroborate targets, binds to, and is taken up by NIS, which is expressed on the surface of cells in the normal thyroid gland, lactating mammary gland and various tumors. Then, NIS-expressing cells can be visualized and NIS expression levels can be assessed using PET. Since iodides are taken up by NIS, this agent may predict the uptake of radioactive iodine by cancer cells.
fluorine F 18 trioxolane: A labile iron pool (LIP) radiotracer composed of 1,2,4-trioxolane (TRX) radiolabeled with the positron-emitting isotope fluorine F 18, with potential cancer cell imaging activity during positron emission tomography (PET). As tumor cells accumulate more iron than normal, healthy cells due to their increased need for energy to proliferate, when fluorine F 18 TRX is administered, it is selectively taken up by rapidly proliferating tumor cells, reacts with ferrous iron (Fe2+), and accumulates in tumor cells. Upon PET, tumor cells.
fluorine F 18 W372: A radiotracer composed of W372 radiolabeled with the radioisotope fluorine F 18, with potential amyloid-beta (Abeta) peptide imaging activity upon positron emission topography (PET). Upon administration, the W372 moiety of fluorine F 18 W372 selectively targets and binds to amyloid-beta in the brain. Upon binding, amyloid-beta plaques can be visualized and detected during PET imaging. Amyloid-beta accumulates in the brain and is a key component in plaque formation in Alzheimer's disease.
fluorine F 18 WC-4-116: A radioconjugate composed of an isatin sulfonamide analog labeled with the positron-emitting isotope fluorine F 18, with potential imaging activity for activated caspase-3, which is a marker for apoptosis, using positron emission tomography/computed tomography (PET/CT). Upon administration, fluorine F 18 WC-4-116 is preferentially taken up by and accumulates in cells with high caspase-3 activity. Upon PET/CT imaging, caspase-3 activation may be detected, and apoptotic activity, including chemotherapy-induced tumor apoptosis, may be assessed. Caspase-3, a cysteine protease, plays an important role in apoptosis.
fluorine F 18-4-L-fluoroglutamine (2S,4R): A radioconjugate and glutamine analog consisting of the fluorine F 18 labeled 2S, 4R stereoisomer of 4-fluoroglutamine with potential use as a metabolic tracer for tumor imaging. Upon intravenous administration, fluorine F 18-4-L-fluoroglutamine (2S,4R) is preferentially taken up by cancer cells, possibly driven by c-Myc upregulation. Upon positron emission tomography (PET), cancer cells can be imaged. Tumor cells use the amino acid glutamine for nutritional purposes necessary for energy production and growth; as tumor cells proliferate more rapidly than normal healthy cells, glutamine uptake is higher in certain cancer cells.
fluorine F 18-5-fluoro-2-deoxycytidine: A radioconjugate composed of a fluorinated pyrimidine analog, linked to the radioisotope fluorine F 18 with potential imaging activity using positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18-5-fluoro-2-deoxycytidine ([F-18]-FdCyd), the FdCyd moiety is phosphorylated by deoxycytidine kinase to 5-fluoro-2’-deoxycytidylate (FdCMP) and deaminated by deoxycytidylate (dCMP) deaminase, an enzyme overexpressed by tumor cells, to 5-fluoro-2-deoxyuridine monophosphate (FdUMP). Eventually, FdUMP is metabolized to the triphosphate forms 5-fluoro-2′-deoxycytidine-triphosphate (FdCTP) and fluorodeoxyuridine triphosphate (FdUTP). FdCTP and FdUTP inhibit DNA methyltransferase (DNMT) and DNA methylation, and induce DNA strand breaks, respectively. FdCyd is coadministered with tetrahydrouridine (THU), an inhibitor of cytidine/deoxycytidine deaminase, which prevents FdCyd breakdown and increases its efficacy. The fluorine F 18 moiety can be imaged upon PET/CT, thereby allowing for the evaluation of the biodistribution of FdCyd and its uptake by tumor cells.
fluorine F 18-6-fluorodopamine: A radioconjugate consisting of 6-fluorodopamine labeled with fluorine F18 (6-[18F]FDA), with potential diagnostic activity. Upon administration, 6-[18F]FDA is taken up by presynaptic sympathetic nerve endings via the norepinephrine transporter (NET) uptake-1. Once inside, 6-[18F]FDA is rapidly converted by dopamine-beta-hydroxylase into 6-[18F]fluoronorepinephrine (6-[18F]FNE) and stored into neuronal storage vesicles. Upon positron emission tomographic (PET) scanning of the F18, sympathetic innervated regions can be visualized, such as those in pheochromocytoma.
fluorine F 18-active site inhibited factor VIIa: A radioconjugate containing a tissue factor (TF) tracer, a derivative of activated factor VII (FVIIa), labeled with fluorine F 18, with potential use for TF-expressing tumor imaging using positron emission tomography (PET). Upon administration of fluorine F 18 active site inhibited factor VIIa (18F-ASIS), the active site inhibited factor VIIa (FVIIai) moiety selectively targets and binds, with a much higher binding affinity than FVIIa, to TF. Upon PET imaging, tumor cells expressing TF can be visualized and assessed. TF, a transmembrane glycoprotein, is overexpressed on certain tumor cell types and is correlated with tumor aggression and poor prognosis.
fluorine F 18-AIF-NOTA-neurotensin: A radioconjugate containing neurotensin (NT) linked to the radionuclide fluorine F 18 (18F), by the macrocyclic chelating agent, 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), through a method that first couples 18F to aluminum (Al), with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18-Al-NOTA-neurotensin, the ligand moiety targets and binds to the neurotensin receptor (NTR). Upon PET/CT, NTR-expressing tumor cells can then be visualized and NTR tumor cell expression can be assessed, as well as the diagnosis and stage of cancer. The neuropeptide NT is overexpressed in certain types of cancers and plays a key role in tumor cell proliferation.
fluorine F 18-AIF-NOTA-pentixather: A radioconjugate composed of the pentapeptide pentixather, a chemokine receptor C-X-C chemokine receptor type 4 (CXCR4)-targeting ligand, conjugated, via the macrocyclic chelating agent, 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), to fluorine F 18 radiolabeled aluminum fluoride ([18F]AIF), with potential diagnostic imaging activity upon positron emission tomography (PET)/computed tomography (CT). Upon administration, fluorine F 18-AIF-NOTA-pentixather targets and binds to CXCR4-expressing cells. This allows for the visualization of CXCR4-expressing cells upon PET/CT. CXCR4, a G-protein-coupled receptor and marker of poorly differentiated cells, is overexpressed on various cancer cells and in aldosterone-producing tissues. It plays a key role in tumor growth, progression, invasiveness and metastasis.
fluorine F 18-Al-NOTA-MATBBN: A radioconjugate containing a bombesin (BBN) peptide analog, derived from an unspecified GRPR antagonist (MATBBN) that targets the gastrin-releasing peptide receptor (GRPR), and is linked to the radionuclide fluorine F 18 (18F), by the macrocyclic chelating agent, 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), through a method that first couples 18F to aluminum (Al), with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of fluorine F 18-Al-NOTA-MATBBN, the peptide moiety targets and binds to GRPR. Upon PET/CT, GRPR-expressing tumor cells can then be visualized. GRPR, also called bombesin receptor 2 (BB2), is a seven-transmembrane G protein-coupled receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers. Bombesin is a peptide exhibiting high affinity for the gastrin-releasing peptide receptor (GRPR).
fluorine F 18-Al-NOTA-octreotide: A radioconjugate consisting of octreotide linked to the radionuclide fluorine F 18 (18F), by the macrocyclic chelating agent, 1,4,7-triazacyclononane-1,4,7-triacetate (NOTA), through a method that first couples 18F to aluminum (Al), with potential imaging activity using positron emission tomography (PET). Upon administration of fluorine F 18-Al-NOTA-octreotide, the octreotide moiety targets and binds to somatostatin receptors (SSTRs) on SSTR-expressing tumor cells. This allows for visualization of SSTR-expressing tumor cells upon PET imaging. SSTRs have been shown to be present in large numbers on neuroendocrine tumors (NETs) and their metastases, while most other normal tissues express low levels of SSTRs.
