(Other name for: estramustine phosphate sodium)
A liposome-encapsulated peptide vaccine consisting of a synthetic peptide derived from the mucin 1 (MUC-1) antigen with potential antineoplastic activity. Upon vaccination, emepepimut-S may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against MUC-1-expressing tumor cells, resulting in growth inhibition. MUC-1 antigen is a high-molecular-weight transmembrane glycoprotein that is overexpressed on the cell surfaces of many epithelial tumor cells as well as on the cell surfaces of some B-cell lymphoma cells and multiple myeloma cells.
(Other name for: hydrocortisone sodium succinate)
(Other name for: acetylsalicylic acid)
A synthetic fluoro derivative of thiacytidine with potent antiviral activity. Emtricitabine is phosphorylated to form emtricitabine 5'-triphosphate within the cell. This metabolite inhibits the activity of human immunodeficiency virus (HIV) reverse transcriptase both by competing with the natural substrate deoxycytidine 5'-triphosphate and by incorporation into viral DNA causing a termination of DNA chain elongation (due to the lack of the essential 3'-OH group).
(Other name for: emtricitabine)
(Other name for: enalapril maleate)
The maleate salt form of enalapril, a dicarbocyl-containing peptide and angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, enalapril is converted by de-esterification into its active form enalaprilat. Enalaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Enalapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.
A humanized monoclonal antibody directed against the tumor necrosis factor-like weak inducer of apoptosis receptor (TWEAKR) with potential antineoplastic, immunomodulating and antiangiogenic activities. Enavatuzumab binds to TWEAKR and inhibits TWEAK ligand binding and activation of NF-kappaB-mediated cytokine release, which may result in tumor cell apoptosis. TWEAKR is a cell-surface receptor with homology to tumor necrosis factor receptors. Upon binding with its ligand, TWEAKR has been shown to stimulate cytokine release and cell proliferation, migration, and survival; it may also promote apoptosis under some conditions. This receptor may be overexpressed in a variety of tumors including those of the pancreas, colon, lung, kidney, and breast.
(Other name for: etanercept)
The orally bioavailable citrate salt of enclomiphene, the trans-isomer of the nonsteroidal triphenylethylene compound clomiphene, with tissue-selective estrogenic and antiestrogenic activities. As a selective estrogen receptor modulator (SERM), enclomiphene binds to hypothalamic estrogen receptors, blocking the negative feedback of endogenous estrogens and stimulating the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus; released GnRH subsequently stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary, resulting in ovulation. In addition, this agent may bind to estrogen receptors on breast cancer cells, resulting in the inhibition of estrogen-stimulated proliferation in susceptible cell populations.
(Other name for: progesterone vaginal insert)
endothelin B receptor agonist SPI-1620
A highly selective peptide agonist of the endothelin-B receptor. Endothelin B receptor agonist SPI-1620 binds to endothelin-B receptors on endothelial cells in tumor blood vessels, which, unlike the angioarchitecture of normal blood vessels, are relatively devoid of smooth muscle. This agent may induce a transient, selective increase in blood flow to a tumor, which may result in an increase in the delivery of anticancer agents to the tumor and, so, an increase in anticancer agent efficacy.
(Other name for: hepatitis B vaccine (recombinant))
(Other name for: Detox-B adjuvant)
A chimeric monoclonal antibody against human colorectal and pancreatic carcinoma-associated antigens (CPAAs) with potential immunomodulating and anti-tumor activities. Ensituximab binds to CPAAs, which may activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response and an antibody-dependent cellular cytotoxicity (ADCC) response against CPAA-expressing tumor cells. CPAAs, cell surface proteins, are upregulated on colon and pancreatic tumor cells. Ensituximab contains the variable region of the heavy and light chain of murine NPC-1 and linked in-frame to constant regions of a human IgG1 isotype.
A synthetic analog of 2-deoxyguanosine with antiviral activity against hepatitis B virus (HBV). Entecavir is activated in vivo to a 5-triphosphate metabolite. In turn, the triphosphate form competes with the natural substrate deoxyguanosine triphosphate (dGTP) for incorporation into viral DNA. The incorporation of the activated triphosphate metabolite of entecavir inhibits the reverse transcriptase (RT) viral RNA-dependent HBV DNA polymerase and, so, the replication of viral DNA and transcription.
