F 18 fluorodeoxygalactose
A radioconjugate containing the galactose analogue 2-deoxy-2-fluoro-D-glucose (FDGal) that contains 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.
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.
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.
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 PF-04554878
An orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. The tyrosine kinase FAK is , a signal transducer for integrins that is upregulated in many tumor cell types and is involved in tumor cell invasion, migration and proliferation.
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.
(Other name for: toremifene)
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.
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.
(Other name for: tinidazole)
(Other name for: piroxicam)
(Other name for: conjugated estrogens)
(Other name for: ethinyl estradiol)
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.
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 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 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.
(Other name for: fentanyl citrate buccal tablet)
(Other name for: ferumoxytol)
(Other name for: ferumoxides injectable solution)
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.
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.
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.
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
FGFR inhibitor AZD4547
An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor AZD4547 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.
FGFR1 receptor antagonist FP-1039
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.
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.
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.
(Other name for: prasterone)
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.
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.
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.
(Other name for: sodium biphosphate/sodium phosphate oral laxative)
(Other name for: fluticasone propionate)
(Other name for: tegafur)
(Other name for: fludrocortisone acetate)
(Other name for: fluticasone propionate)
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.
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.
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.
(Other name for: trivalent influenza vaccine)
A synthetic glucocorticoid and derivative of fluocinolone acetonide with anti-inflammatory and antipruritic activities. Fluocinonide binds the glucocorticoid receptor, followed by translocation of the ligand-receptor complex to the nucleus and transcription activation of genes containing glucocorticoid-responsive elements. Lipocortin-1 is one factor induced by fluocinonide that interacts and inhibits cytosolic phospholipase 2 alpha, thereby preventing phospholipase translocation to the perinuclear membrane and subsequent release and conversion of arachidonic acid to inflammatory prostaglandins. In addition, MAPK phosphatase 1 is induced, thereby preventing the triggering of the MAPK cascade resulting in pro-inflammatory effects via Jun N-terminal kinase and c-Jun. Finally, fluocinonide binds to and inhibits nuclear factor kappa-B directly, resulting in inhibition of cyclooxygenase 2 transcription and subsequent prostaglandin synthesis.
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.
(Other name for: fluorescein sodium injection)
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 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 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 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 fluorodopa
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.
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 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 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 RGD-based integrin peptide-polymer AH111585
A small synthetic peptide containing an RGD-sequence (Arg-Gly-Asp) attached to 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 fluorine F 18 RGD-based integrin peptide-polymer AH111585 selectively binds to the alphaVbeta3 integrin receptor, commonly upregulated on the surfaces of tumor cells and tumor vasculature endothelial cells. This agent may be of use in visualizing and quantifying a decrease in tumor vascularity in response to antiangiogenic agents.
fluorine F 18 sodium fluoride
A radiopharmaceutical consisting of the sodium salt of fluorine F 18 fluoride with radioisotopic and bone mineralizing activities. Fluoride binds to calcium ions in hydroxyapatite crystals in bone. The uptake and incorporation of positron-emitting fluorine F 18 fluoride into bone can be imaged using positron emission tomography (PET) or single-photon emission computed tomography (SPECT), allowing visualization of malignant bone lesions in which regional blood flow and bone turnover are increased.
(Other name for: tegafur)
(Other name for: fluorouracil)
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.
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.
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.
(Other name for: tarenflurbil)
(Other name for: trivalent influenza vaccine)
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.
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.
(Other name for: trivalent influenza vaccine)
(Other name for: trivalent influenza vaccine)
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 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.
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.
folate-vinca alkaloid conjugate EC145
A water-soluble, folate-receptor-targeted conjugate of folate and the vinca alkaloid desacetylvinblastine monohydrazide (DAVLBH) with potential antineoplastic activity. The folate moiety of folate-vinca alkaloid conjugate EC145 binds to folic acid receptors on the tumor cell surface and the agent is internalized via folate receptor-mediated endocytosis, delivering the tubulin-binding DAVLBH moiety directly into the tumor cell; DAVLBH binding to tubulin results in the disruption of microtubule assembly-disassembly dynamics, cell cycle arrest, and tumor cell apoptosis. Folic acid receptors are frequently upregulated on the surfaces of many tumor cell types. DAVLBH is a derivative of the natural product vinblastine.
(Other name for: methotrexate)
(Other name for: methotrexate)
(Other name for: recombinant human chorionic gonadotropin)
(Other name for: diethylstilbestrol)
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.
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.
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.
(Other name for: ceftazidime sodium)
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/?-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.
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.
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.
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.
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.
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.
A cancer vaccine consisting of a recombinant fowlpox virus encoding human prostate-specific antigen (PSA) and TRICOM, a combination of three immunostimulants (i.e., B7.1, ICAM-1, and LFA-3). Administration of this agent may induce a cytotoxic T cell response against PSA-expressing tumor cells. Dendritic cells infected with TRICOM vectors greatly enhance naive T-cell activation and peptide-specific T-cell stimulation. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
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.
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, whcih 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.
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.
(Other name for: floxuridine)
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.
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.