fluorine F 18-AlF-cys-variant 3 pH low insertion peptides: A radioconjugate composed of pH (low) insertion peptides (pHLIP) variant 3 (Var3) conjugated, via a cysteine residue, to fluorine F 18-labeled aluminum fluoride (AlF) complex, with potential use as an imaging agent for the acidic extracellular environment surrounding tumors upon positron emission tomography (PET). Upon administration of fluorine F 18-AlF-cys-Var3 pHLIP, the Var3 pHLIP moiety specifically targets, tightly binds to and gets inserted into the cellular membrane of tumor cells in environments with low extracellular pH. Upon PET, tumor cells and the extent of acidity can be visualized and assessed using PET. Tumor cell environments are more acidic than normal, healthy tissue environments. The pHLIPs specifically fold into an alpha-helical conformation and become inserted across the membrane at low extracellular pH whereas they are unfolded and unbound at higher pHs.
fluorine F 18-alfatide II: A radiotracer composed of a pegylated, dimeric arginine-glycine-aspartic acid (RGD) peptide (PRGD2), radiolabeled, via the chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), to a fluorine F 18-aluminum complex (AlF), with potential alphaVbeta3 integrin (vitronectin receptor) imaging activity using positron emission topography (PET). Upon administration, the RGD moiety of fluorine F 18-alfatide II selectively binds to alphaVbeta3 integrin. During PET, alphaVbeta3-expressing tumor cells can be visualized and the degree of tumor angiogenesis can be determined. AlphaVbeta3 integrin, a cell adhesion and signaling receptor, is upregulated in tumor vessel endothelial cells and has been associated with neovascularization, differentiation, proliferation of tumor cells, and metastasis. Pegylation provides improved drug penetration into tumors and decreases drug clearance, thereby increasing efficacy while lowering systemic toxicity.
fluorine F 18-AMBF3-TATE: A radioconjugate consisting of a alkyltrifluoroborate conjugated to tyrosine-3-octreotate (Tyr3-octreotate or TATE) and labeled with the positron emission tomography (PET) tracer fluorine F 18, which may be used as a somatostatin receptor (SSTR) imaging agent in conjunction with PET to image neuroendocrine tumors (NETs). Upon administration, fluorine F 18-AMBF3-TATE specifically binds to type 2 SSTR, present on the cell membranes of many types of NETs. This allows for visualization of SSTR2-positive cells upon imaging. SSTR subtypes have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTR subtypes.
fluorine F 18-ara-G: A radioconjugate composed of the guanosine analog arabinosyl guanine (Ara-G), a high-affinity substrate for both cytoplasmic deoxycytidine kinase (DCK) and mitochondrial deoxyguanosine kinase (dGK), labeled with fluorine F 18, that can potentially be used as a tracer for imaging of activated T lymphocytes during positron emission tomography (PET). Upon administration, fluorine F 18-ara-G is taken up by and accumulates in activated T lymphocytes with high levels of DCK and dGK. After phosphorylation by DCK and dGK, the 18F moiety can be visualized by PET imaging. Fluorine F 18 ara-G can potentially be used as an imaging agent to detect anti-tumor immune responses and to predict the therapeutic efficacy of immunotherapies. DCK and dGK, both nucleoside salvage pathway enzymes, are overexpressed in activated T cells.
fluorine F 18-azafol: A radioconjugate containing a folic acid receptor (FR; folate receptor) tracer labeled with fluorine F 18, with potential use for FR-expressing tumor imaging using positron emission tomography (PET). Upon administration of fluorine F 18-azafol, the azafol moiety selectively targets and binds to FR. This allows the visualization of tumor cells expressing FR using PET. FR is overexpressed on certain tumor cell types.
fluorine F 18-BMS-986229: A radiotracer composed of BMS-986229, a tracer targeting programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), labeled with the radioisotope fluorine F 18, with potential use for assessing PD-L1 tumor antigen expression using positron emission tomography (PET). Upon administration of fluorine F 18-BMS-986229, the BMS-986229 moiety targets and binds to PD-L1 expressed on certain tumor cells. Upon PET imaging, the radiotracer can be visualized and the extent of PD-L1 expression can be assessed.
fluorine F 18-DPA-714: A radioconjugate composed of DPA-714, a ligand for the 18 kDa translocator protein (TSPO), and labeled with the positron-emitting isotope fluorine F 18, that can be used as a diagnostic imaging agent to detect TSPO-expressing cells using positron emission tomography (PET). Upon administration of fluorine F 18 DPA-714, the DPA-714 moiety targets and binds to TSPO-expressing cells. Upon PET, fluorine F 18 can be detected and TSPO-expressing cells can be visualized. This can facilitate detection of inflammatory sites and cancer cells. TSPO, also called the peripheral benzodiazepine receptor (PBR), is found on the outer mitochondrial membrane and is overexpressed on a variety of cancer cells, tumor-infiltrating macrophages, and during inflammation.
fluorine F 18-FETrp: A radioconjugate containing an analog of tryptophan, fluoroethyl-tryptophan (FETrp), labeled with the positron-emitting radioisotope fluorine F 18, with potential imaging applications upon positron emitting tomography (PET). Upon administration, fluorine F 18-FETrp is taken up by and accumulates in tumor cells. This may allow for the visualization of tumors upon PET. The immunosuppressive kynurenine pathway present in tumor cells leads to abnormal tryptophan metabolism and increased uptake of tryptophan by tumor cells.
fluorine F 18-fluoroazomycin arabinoside: A radiofluorinated 2-nitroimidazole derivative with hypoxia-specific tracer activity. Fluorine F 18-fluoroazomycin arabinoside is reduced under hypoxic conditions and is often seen in various malignant tumors, forming highly reactive intermediates. In its reduced form, fluorine F 18-fluoroazomycin arabinoside covalently binds to macromolecules, thereby accumulating in hypoxic cells and allowing radioisotopic imaging of these particular cells. Compared to fluorine F 18-misonidazole, fluorine F 18-fluoroazomycin arabinoside has a lower octanol:water partition coefficient; it therefore has less tendency to accumulate in lipophilic tissues and exhibits a faster renal clearance, leading to an improved imaging ability of hypoxic tissue.
fluorine F 18-fluorothymidine: A radioconjugate consisting of a thymidine analogue radiolabeled with fluorine F 18, a positron emitting isotope. Phosphorylated by S-phase-specific thymidine kinase 1, fluorine F 18 fluorothymidine is trapped intracellularly by entering the salvage pathway of DNA synthesis without incorporation into DNA. 18F-FLT serves a marker of tumor cell proliferation for imaging with positron emission tomography (PET); as a marker of proliferation rather than metabolism, it is more specific to tumor tissue than 2-deoxy-2-[18F] fluoro-D-glucose (18F-FDG). This agent is metabolically stable, accumulates in the normal bone marrow and the liver, and does not cross the blood-brain barrier.
fluorine F 18-labeled 2-FACPC: A radioconjugate composed of an analog of the synthetic, alicyclic amino acid aminocyclopentane carboxylic acid (ACPC) radiolabeled with the positron-emitting isotope fluorine F 18 (2-[18F]FACPC), with potential cancer cell imaging activity during positron emission tomography (PET). As tumor cells have a higher rate of protein synthesis than normal, healthy cells, upon administration, fluorine F 18 labeled 2-FACPC is selectively taken up by rapidly proliferating tumor cells through the sodium-independent subtype L amino acid transport system (AAT) which leads to the accumulation of this tracer in tumor cells. Upon PET, tumor cells can then be visualized.
fluorine F 18-labeled DX600: A radioconjugate composed of DX600, a peptide targeting angiotensin converting enzyme 2 (ACE2), labeled with the radioisotope fluorine F 18, with potential imaging activity upon positron emission tomography (PET). Upon administration of fluorine F 18-labeled DX600, DX600 targets and binds to ACE2. Upon PET imaging, ACE2 expression can be assessed. ACE2 plays an important role in the renin-angiotensin system (RAS), and may be overexpressed in tumors.
fluorine F 18-labeled MeFAMP: A radioconjugate composed of the non-natural amino acid (R)-3-fluoro-2-methyl-2-(methylamino)propanoic acid (MeFAMP) radiolabeled with the positron-emitting isotope fluorine F 18, with potential cancer cell imaging activity during positron emission tomography (PET). Due to their altered metabolic states, tumor cells have a higher rate of protein synthesis than normal, healthy cells and, upon administration, fluorine F 18-labeled MeFAMP is selectively taken up by rapidly proliferating tumor cells through the membrane-associated amino acid transport system (AAT). It is neither incorporated into proteins nor readily degraded, resulting in the accumulation of this imaging agent in tumor cells. Upon PET, tumor cells can then be visualized.