(Other name for: alvimopan)
enteric-coated TRPM8 agonist D-3263 hydrochloride
An enteric-coated orally bioavailable formulation of the hydrochloride salt of a small-molecule agonist for transient receptor potential melastatin member 8 (TRPM8 or Trp-p8) with potential antineoplastic activity. The active ingredient in enteric-coated TRPM8 agonist D-3263 hydrochloride binds to and activates TRPM8, which may result in an increase in calcium and sodium entry; the disruption of calcium and sodium homeostasis; and the induction of cell death in TRPM8-expressing tumor cells. This agent may decrease dihydrotestosterone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and BPH. TRPM8 is a transmembrane calcium channel protein that is normally expressed in prostate cells and appears to be overexpressed in benign prostatic hyperplasia (BPH) and in prostate cancer.
enteric-coated zoledronic acid tablet MER-101
An oral tablet formulation containing zoledronic acid combined with a proprietary absorption enhancer for improved zoledronic acid gastrointestinal absorption with anti-bone-resorption activity. The third-generation bisphosphonate zoledronic acid binds to hydroxyapatite crystals in the bone matrix, slowing their dissolution and inhibiting the formation and aggregation of these crystals. This agent also inhibits farnesyl pyrophosphate synthase, an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids, donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which are important in the process of osteoclast turnover. The proprietary absorption enhancer is a GRAS (generally-recognized-as-safe) food additive.
(Other name for: acetylsalicylic acid)
(Other name for: apaziquone)
(Other name for: gadoxetate disodium)
(Other name for: ketamine/amitriptyline NP-H cream)
(Other name for: carbamazepine)
(Other name for: lamivudine)
(Other name for: epoetin alfa)
A second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration, and reduced CNS exposure. In addition, epothilone KOS-1584 is a poor substrate for the P-glycoprotein (P-gp) drug efflux pump.
(Other name for: epoetin alfa)
ERa36 modulator icaritin
A metabolite of A metabolite of icariin, a principal flavonoid glycoside in Herba Epimedii (a traditional Chinese medicine herb used in treating osteoporosis) with potential antineoplastic activity. ERa36 modulator icaritin selectively binds to a novel variant of estrogen receptor alpha, a36, and mediates a membrane-initiated "nongenomic" signaling pathway, which is linked to activated signaling pathways like the MAPK/ERK and the PI3K/Akt pathways. This agent induces cell cycle arrest at G1, or G2/M arrest depending upon the dose. Consistently with G1 arrest, icaritin increases protein expressions of pRb, p27(Kip1) and p16(Ink4a), while decreasing phosphorylated pRb, Cyclin D1 and CDK4. Forty percent of ER-negative breast cancer tumors express high levels of ERa36, and this subset of patients is less likely to benefit from tamoxifen treatment compared with those with ERa66-positive/ERa36-negative tumors.
erastin analogue PRLX 93936
A structural analogue of erastin with potential antineoplastic activity. Erastin analogue PRLX 93936 appears to inhibit mitochondrial outer membrane protein VDACs (voltage-dependent anion channels) 2 and 3, resulting in an oxidative, non-apoptotic cell death. Erastin analogue PRLX 93936 exhibits greater lethality in cell lines harboring mutations in the GTPase protein oncogenes HRAS and KRAS or the serine-threonine protein kinase oncogene BRAF than in non-tumorigenic cell lines. VDACs 2 and 3 are up-regulated in a wide variety of tumor cell lines.
(Other name for: anidulafungin)
erbB kinase inhibitor AZD8931
An erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. erbB kinase inhibitor AZD8931 binds to and inhibits erbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing erbB. The erbB protein family, also called the epidermal growth factor receptor (EGFR) family, plays major roles in tumor cell proliferation and tumor vascularization.
ErbB-2 inhibitor ARRY-380
An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. ErbB-2 inhibitor ARRY-380 selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.
ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.
(Other name for: levamisole hydrochloride)
The mesylate salt of a synthetic analogue of halichondrin B, a substance derived from a marine sponge (Lissodendoryx sp.) with antineoplastic activity. 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, potentially, tumor regression.
An orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Erismodegib selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway and, so, the inhibition of tumor cells in which this pathway is abnormally activated. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Inappropriate activation of Hh pathway signaling and uncontrolled cellular proliferation, as is observed in a variety of cancers, may be associated with mutations in the Hh-ligand cell surface receptor Smo.
The tetrasodium salt of a synthetic analogue of the lipid A portion of the endotoxin lipopolysaccharide (LPS) with potential immunomodulating activity. Eritoran binds to the Toll-like receptor (TLR)/CD14/MD2 receptor complex present on most cells of the immune system, inhibiting the activation of the receptor complex by LPS, which may result in the inhibition of pro-inflammatory cytokine secretion and a potentially fatal systemic inflammatory response syndrome (SIRS). LPS is found in the outer membrane of Gram-negative bacteria and binds to the TLR/CD14/MD2 receptor complex of immune cells, especially macrophages, resulting in the release of pro-inflammatory cytokines.