fluorine F 18-labeled S-(3-Fluoropropyl)homocysteine hydrochloride: The hydrochloride salt form of a radioconjugate composed of a synthetic derivative of the amino acid methionine radiolabeled with fluoride F 18, with potential use as a tumor imaging agent during positron emission tomography (PET). Upon administration, fluorine F 18-labeled S-(3-fluoropropyl) homocysteine is preferentially taken up by tumor cells through an amino acid transporter, which is overexpressed by cancer cells. Because tumor cells have a higher rate of proliferation than normal cells, these cancer cells have increased rates of protein synthesis and thus an increased demand for amino acids. This allows for visualization of tumors cells upon PET.
fluorine F 18-PEG3-FPN: A radioconjugate comprised of PEG3-FPN, a pegylated tracer for melanin, and labeled with the positron-emitting isotope fluorine F 18, that can be used as a diagnostic imaging agent to detect melanin-expressing cells using positron emission tomography (PET). Upon administration, fluorine F 18-PEG3-FPN targets and binds to melanin-expressing cells. Upon PET, fluorine F 18 can be detected, and melanin-expressing cells can be visualized. Melanin is expressed in many melanomas, and pegylation lowers nonspecific uptake by the liver.
fluorine F 18-WL12: A radiotracer composed of the programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274)-binding peptide WL12 radiolabeled with the radionuclide fluorine F 18, with potential PD-L1 imaging activity using positron emission tomography (PET). Upon administration of fluorine F 18-WL12, the WL12 moiety targets and binds to PD-L1 expressed on certain tumor cells. Upon uptake and PET imaging, the radioisotope moiety can be visualized and the extent of PD-L1 expression can be assessed. This may be used to predict the therapeutic response to PD-L1-targeting agents.
fluorine F-18 fluoropaclitaxel: A radiotracer containing paclitaxel labeled with the radioisotope fluorine F18 with potential use as an imaging agent. After cellular uptake, the paclitaxel moiety of fluorine F18 fluoropaclitaxel binds to tubulin. Upon uptake, the radioisotope moiety may be detected using positron emission tomography (PET), thereby allowing imaging and quantification of the biodistribution of paclitaxel. This could identify multidrug resistant (MDR) status of tumor cells and select patients that will likely respond to paclitaxel treatment.
fluorine F18 BMS-986192: A radiotracer composed of the adnectin BMS-986192, a fibronectin-based protein that targets programmed cell death-1 ligand 1 (PD-L1; cluster of differentiation 274; CD274), labeled with the radioisotope fluorine F 18, with potential use for assessing PD-L1 tumor antigen expression using positron emission tomography (PET). Upon administration of fluorine F 18 BMS-986192, the BMS-986192 moiety specifically targets and binds to PD-L1 expressed on certain tumor cells. Upon PET imaging, the radiotracer can be visualized and the extent of PD-L1 expression can be assessed. Adnectins, a protein family derived from the 10th type III domain of human fibronectin with high-affinity targeting capabilities, have favorable physicochemical properties, such as small size, high stability, high affinity and specificity.
fluorodopa F 18: The amino acid analog fluorodopa (FDOPA) labeled with fluorine F 18, a positron-emitting isotope, with potential tumor tracer property. Fluorine F 18 fluorodopa is able to cross the blood-brain barrier and is taken up by brain tumor cells. As uptake is higher in tumor cells, tumors may then be imaged using positron emission tomography (PET). Assessing tumor uptake of FDOPA may be beneficial for diagnosis, localization and in determining further treatment.
Fluorofur: (Other name for: tegafur)
Fluoroplex: (Other name for: topical fluorouracil)
fluoropyrimidine: Any fluoropyrimidine-based agent with potential antineoplastic activity. As an antimetabolite, a fluoropyrimidine interferes with pyrimidine utilization and incorporation into DNA and RNA.
fluorouracil: An antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions.
fluorouracil implant: An implant containing a sustained release particle of fluorouracil, an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine, with antineoplastic activity. Upon implantation and subsequent release, fluorouracil is converted into the active metabolite 5-fluoroxyuridine monophosphate that competes with the pyrimidine uracil during RNA synthesis while another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate, inhibits thymidylate synthase and thus DNA synthesis.
fluorouracil-e therapeutic implant: An injectable collagen matrix gel containing the antimetabolite fluorouracil and the sympathicomimetic agent epinephrine with potential antineoplastic activity. After intratumoral injection, fluorouracil is converted into the active metabolite 5-fluoroxyuridine monophosphate that competes with uracil during RNA synthesis while another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate, inhibits thymidylate synthase and, so, DNA synthesis. Epinephrine, a potent vasoconstrictor, is added to the gel to enhance penetration of fluorouracil into tumor tissue and reduce dispersion to surrounding tissues, thus enhancing the local concentration of fluorouracil. Compared to systemic administration, the intratumoral injection of fluorouracil combined with epinephrine may increase fluorouracil's chemotherapeutic efficacy while minimizing systemic toxicity.
fluosol-DA: A perfluorocarbon blood substitute in trials for the treatment of severe anemia
fluoxetine: A diphenhydramine derivative and selective serotonin reuptake inhibitor with antidepressant, anti-anxiety, antiobsessional and antibulimic activity and with potential immunomodulating activity. Upon administration, fluoxetine binds to the presynaptic serotonin (5-HT) receptor resulting in negative allosteric modulation of the receptor complex, thereby blocking recycling of serotonin by the presynaptic receptor. Inhibition of serotonin reuptake by fluoxetine enhances serotonergic function through serotonin accumulation in the synaptic space, resulting in long-term desensitization and downregulation of 5-HT receptors, preventing 5-HT-mediated signaling and leading to antidepressant, anti-anxiety, antiobsessional and antibulimic effects. In addition, fluoxetine may inhibit the expression of pro-inflammatory cytokines, including interleukin-6 (IL-6). This may prevent IL-6-mediated inflammation and cytokine storm.
fluoxymesterone: A halogenated derivative of 17-alpha-methyltestosterone. Similar to testosterone, fluoxymesterone binds to and activates specific nuclear receptors, resulting in an increase in protein anabolism, a decrease in amino acid catabolism, and retention of nitrogen, potassium, and phosphorus. This agent also may competitively inhibit prolactin receptors and estrogen receptors, thereby inhibiting the growth of hormone-dependent tumor lines. Fluoxymesterone is approximately five times more potent than methyltestosterone.
fluphenazine hydrochloride: The hydrochloride salt of fluphenazine, a phenothiazine with antipsychotic activity and potential antineoplastic activity. Fluphenazine blocks postsynaptic dopamine D2 receptors in the limbic system, cortical system and basal ganglia, resulting a reduction of schizophrenia-associated hallucinations and delusions. In addition, as a serotonin antagonist, this agent may inhibit lymphocyte and myeloma cell proliferation by blocking 5-hydroxytrptamine type 1B (5-HT type 1B) receptors for serotonin.
flurbiprofen: A derivative of propionic acid, and a phenylalkanoic acid derivative of non-steroidal antiinflammatory drugs (NSAIDs) with analgesic, antiinflammatory and antipyretic effects. Flurbiprofen non-selectively binds to and inhibits cyclooxygenase (COX). This results in a reduction of arachidonic acid conversion into prostaglandins that are involved in the regulation of pain, inflammation and fever. This NSAID also inhibits carbonic anhydrase, thereby reducing the production of hydrogen and bicarbonate ions. Upon ocular administration, flurbiprofen may reduce bicarbonate ion concentrations leading to a decrease in the production of aqueous humor, thereby lowering intraocular pressure.
Flurizan: (Other name for: tarenflurbil)
flurocitabine: A Cytosine Arabinoside derivative that inhibits pyrimidine synthesis, causing inhibition of DNA synthesis. (NCI)
Flushield: (Other name for: trivalent influenza vaccine)
flutamide: A toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide. Flutamide and its more potent active metabolite 2-hydroxyflutamide competitively block dihydrotestosterone binding at androgen receptors, forming inactive complexes which cannot translocate into the cell nucleus. Formation of inactive receptors inhibits androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest or transient tumor regression.
flutemetamol F 18: A radiopharmaceutical containing flutemetamol, a thioflavin derivative of Pittsburgh compound B (PiB) labeled with the radioisotope fluorine F18 that can be used to detect beta-amyloid deposition upon positron emission tomography (PET). After intravenous administration of flutemetamol F 18, the flutemetamol moiety selectively accumulates in and binds to cerebral fibrillar amyloid-beta in the brain. The fluorine F18 radioisotope moiety is detected using PET, which allows imaging and quantification of amyloid-beta density. Amyloid plaque deposition is linked to cognitive decline, including Alzheimer’s disease, and may be linked to chemotherapy-induced cognitive impairment (CICI).
fluticasone propionate: The propionate salt form of fluticasone, a synthetic trifluorinated glucocorticoid receptor agonist with antiallergic, antiinflammatory and antipruritic effects. Binding and activation of the glucocorticoid receptor results in the activation of lipocortin that in turn inhibits cytosolic phospholipase A2, which triggers cascade of reactions involved in synthesis of inflammatory mediators, such as prostaglandins and leukotrienes. Secondly, mitogen-activated protein kinase (MAPK) phosphatase 1 is induced, thereby leads to dephosphorylation and inactivation of Jun N-terminal kinase directly inhibiting c-Jun mediated transcription. Finally, transcriptional activity of nuclear factor (NF)-kappa-B is blocked, thereby inhibits the transcription of cyclooxygenase 2, which is essential for prostaglandin production.
fluvastatin sodium: The sodium salt of a synthetic lipid-lowering agent with potential antineoplastic activity. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Through the inhibition of mevalonate synthesis, statins, like fluvastatin, have been shown to inhibit the production of dolichol, geranylpyrophosphate (GPP) and farnesylpyrophosphate (FPP) and the isoprenylation of the intracellular G-proteins Ras and Rho, which may result in antiangiogenic, apoptotic, and antimetastatic effects in susceptible tumor cell populations.
Fluvirin: (Other name for: trivalent influenza vaccine)
fluvoxamine maleate: The maleate salt form of fluvoxamine, a 2-aminoethyl oxime ether of aralkylketones, with antidepressant, antiobsessive-compulsive, and antibulimic activities. Fluvoxamine blocks serotonin reuptake by inhibiting the serotonin reuptake pump of the presynaptic neuronal membrane leading to an increase of serotonin levels within the synaptic cleft. This results in facilitated serotonergic transmission and decreased serotonin turnover leading to antidepressant and antiobsessive-compulsive effects.
Fluzone: (Other name for: trivalent influenza vaccine)
FMS inhibitor JNJ-40346527: A small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between FMS and its ligand CSF1, thereby preventing autophosphorylation of FMS. As a result, unphosphorylated FMS cannot activate FMS-mediated signaling pathways, thus potentially inhibiting cell proliferation in FMS-overexpressed tumor cells. FMS, a tyrosine kinase receptor, is overexpressed in certain tumor cell types and plays an essential role in macrophage differentiation, recruitment, and activation as well as the regulation of cell proliferation.
Fms/Trk tyrosine kinase inhibitor PLX7486: The tosylate salt form of PLX7486, a selective inhibitor of the receptor tyrosine kinases colony-stimulating factor-1 receptor (CSF1R; fms) and neurotrophic tyrosine kinase receptor types 1, 2 and 3 (TrkA, TrkB, and TrkC, respectively) with potential antineoplastic activity. Upon administration, PLX7486 binds to and inhibits the activity of these tyrosine kinases. This inhibits Fms and Trk-mediated signaling transduction pathways that are upregulated in certain cancer cell types. This may eventually halt tumor cell proliferation in Fms and TrkA, TrkB, and/or TrkC-overexpressing tumor cells. Fms and TrkA, TrkB, and TrkC are receptor tyrosine kinases that are upregulated or mutated in a variety of tumors and promote tumor cell proliferation and survival.
folate binding protein E39 peptide vaccine: A cancer vaccine comprised of human leukocyte antigen (HLA) A2 restricted folate binding protein (FBP) epitope E39 (amino acids 191 to 199), with potential immunostimulatory and antineoplastic activity. Upon intradermal injection, FBP E39 peptide vaccine may induce a specific cytotoxic T-lymphocyte (CTL) response against FBP-expressing tumor cell types. FBP is a membrane-bound, tumor-associated antigen highly overexpressed in various tumor cell types, such as in breast, ovarian and endometrial cancers; E 39 is a strong immunogenic peptide.
folate binding protein J65 peptide vaccine: A cancer vaccine comprised of human leukocyte antigen (HLA)-A2-restricted folate binding protein (FBP) epitope J65 (9 amino acids; EIWTFSTKV), with potential immunostimulatory and antineoplastic activities. Upon intradermal injection, FBP J65 peptide vaccine may induce a specific cytotoxic T-lymphocyte (CTL) response against J65 FBP-expressing tumor cell types. FBP is a membrane-bound, tumor-associated antigen overexpressed in various tumor types, including breast, ovarian and endometrial cancers. J65 is a strongly immunogenic peptide.
folate receptor alpha-loaded dendritic cell vaccine: A cell-based vaccine composed of autologous-monocyte-derived dendritic cells (DCs) loaded with five immunogenic peptide epitopes, derived from the tumor-associated antigen human folate receptor alpha (FR alpha or FOLR1), including FR30, FR56, FR76, FR113, and FR238, with potential immunomodulatory and antineoplastic activity. Ex vivo treatment of the DCs with a p38 inhibitor decreases p38-mediated signaling and enhances ERK activation. This may allow, upon intradermal administration of the multi-epitope FR alpha-loaded DC vaccine into the patient, for decreased activation and expansion of CD4+ regulatory T-cells (Tregs), increased differentiation and expansion of interleukin-17 secreting T helper cells (Th17) and activation of CD8+ CTLs, which induces a strong anti-tumor T-cell immune response against FR alpha-overexpressing tumor cells. FR alpha is a high-affinity folate-binding protein and a member of the folate receptor family; this receptor is overexpressed in the majority of ovarian cancers and in about approximately 50% of breast cancers.
folate receptor-targeted epothilone BMS753493: A folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation.
folate receptor-targeted technetium Tc 99m EC20: A folate receptor-targeting radiopharmaceutical consisting of a folate-containing tetrapeptide chelator to which technetium Tc 99m is linked. The folate component of folate receptor-targeted technetium Tc 99m EC20 binds to folic acid receptors, which are frequently upregulated in many types of tumor cells and activated macrophages. Gamma scintigraphy may then be used to image folate receptor-positive tumors.
folate receptor-targeted tubulysin conjugate EC1456: An injectable targeted small molecule drug conjugate (SMDC) consisting of folate (vitamin B9) covalently linked to the potent mitotic poison and cytotoxic agent, tubulysin B hydrazide (Tub-B-H) with potential antineoplastic activity. Upon administration, the folate moiety of folate receptor-targeted tubulysin conjugate EC1456 preferentially binds to tumor cells expressing folate receptors (FR). After binding to FR, the agent is internalized by tumor cells and the Tub-B-H moiety inhibits the polymerization of tubulin into microtubules. This may lead to both cell cycle arrest and tumor cell apoptosis. FR, the membrane-bound, high-affinity receptor for folate, is overexpressed on a wide range of primary and metastatic human cancers.
folate receptor-targeted vinca alkaloid EC0489: A folate receptor-targeting cytotoxic drug conjugate consisting of a folate vitamin analogue linked to a vinca alkaloid microtubule destabilizing agent with potential antineoplastic activity. Mediated through its folate moiety, folate receptor-targeted Vinca alkaloid EC0489 delivers the cytotoxic vinca alkaloid moiety directly to cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the vinca alkaloid moiety binds to tubulin and disrupts microtubule assembly-disassembly dynamics, resulting in cell cycle arrest and apoptosis. The relative tumor cell specificity of this agent reduces the toxicity profile of its Vinca alkaloid moiety.
folate receptor-targeted vinca alkaloid/mitomycin C EC0225: A folate receptor-targeting cytotoxic agent with potential antineoplastic activity. Folate receptor-targeted vinca alkaloid/mitomycin C EC0225 contains two potent cytotoxic agents, a vinca alkaloid and mitomycin C, linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the cytotoxic agents directly into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the vinca alkaloid moiety binds to tubulin and disrupts microtubule assembly-disassembly dynamics, resulting in cell cycle arrest and apoptosis. Mitomycin C alkylates DNA, producing DNA cross-links and inhibiting DNA replication. The relative tumor cell specificity of EC0225 reduces the toxicity profiles of its cytotoxic agent moieties.
folate-FITC: A conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic activity. Folate-FITC binds to folate receptors, which are overexpressed on the surfaces of many cancer cells including kidney and ovarian cancer cells. Once bound to the cancer cell through the folate moiety of the conjugate, curculating anti-fluorescein antibodies.may recognize and bind to the FITC moiety, resulting in antibody-dependent cellular cytotoxicity.
FOLFIRI regimen: A regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan that can be used in the treatment of appendiceal, small bowel, pancreatic and occult primary adenocarcinoma; colorectal, esophageal and esophagogastric junction, gastric, and hepatobiliary cancers; well-differentiated grade 3 neuroendocrine tumors (NETs), and extrapulmonary poorly differentiated neuroendocrine carcinoma, large or small cell carcinoma and mixed neuroendocrine-non-neuroendocrine neoplasm.