The sodium salt of ertapenem, a 1-beta-methyl carbapenem and a broad-spectrum beta-lactam antibiotic with bactericidal activity. Ertapenem binds to penicillin binding proteins (PBPs) located on the bacterial cell wall, in particular PBPs 2 and 3, thereby inhibiting the final transpeptidation step in the synthesis of peptidoglycan, an essential component of the bacterial cell wall. Inhibition of peptidoglycan synthesis results in weakening and lysis of the cell wall and cell death. In vitro, this agent has shown activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Erapenem is resistant to hydrolysis by a variety of beta-lactamases, including penicillinases, cephalosporinases and extended-spectrum beta-lactamases.
A murine monoclonal antibody with two antigen-recognition sites: one for CD3, an antigen expressed on mature T cells, and one for HER-2-neu, a tumor-associated antigen that promotes tumor growth. Ertumaxomab attaches to CD3-expressing T cells and HER-2-neu-expressing tumor cells, selectively cross-linking tumor and immunologic cells which results in the recruitment of cytotoxic T cells to the T cell/tumor cell aggregate.
(Other name for: asparaginase-Erwinia)
(Other name for: erythromycin)
(Other name for: erythromycin)
A broad-spectrum, topical macrolide antibiotic with antibacterial activity. Erythromycin diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved.
erythromycin topical cream
A topical cream formulation containing the broad-spectrum macrolide antibiotic erythromycin with anti-bacterial activity. Erythromycin interacts with the 50S subunit of the bacterial 70S ribosomal RNA complex resulting in the inhibition of protein synthesis and bacterial cell death.
The oxalate salt of escitalopram, a pure S-enantiomer of the racemic bicyclic phthalane derivative citalopram, with antidepressant activity. As a selective serotonin reuptake inhibitor (SSRI), escitalopram blocks the reuptake of serotonin by neurons in the central nervous system (CNS), thereby potentiating CNS serotonergic activity.
(Other name for: lithium carbonate)
A synthetic derivative of the anthracycline antineoplastic antibiotic doxorubicin with potential antineoplastic activity. Esorubicin intercalates into DNA and inhibits topoisomerase II, thereby inhibiting DNA replication and ultimately, interfering with RNA and protein synthesis. This agent exhibits less cardiotoxicity than the parent antibiotic doxorubicin, but may cause more severe myelosupression compared to other compounds within the anthracycline class.
(Other name for: ethinyl estradiol)
(Other name for: therapeutic estradiol)
estradiol vaginal ring
A flexible elastomer ring containing 17 beta-estradiol used for estrogen replacement. Upon vaginal insertion, estradiol vaginal ring releases a consistent low-dose of estrogen which binds to and activates nuclear receptors in estrogen-responsive tissues. By increasing the amount of estradiol locally, symptoms of vaginal dryness or decreased sexual interest may improve. 17 beta-estradiol is the major naturally occurring estrogen produced in the ovaries of premenopausal women.
The parenterally-administered synthetic valerate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. This agent exhibits mild anabolic and metabolic properties, and increases blood coagulability.
estradiol/norethindrone acetate tablet
An orally bioavailable tablet formulation containing the semisynthetic estrogen estradiol in combination with the acetate form of the synthetic progestin norethindrone, with estrogenic and progesteronic activities. Estradiol binds to and activates intracellular estrogen receptors found in the reproductive tract and other estrogen-responsive tissues. The activated complex enters the nucleus, binds to the estrogen response elements on DNA, and activates the transcription of genes involved in the maintenance of the female reproductive system and secondary sexual characteristics, the proliferation of the endometrium, and bone metabolism. Norethindrone binds to the intracellular progesterone receptors in the reproductive system and the activated ligand/receptor complex interacts with specific DNA response elements, resulting in an alteration in protein synthesis; inhibition of luteinizing hormone (LH) and follicle stimulating hormone (FSH) release; inhibition of ovulation; an increase in cervical mucus production; and induction of the secretory phase of the endometrial cycle.
Administration of estradiol/norethindrone acetate may abrogate vasomotor symptoms associated with menopause and prevent bone loss associated with the postmenopause. Because chronic estrogen stimulation unopposed by progesterone may increase the risk of endometrial carcinoma, administration of a combination estrogen-progestin in postmenopause may reduce the risk for women who require estrogen replacement therapy.
estramustine phosphate sodium
The orally available disodium salt, monohydrate, of estramustine phosphate, a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. This agent also exhibits anti-androgenic effects.