FOLFIRI-bevacizumab regimen: A regimen consisting of bevacizumab, fluorouracil, irinotecan and leucovorin that may be used in the treatment of appendiceal adenocarcinoma, colorectal cancer, and small bowel adenocarcinoma.
FOLFIRI-cetuximab regimen: A chemoimmunotherapy regimen consisting of leucovorin (folinic acid), 5-fluorouracil, and irinotecan plus cetuximab used for the treatment of metastatic colorectal cancer that is positive for the expression of the epidermal growth factor receptor (EGFR) and the wild-type form of KRAS.
Folfirinox regimen: A regimen consisting of fluorouracil, irinotecan, leucovorin and oxaliplatin that can be used for the treatment of pancreatic and colorectal cancers; occult primary, appendiceal and small bowel adenocarcinomas; well-differentiated grade 3 neuroendocrine tumors (NETs), and extrapulmonary poorly differentiated neuroendocrine carcinoma, large or small cell carcinoma and mixed neuroendocrine-non-neuroendocrine neoplasm.
FOLFOX regimen: One of several chemotherapy regimens that include leucovorin calcium (calcium folinate), 5-fluorouracil and oxaliplatin and which may be used in the treatment of advanced-stage and metastatic colorectal cancer. FOLFOX regimens differ in agent dosing and administration schedule and include FOLFOX 4, FOLFOX 6, modified FOLFOX 6 (mFOLFOX 6) and FOLFOX 7.
Folic Acid: A collective term for pteroylglutamic acids and their oligoglutamic acid conjugates. As a natural water-soluble substance, folic acid is involved in carbon transfer reactions of amino acid metabolism, in addition to purine and pyrimidine synthesis, and is essential for hematopoiesis and red blood cell production.
folitixorin: A folate-based biomodulator with potential antineoplastic activity. Folitixorin stabilizes the covalent binding of the fluorouracil metabolite 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (FdUMP) to its target enzyme, thymidylate synthase, which results in inhibition of thymidylate synthase, depletion of thymidine triphosphate (TTP), a necessary constituent of DNA, and tumor cell death. Unlike leucovorin, folitixorin, as the active form of folate, does not require metabolic activation and may increase the chemotherapeutic effects of fluorouracil with lower toxicity.
Follutein: (Other name for: recombinant human chorionic gonadotropin)
Folotyn: (Other name for: pralatrexate)
Fonatol: (Other name for: diethylstilbestrol)
fondaparinux sodium: The sodium salt form of fondaparinux, a synthetic glucopyranoside with antithrombotic activity. Fondaparinux sodium selectively binds to antithrombin III, thereby potentiating the innate neutralization of activated factor X (Factor Xa) by antithrombin. Neutralization of Factor Xa inhibits its activity and interrupts the blood coagulation cascade, thereby preventing thrombin formation and thrombus development.
foralumab: A monoclonal antibody directed against cluster of differentiation 3 (CD3) epsilon, with immunomodulatory activity. Foralumab binds to CD3 epsilon on T cells, preventing T-cell activation and may also suppress immune responses. CD3 epsilon is a polypeptide that is part of the CD3-T cell receptor (TCR) complex.
Forane: (Other name for: isoflurane)
foretinib: An orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. VEGFR2 is found on endothelial and hematopoietic cells and mediates the development of the vasculature and hematopoietic cells through VEGF signaling.
Forfivo XL: (Other name for: bupropion hydrochloride)
forimtamig: A T-cell engaging bispecific antibody directed against both the tumor-associated antigen (TAA) G-protein coupled receptor family C group 5 member D (GPRC5D) and the T-cell surface antigen CD3, with potential antineoplastic activity. Upon administration, forimtamig binds to both GPRC5D expressed on tumor cells and CD3 on T cells. This results in the cross-linking of T cells and tumor cells and induces a potent cytotoxic T-lymphocyte (CTL) response against GPRC5D-expressing tumor cells. GPRC5D is overexpressed on certain tumors, such as multiple myeloma, while minimally expressed on normal, healthy cells, and plays a key role in tumor cell proliferation.
foritinib succinate: The succinate salt form of foritinib, an orally bioavailable inhibitor of the receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (ROS1), with potential antineoplastic activity. Upon oral administration, foritinib targets, binds to and inhibits the activity of ALK and ROS1, which leads to the disruption of ALK- and ROS1-mediated signaling and the inhibition of cell growth in ALK- and ROS1-expressing tumor cells. In addition, foritinib is able to cross the blood brain barrier. ALK and ROS1, overexpressed or mutated in many tumor cell types, play key roles in tumor cell proliferation, survival, invasion and metastasis.
formestane: A synthetic steroidal substance with antineoplastic activity. Formestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens.
formoterol fumarate oral: The orally bioavailable fumarate salt of formoterol, a long-acting, selective beta2-adrenergic receptor agonist with bronchodilating and potential anti-cachexia and anabolic activities. In addition to formoterol’s bronchodilating activity, formoterol exhibits anti-cachexia activity through the inhibition of the ATP-ubiquitin-dependent proteolytic system, which may result in a decrease in protein degradation and muscle cell apoptosis. In addition, formoterol may also increase insulin-like growth factor (IGF) signaling, resulting in an increase in protein synthesis. This agent may also inhibit the calcium-dependent calpain system, resulting in the inhibition of muscle wasting.
formoterol fumarate/roxithromycin: A combination preparation of the fumarate salt of a beta2-adrenergic receptor agonist and a macrolide antibiotic, with muscle-sparing and anti-cachexia effects. Formoterol appears to antagonize cachexia by reducing proteolysis mediated through the ubiquitin-protease pathway. Roxithromycin strongly inhibits inflammatory cytokine production and secretion from T cells and macrophages in vitro and in vivo. The combination exhibits a greater muscle sparing effect than either drug given individually at comparable doses.
forodesine hydrochloride: The hydrochloride salt of the synthetic high-affinity transition-state analogue forodesine. Forodesine binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction.
Fortamet: (Other name for: metformin hydrochloride)
Fosamax: (Other name for: alendronate sodium)
fosaprepitant dimeglumine: The dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis.
fosbretabulin disodium: The disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combretum caffrum) with potential vascular disrupting and antineoplastic activities. Upon administration, the prodrug fosbretabulin is dephosphorylated to its active metabolite, the microtubule-depolymerizing agent combretastatin A4, which binds to tubulin dimers and prevents microtubule polymerization, resulting in mitotic arrest and apoptosis in endothelial cells. In addition, this agent disrupts the engagement of the endothelial cell–specific junctional molecule vascular endothelial-cadherin (VE-cadherin) and so the activity of the VE-cadherin/β-catenin/Akt signaling pathway, which may result in the inhibition of endothelial cell migration and capillary tube formation. As a result of fosbretabulin's dual mechanism of action, the tumor vasculature collapses, resulting in reduced tumor blood flow and ischemic necrosis of tumor tissue.
fosbretabulin tromethamine: The tromethamine salt form of prodrug fosbretabulin, a water-soluble phosphate derivative of a stilbenoid phenol derived from the African bush willow (Combretum caffrum) with antineoplastic activities. Upon administration, fosbretabulin is dephosphorylated to its active metabolite, combretastatin A4, which targets and binds to tubulin dimers and prevents microtubule polymerization, thereby resulting in mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrata, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis.
foscenvivint: A potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. Foscenvivint specifically inhibits the recruiting of beta-catenin with its coactivator CBP (the binding protein of the cAMP response element-binding protein CREB); together with other transcription factors beta-catenin/CBP binds to WRE (Wnt-responsive element) and activates transcription of a wide range of target genes of Wnt/beta-catenin signaling. Blocking the interaction of CBP and beta-catenin by this agent prevents gene expression of many proteins necessary for growth, thereby potentially suppressing cancer cell growth. The Wnt/beta-catenin signaling pathway regulates cell morphology, motility, and proliferation; aberrant regulation of this pathway leads to neoplastic proliferation.
fosciclopirox: A phosphoryloxymethyl (POM) ester-based prodrug of ciclopirox (CPX), a synthetic, broad-spectrum antifungal agent with antibacterial, anti-inflammatory and potential antineoplastic activities. Upon intravenous administration of fosciclopirox, the POM moiety is cleaved off by phosphatases and the active metabolite CPX is released. Although its exact anticancer mechanism is not yet fully elucidated, CPX has been shown to inhibit tumor cell proliferation, induce apoptosis, and reduce tumor cell mobility in certain cancer types. CPX inhibits Notch1 activation and inhibits the Notch1-mediated signaling pathway, which is upregulated in many cancer cell types. This inhibits Notch downstream target proteins, inhibits the expression of gamma-secretase complex proteins, and prevents proliferation in susceptible cancer cells. CPX inhibits the iron-containing enzymes, catalase and peroxidase, which facilitate the decomposition of hydrogen peroxide, a reactive oxygen species (ROS) involved in oxidative stress. CPX also inhibits the iron-dependent enzyme ribonucleotide reductase, which is essential in DNA synthesis. CPX downregulates protein expression of cyclin D1 and cyclin E1, as well as their enzymatic counterparts cyclin-dependent kinases 4 and 2 (CDK4 and CDK2), which may inhibit tumor cell proliferation by slowing cell cycle progression from G1/G0 to S phase. Further, CPX may induce apoptosis by downregulating the expression of anti-apoptotic proteins, Bcl-xL and survivin, and increasing cleavage of Bcl-2. Additionally, CPX may inhibit tumor cell proliferation, survival and motility by inhibiting the phosphorylation of p70 S6 kinase 1 (S6K1) and eukaryotic initiation factor 4E binding protein 1 (4E-BP1), two downstream effector molecules of the mammalian target of rapamycin complex 1 (mTORC1). The CPX-POM prodrug improves the solubility of CPX and increases systemic efficacy.
fosdesdenosine sipalabenamide: A phosphoramidate derivative of the monophosphate form of cordycepin (3'-deoxyadenosine; 3'-dA), an adenosine derivative first isolated from Cordyceps sinensis, with potential antineoplastic, antioxidant, and anti-inflammatory activities. Upon administration and cellular uptake of fosdesdenosine sipalabenamide by passive diffusion, cordycepin monophosphate (3'-dAMP) is converted into its active anti-cancer metabolite 3'-deoxyadenosine triphosphate (3'-dATP). 3'-dATP functions as a ribonucleoside analogue and competes with ATP during transcription. Therefore, this agent causes RNA synthesis inhibition, inhibits cellular proliferation, and induces apoptosis. Also, 3'-dAMP activates AMP-activated protein kinase (AMPK) and reduces mammalian target of rapamycin (mTOR) signaling. This prevents the hyperphosphorylation of the translation repressor protein 4E-BP1. This results in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. mTOR, a serine/threonine kinase belonging to the phosphatidylinositol 3-kinase (PI3K)-related kinase (PIKK) family, plays an important role in the PI3K/AKT/mTOR signaling pathway that regulates cell growth and proliferation, and its expression or activity is frequently dysregulated in human cancers. Compared to cordycepin alone, the addition of the phosphoramidate moiety may overcome cancer resistance and allow for greater cytotoxicity as fosdesdenosine sipalabenamide does not require a nucleoside transporter for cellular uptake, is independent of enzymatic activation by adenosine kinase (AK) and is not susceptible to enzymatic degradation by adenosine deaminase (ADA). Altogether, this may help overcome cancer resistance to cordycepin.
fosfestrol: The diphosphate ester of a synthetic, nonsteroidal form of estrogen. A well-known teratogen and carcinogen, diethylstilbestrol inhibits the hypothalamic-pituitary-gonadal axis, thereby blocking the testicular synthesis of testosterone, lowering plasma testosterone, and inducing a chemical castration.
fosfomycin tromethamine: The tromethamine salt form of fosfomycin, a synthetic broad-spectrum antibiotic. Fosfomycin tromethamine binds to and inactivates the enzyme enolpyruvyl transferase. This leads to an irreversible blockage of the condensation of uridine diphosphate-N-acetylglucosamine with p-enolpyruvate, which is one of the first steps of bacterial cell wall synthesis, thereby eventually causing cell lysis. In addition, fosfomycin tromethamine reduces the adherence of bacteria to uroepithelial cells.
fosgemcitabine palabenamide: A pyrimidine analogue and a proprietary prodrug based on an aryloxy phosphoramidate derivative of gemcitabine with potential antineoplastic activity. Upon intravenous administration and cellular uptake, fosgemcitabine palabenamide is converted into the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP is incorporated into DNA, resulting in premature termination of DNA replication and eventually induction of apoptosis. With the phosphoramidate moiety on the gemcitabine monophosphate group, NUC-1031 has improved properties over its parent molecule: 1) is more lipophilic and accumulates in cancer cells by passive diffusion and does not require a nucleoside transporter, 2) as the agent is delivered in the monophosphate form, the first phosphorylation step by deoxycytidine kinase is not required, 3) this agent is not susceptible to deactivation by cytidine deaminase cleavage of the monophosphorylated form. Altogether, this may help overcome resistance to gemcitabine.
fosifloxuridine nafalbenamide: A phosphoramidate-based prodrug of the monophosphate (MP) form of 5-fluoro-2'-deoxyuridine (FUdR; FUDR), the active metabolite of fluorouracil (5-FU), an antimetabolite fluoropyrimidine analog of the pyrimidine nucleoside, with potential antineoplastic activity. Upon administration of the nucleotide analog prodrug fosifloxuridine nafalbenamide, fosifloxuridine nafalbenamide is readily taken up by tumor cells. In the tumor cell, the phosphoramidate moiety is removed and fosifloxuridine nafalbenamide is converted to its active form FUDR-MP. In turn, FUDR-MP binds to and inhibits thymidylate synthase (TS), resulting in the depletion of thymidine triphosphate (TTP) and thus DNA synthesis. With the phosphoramidate moiety attached to FUDR-MP, fosifloxuridine nafalbenamide, compared to 5-FU, is more lipophilic and accumulates in cancer cells by passive diffusion and does not require a nucleoside transporter, thereby generating higher intracellular concentrations. In addition, compared to 5-FU, once inside the cell FUDR-MP does not need to be phosphorylated and is already in its active form. Unlike 5-FU, fosifloxuridine nafalbenamide does not get deactivated or converted into toxic metabolites by dihydropyrimidine dehydrogenase (DPD) and thymidine phosphorylase (TP), which leads to both a longer half-life and less toxicity.
foslevcromakalim: An ophthalmic solution containing a prodrug of levcromakalim, a modulator of the adenosine triphosphate (ATP)-sensitive potassium (KATP) channel, with potential vasodilating and episcleral venous pressure (EVP)-lowering activities. Upon application into the eye, foslevcromakalim is converted to levcromakalim, which dilates blood vessels by opening the KATP channel. This lowers both EVP and elevated intraocular pressure (IOP).
foslinanib: An orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry activities. Upon oral administration, foslinanib targets and inhibits the formation of vasculogenic mimicry (VM; vascular mimicry). By destroying the VM channels and network, cancer cells are devoid of perfusion leading to an induction of cancer cell apoptosis and inhibition of cancer cell proliferation. VM is associated with tumor metastasis.
fosnetupitant/palonosetron hydrochloride: A combination formulation containing the prodrug of netupitant, fosnetupitant, a selective neurokinin 1 receptor (NK1R; TACR1) antagonist, and the hydrochloride salt form of palonosetron, a selective serotonin (5-hydroxytrytamine; 5-HT) receptor subtype 3 (5-HT3R) antagonist, with potential antiemetic activity. Upon intravenous administration, fosnetupitant is converted by phosphatases to its active form netupitant. Netupitant competitively binds to and blocks the activity of NK1Rs in the central nervous system (CNS), by inhibiting binding of the endogenous tachykinin-derived neuropeptide substance P (SP) to NK1R. This prevents delayed emesis, which is associated with SP secretion. Palonosetron competitively blocks the interaction of 5-HT with 5-HT3Rs located on vagal afferent nerves in the chemoreceptor trigger zone (CTZ). This inhibits acute emesis associated with 5-HT secretion and subsequent 5-HT3R activation. Altogether, this results in inhibition of acute and delayed nausea and vomiting, and may prevent chemotherapy-induced nausea and vomiting (CINV).
fosphenytoin sodium: The sodium salt form of fosphenytoin, a prodrug that is hydrolyzed to the anticonvulsant phenytoin upon parental administration. Phenytoin exerts its effect most likely through an enhancement of sodium efflux from neurons in the motor cortex. This leads to a suppression of excessive neuronal firing and spread of seizure activity. Other physiologic effects from actions of phenytoin include modulation of the voltage-dependent calcium channels of neurons, inhibition of calcium flux across neuronal membranes and enhancement of sodium-potassium ATPase activity of neurons and glial cells.
fosquidone: A water-soluble pentacyclic pyrolloquinone analogue of mitoquidone with potential antineoplastic activity. Currently, the mechansim of action of fosquidone is unknown. In vitro studies indicate that this agent does not bind to DNA or inhibit topoisomerases.
fostamatinib disodium: An orally available disodium salt of the Syk kinase inhibitor fostamatinib with potential anti-inflammatory and immunomodulating activities. Fostamatinib inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage. Syk kinase, widely expressed in hematopoietic cells, is a nonreceptor tyrosine kinase that is involved in coupling activated immunoreceptors to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis.
fostriecin: An anti-tumor antibiotic isolated from the bacterium Streptomyces pulveraceus. Fostriecin inhibits topoisomerase II catalytic activity, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis in various malignant cell types. This agent also inhibits serine/threonine protein phosphatase type 2A in some tumor cell types, thereby interfering with cellular proliferation and differentiation.
fotemustine: A chloroethylating nitrosourea with antineoplastic activity. Fotemustine alkylates guanine by forming chloroethyl adducts at the 6 position of guanine, resulting in N1-guanine and N3-cytosine cross linkages, inhibition of DNA synthesis, cell cycle arrest, and finally apoptosis. This agent is lipophilic and crosses the blood-brain barrier.