(Other name for: estradiol vaginal ring)
(Other name for: diethylstilbestrol)
(Other name for: transdermal estrogen)
estrogen receptor agonist GTx-758
An orally available, nonsteroidal selective estrogen receptor (ER) alpha agonist with potential antineoplastic activity. Upon administration of GTx-758, this agent suppresses the secretion of the gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH) by the pituitary gland through feedback inhibition. In males, the inhibition of LH secretion prevents the synthesis of androgens, including testosterone, by the testes. This may result in suppressed total serum testosterone to the levels observed in castration.
(Other name for: diethylstilbestrol)
(Other name for: Polo-like kinase 1 inhibitor ON 01910.Na)
A nonbenzodiazepine cyclopyrrolone and active dextrorotatory stereoisomer of zopiclone with hypnotic and sedative activities and without significant anxiolytic activity. Although the exact mechanism of action remains to be fully elucidated, eszopiclone binds to and activates the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization and inhibition of neuronal firing, which may result in a hypnotic effect and the induction of sleep.
An aryloxy-acetic acid derivative belonging to the class of loop diuretics. Ethacrynic acid interferes with the chloride binding site of the Na+, K+, Cl- cotransporter system in the thick ascending loop of Henle, thereby inhibiting the reabsorption of sodium, potassium, and chloride ions. This leads to an increase in the excretion of sodium, potassium, chloride, calcium, and water.
An antibiotic with bacteriostatic, antimicrobial and antitubercular properties. Ethambutol interferes with the biosynthesis of arabinogalactan, a major polysaccharide of the mycobacterial cell wall. It inhibits the polymerization of cell wall arabinan of arabinogalactan and lipoarabinomannan by blocking arabinosyl transferases and induces the accumulation of D-arabinofuranosyl-P-decaprenol, an intermediate in arabinan biosynthesis. This results in halting bacterial growth.
A colorless organic liquid also known as ethyl alcohol or grain alcohol. Ethanol's primary physiologic effects involve the central nervous system. Depending on the dose delivered, ethanol behaves as an anxiolytic, a depressant, or a general anesthetic. Ethanol-induced immunosuppression involves dysregulation of CD4+ T cells.
(Other name for: ethinyl estradiol)
A semisynthetic estrogen. Ethinyl estradiol binds to the estrogen receptor complex and enters the nucleus, activating DNA transcription of genes involved in estrogenic cellular responses. This agent also inhibits 5-alpha reductase in epididymal tissue, which lowers testosterone levels and may delay progression of prostatic cancer. In addition to its antineoplastic effects, ethinyl estradiol protects against osteoporosis. In animal models, short-term therapy with this agent has been shown to provide long-term protection against breast cancer, mimicking the antitumor effects of pregnancy.
A synthetic iodine addition product of the ethyl ester of the fatty acids of poppyseed oil. Ethiodized oil contains 37% organically bound iodine and is used as a diagnostic radiopaque medium or, labeled with I-131, as an antineoplastic agent. Selectively retained in tumor vessels for long periods, ethiodized oil is used for imaging organs such as liver, lung, stomach, and thyroid. Labeled with I-131 or other beta emitters (Y-90 or P-32), ethiodol can deliver a high internal radiation dose to certain tumors with minimal effect on healthy tissues.
A succinimide with anticonvulsant activity. The exact mechanism of action is not entirely understood, but most likely ethosuximide exerts its effects by partial antagonism of T-type calcium channels of the thalamic neurons. This leads to a decrease in burst firing of thalamocortical neurons, which stabilizes the nerve activity in the brain and prevents seizures.
(Other name for: amifostine trihydrate)
(Other name for: buserelin)
A pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. Etodolac inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.
A synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic ,and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.
(Other name for: hycanthone)
(Other name for: acitretin)
(Other name for: flutamide)
(Other name for: cevimeline hydrochloride)
ex vivo-expanded HER2-specific T cells
T cells specific for the human epidermal growth factor receptor 2 (HER2) with potential immunopotentiating activity. T cells directed against HER2, overexpressed on many tumor cells, are collected from HER2-expressing tumor tissue, expanded ex vivo and, then re-introduced in the patient. Re-introduction of ex vivo-expanded HER2-specific T cells may enhance the cytotoxic T cell response against tumor cells overexpressing HER2, resulting in inhibition of tumor growth.
(Other name for: ADH-1)
(Other name for: acetylsalicylic acid)
The hydrochloride salt of a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity. After intracellular de-esterification, the active form of ezatiostat binds to and inhibits GST P1-1, thereby restoring Jun kinase and MAPK pathway activities and promoting MAPK-mediated cellular proliferation and differentiation pathways. This agent promotes the proliferation and maturation of hematopoietic precursor cells, granulocytes, monocytes, erythrocytes and platelets.
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.