Fotivda: (Other name for: tivozanib hydrochloride)
fowlpox virus vaccine vector: A recombinant fowlpox virus-based vaccine vector designed to express various tumor-associated peptide antigens. Strong CD8 cytotoxic T cell responses may be induced after prolonged immunization with fowlpox virus vaccines and have been associated with tumor regression. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it does not multiply in human tissues.
fowlpox-NY-ESO-1 vaccine: A cancer vaccine consisting of a recombinant fowlpox virus vector encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1, an antigen found in normal testis and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. Vaccination with NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis.
FPV vaccine CV301: A cancer vaccine consisting of a recombinant fowlpox viral (FPV) vector encoding both the two human tumor-associated antigens (TAAs) carcinoembryonic antigen (CEA) and mucin-1 (MUC-1), and TRICOM, which is comprised of the three human immune-enhancing co-stimulatory molecules B7-1, ICAM-1 and LFA-3, with potential immunostimulatory and antineoplastic activities. Upon subcutaneous administration following the administration of a proprietary modified vaccinia Ankara developed by Bavarian Nordic-based prime vaccine MVA-BN-CV301, the FPV vaccine CV301, which is used as a booster vaccine, activates a cytotoxic T-lymphocyte (CTL) response against CEA- and MUC-1-expressing tumor cells. In addition, the CV301-dependent anti-tumor CTL response upregulates the expression of programmed cell death ligand 1 (PD-L1); therefore, when FPV-CV301 is combined with a programmed cell death 1 (PD-1) immune checkpoint inhibitor, the antitumor effect may be increased. The TAAs CEA and MUC-1 are overexpressed in a variety of cancers.
FPV-brachyury-TRICOM vaccine: A cancer vaccine consisting of a recombinant fowlpox viral (FPV) vector encoding the human transcription factor and tumor-associated antigen (TAA) brachyury, and a triad of T-cell co-stimulatory molecules (TRICOM), which is comprised of the three human immune-enhancing co-stimulatory molecules B7-1, ICAM-1 and LFA-3, with potential immunostimulatory and antineoplastic activities. Upon subcutaneous administration occurring after the administration of a proprietary modified vaccinia Ankara developed by Bavarian Nordic-based prime vaccine (MVA-BN-brachyury), the booster vaccine FPV-brachyury vaccine potentiates a cytotoxic T-lymphocyte (CTL) response against brachyury-expressing tumor cells. The expression of brachyury, a member of the T-box family of transcription factors that is overexpressed in numerous cancer cell types, is correlated with increased epithelial-mesenchymal transition (EMT), cancer resistance, cancer progression and metastasis. TRICOM enhances antigen-specific T-cell activation.
FR Alpha/TRPV6 bispecific ligand drug conjugate CBP-1008: A bispecific ligand drug conjugate targeting both human folate receptor alpha (FR alpha; FOLR1) and transient receptor potential cation channel subfamily V member 6 (TRPV6; CaT1; CATL) and conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration of FR alpha/TRPV6 bispecific ligand drug conjugate CBP-1008, the bispecific ligand moiety targets and binds to FR alpha and/or TRPV6, which are overexpressed in certain tumor types. After internalization of the agent, the MMAE moiety is released and binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and apoptosis. This inhibits the proliferation of tumor cells expressing FR alpha and/or TRPV6. FR alpha is a high-affinity folate-binding protein and a member of the folate receptor family; it is overexpressed in certain tumor types. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective for calcium compared to other cations; it is overexpressed in a variety of tumors and initiates tumor cell growth, proliferation and metastases.
Fragmin: (Other name for: dalteparin sodium)
Fragmin V: (Other name for: dalteparin sodium)
freeze-dried black raspberry bioadhesive gel: A bioadhesive gel containing 10% freeze-dried black raspberries (FBR) with potential chemopreventive and antioxidant activities. The four main constituent black raspberry anthocyanins that contribute significantly to the chemopreventive effects are cyanidin 3-glucoside (C3GLU), cyanidin 3-rutinoside (C3RUT), cyanidin 3-sambubioside (C3SAM) and cyanidin 3-(2(G)-xylosyl) rutinoside (C3XRUT). Upon mucosal application, the anthocyanins from the gel penetrate the oral mucosa and are able to modulate expression of certain proapoptotic and terminal differentiation genes, and reduce the expression of epithelial cyclooxygenase-2 (COX-2) protein. In addition, this gel may also reduce vascular densities in the superficial connective tissues.
French maritime pine bark extract: A nutritional supplement containing an extract obtained from the French maritime pine bark Pinus pinaster, with potential immunomodulating and antioxidant activities. The French maritime pine bark extract contains high amounts of the phytochemicals proanthocyanidins. Proanthocyanidins are able to scavenge free radicals, and therefore may inhibit cellular damage. This extract may also ameliorate the symptoms of lymphedema and improve blood flow. It might also stimulate the immune system and have antioxidant effects.
fresolimumab: A pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) -beta 1, 2 and 3 with potential antineoplastic activity. Fresolimumab binds to and inhibits the activity of all isoforms of TGF-beta, which may result in the inhibition of tumor cell growth, angiogenesis, and migration. TGF-beta, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells.
fructooligosaccharide supplement: A supplement containing oligosaccharide fructans, with gastrointestinal (GI) protective and immumopotentiating activities. Upon oral administration of the supplement, the oligosaccharides stimulate the growth of certain GI bacteria and activate the immune system. This improves the intestinal microflora, strengthens the immune system and increases the protective function of the GI barrier.
fructooligosaccharide/Lactobacillus paracasei/Lactobacillus rhamnosus/Lactobacillus acidophilus/Bifidobacterium lactis: A synbiotic nutritional supplement containing fructooligosaccharides (FOS), which are linear chains of fructose units that are linked by beta (2-1) bonds, and probiotic cultures of Lactobacillus paracasei (L. paracasei), L. rhamnosus, L. acidophilus and Bifidobacterium lactis (B. lactis), with gastrointestinal (GI) protective and immunomodulating activities. Upon oral administration, the bacteria in this probiotic supplement help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier that helps maintain the integrity of the epithelial barrier. This will interfere with the attachment of pathogenic bacteria and other harmful substances, prevent inflammation and improve GI function. Additionally, the reconstituted microflora may metabolize FOS, which may promote calcium mobilization into the bloodstream by maintaining a neutral pH in the lower gut.
fruit and vegetable extracts: Extracts from fruits and vegetables that contain fiber, vitamins, minerals, and other natural substances with antioxidant, lipid-lowering, and antiproliferative properties. Used in chemoprevention therapy, these extracts may prevent the development or recurrence of cancer.
fruquintinib: An orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, fruquintinib inhibits VEGF-induced phosphorylation of VEGFRs 1, 2, and 3 which may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death. Expression of VEGFRs may be upregulated in a variety of tumor cell types.
Fruzaqla: (Other name for: fruquintinib)
Fu Zheng Jie Du Hua Yu: A traditional Chinese medicine (TCM) formulation composed of multiple herbs that may reverse hepatic fibrosis and improve liver function in patients with chronic hepatitis B (HBV), liver cirrhosis and hepatocellular carcinoma.
FU-LV regimen: A regimen consisting of fluorouracil and leucovorin, used in both the adjuvant and metastatic disease setting, for the treatment of colorectal cancer. This regimen is also combined with radiation for the treatment of gastric and esophageal cancer.
fucosylated umbilical cord blood regulatory T cells: Fucosylated, human umbilical cord blood (UCB)-derived regulatory T cells (Tregs), with potential immunomodulating activity. Ex vivo, Tregs are isolated from cord blood, expanded, and fucosylated. Upon infusion, the fucosylated UCB Tregs modulate immune responses and induce tolerance to allogeneic transplants, such as hematopoietic stem cell transplants (HSCTs). This suppresses graft-versus-host disease (GVHD). Fucosylation improves the activity of Tregs and reduces the amount of Tregs that need to be expanded and infused.
FUDF: (Other name for: floxuridine)
Fulphila: (Other name for: pegfilgrastim)
fulranumab: A monoclonal antibody directed against nerve growth factor (NGF) with potential analgesic activity. Upon administration, fulranumab binds to NGF, preventing its binding to and activation of the NGF receptors TrkA and p75NTR. Inhibition of the NGF pathway may prevent the perception of pain and may induce analgesia. NGF, a neurotrophic factor that plays a key role in neuropathic and inflammatory-induced pain, promotes hyperalgesia and allodynia.
fulvestrant: A synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines.
Fulyzaq: (Other name for: crofelemer)
fumagillin-derived polymer conjugate XMT-1107: A polymeric prodrug consisting of the fumagillol-derived small molecule XMT-1191 tethered to the hydrophilic, biodegradable70 kDa polymer poly[1- hydroxymethylethylene hydroxymethylformal] (PHF) with potential antiangiogenic and antineoplastic activities. Upon administration, fumagillin-derived polymer conjugate XMT-1107 releases XMT-1191, which may inhibit angiogenesis through the irreversible inhibition of the methionine aminopeptidase 2 (METAP2); although the exact mechanism of action has yet to be fully elucidated, this agent appears to induce cell cycle arrest in endothelial cells, inhibiting their proliferation and migration. Compared to an unconjugated fumagillin analog, XMT-1107 exhibits improved solubility and an extended half life due to its PHF backbone. METAP2, a member of the methionyl aminopeptidase family, binds two cobalt or manganese ions and protects the alpha subunit of eukaryotic initiation factor 2 (EIF2) from inhibitory phosphorylation by removing the amino-terminal methionine residue from nascent protein; this aminopeptidase may be overexpressed in a variety of tumor cell types.
Fungizone: (Other name for: amphotericin B deoxycholate)
fuorescence imaging agent IC2000: A fluorescent imaging agent that can potentially be used as a diagnostic imaging agent.
furazolidone: A nitrofuran antimicrobial agent used in the treatment of diarrhea or enteritis caused by bacteria or protozoan infections. Furazolidone is also active in treating typhoid fever, cholera and salmonella infections.
furosemide: A sulfamoylanthranilic acid derivative, also known as frusemide, and potent loop diuretic. Furosemide is widely used to treat hypertension and edema. This agent is highly bound to albumin and is largely excreted unchanged in the urine.
furosemide topical gel CLS006: A sulfamoylanthranilic acid derivative and loop diuretic, with potential antiviral activity. Upon topical administration, furosemide gel inhibits potassium influx by interacting with cell membrane ion co-transporter, Na+-K+-2Cl-co-transporter-1(NKCC1; SLC12A2). This may inhibit potassium influx and prevent the replication of DNA viruses, such as human papillomavirus (HPV), that rely on potassium for replication.
furosemide/digoxin topical gel CLS003: A topical ionic contra-viral therapy (ICVT) gel-based formulation that combines furosemide, a sulfamoylanthranilic acid derivative and loop diuretic, and digoxin, a cardiac glycoside, with potential antiviral activity. Upon topical administration, furosemide interacts with the cell membrane ion co-transporter, Na+-K+-2Cl-co-transporter-1(NKCC1; SLC12A2) and digoxin reversibly inhibits the sodium/potassium-transporting ATPase, leading to a decrease in potassium influx. This may prevent the replication of certain DNA viruses including human papillomavirus (HPV), that rely on potassium for replication.
Furoxone: (Other name for: furazolidone)
fursultiamine: A nutritional supplement and vitamin B1 derivative, with potential antineoplastic activity. Upon oral administration, fursultiamine inhibits the expressions of octamer-binding transcription factor 4 (OCT-4), SRY (sex determining region Y)-box 2 (SOX-2), and Nanog homeobox (NANOG) in cancer stem cells (CSCs). This may inhibit the proliferation of CSCs thereby preventing tumor cell growth. In addition, fursultiamine inhibits the expression of ATP-binding cassette (ABC) transporters subfamily B member 1 (ABCB1) and subfamily G member 2 (ABCG2) in cancer CSCs, which may abrogate resistance to chemo- and radiotherapy in CSCs. CSCs promote tumor initiation, progression and metastasis; they play a key role in cancer recurrence and resistance to chemotherapy and radiation.
fusidic acid/betamethasone valerate topical cream: A topical cream formulation of the bacteriostatic antibiotic fusidic acid and the synthetic, long-acting glucocorticoid betametasone valerate with potential anti-bacterial and immunomodulating activities. Fusidic acid/betamethasone valerate topical cream inhibits Gram-positive bacterial protein synthesis and replication and inhibits the inflammatory response by preventing phospholipid release, inhibiting eosinophil activity, and decreasing pro-inflammatory cytokine production.
Fusilev: (Other name for: levoleucovorin calcium)
futermestotug: A recombinant, humanized immunoglobulin (Ig) G1 monoclonal antibody directed against the human T-cell-expressed receptor cytotoxic T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4; CD152), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, futermestotug targets and binds to CTLA-4 expressed on T cells and inhibits the CTLA-4-mediated downregulation of T-cell activation. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells, thereby killing cancer cells. CTLA-4, an inhibitory receptor and member of the immunoglobulin superfamily (IgSF), plays a key role in the downregulation of the immune system.
futibatinib: An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. Futibatinib selectively and irreversibly binds to and inhibits FGFR, which may result in the inhibition of both the FGFR-mediated signal transduction pathway and tumor cell proliferation, and increased cell death in FGFR-overexpressing tumor cells. FGFR is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival and its expression is upregulated in many tumor cell types.
futuximab: A recombinant, chimeric monoclonal antibody directed against the epidermal growth factor receptor (EGFR; ErbB1; HER1), with potential antineoplastic activity. Upon administration, futuximab targets and binds to an epitope located in the extracellular domain (ECD) of EGFR, which causes internalization and degradation of EGFR, including the mutated EGFR variant III (EGFRvIII). This prevents EGFR-mediated signaling, thereby inhibiting EGFR-dependent tumor cell proliferation. EGFR, a receptor tyrosine kinase, is overexpressed on the cell surfaces of various solid tumor cell types.
futuximab/modotuximab mixture: A mixture of two recombinant IgG1 antibodies directed against different epitopes in the epidermal growth factor receptor (EGFR) extracellular domain III, with potential antineoplastic activity. Anti-EGFR monoclonal antibody mixture Sym004 binds to the extracellular domain of EGFR, thereby preventing ligand binding. This may prevent activation and subsequent dimerization of the receptor; the decrease in receptor activation may result in an inhibition of downstream ERK and JNK signaling pathways and thus inhibition of EGFR-dependent tumor cell proliferation and metastasis. In addition, binding of Sym004 to EGFRs causes EGFR internalization and degradation. EGFR, a receptor tyrosine kinase, often is overexpressed on the cell surfaces of various solid tumor cell types.
fuzheng yiliu decoction: A traditional Chinese medicine (TCM) formulation composed of many different herbs, including Raw land, Zhimu, raw jaundice, fairy spleen, Bayu Tian, Quanqi, Atractylodes, Poria, Licorice, Cork, American ginseng, Tortoiseshell, and Hedyotis diffusa, with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon administration of fuzheng yiliu decoction, the active ingredients may inhibit several tumor signaling pathways, may induce apoptosis in tumor cells and inhibit tumor cell proliferation. It may also modulate the immune system and may induce anti-tumor immune responses by increasing natural killer cells (NKs), lymphocytes, and certain cytokines.
fuzuloparib: An orally available inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2, with potential antineoplastic activity. Upon oral administration, fuzuloparib inhibits PARP 1 and 2 activity, which inhibits PARP-mediated repair of damaged DNA via the base excision repair (BER) pathway, enhances the accumulation of DNA strand breaks, promotes genomic instability, and leads to an induction of apoptosis. The PARP family of proteins catalyze post-translational ADP-ribosylation of nuclear proteins, which then transduce signals to recruit other proteins to repair damaged DNA. PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance.
Fyarro: (Other name for: sirolimus protein-bound nanoparticles)
Fycompa: (Other name for: perampanel)