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Dictionary of drugs:E

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Dictionary of pharmaceutical drugs/medications sorted alphabetically

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Dictionary of drugs E

  • E. coli CD-expressing genetically modified neural stem cells Genetically-modified neural stem cells (NSCs) transfected with the Escherichia coli (E. coli) suicidal gene cytosine deaminase (CD), with potential antineoplastic adjuvant activity. Upon intracerebral injection, E. coli CD-expressing genetically modified NSCs express the E. coli cytosine deaminase, an enzyme that catalyzes the intracellular conversion of the nontoxic prodrug 5-fluorocytosine (5-FC) into the cytotoxic 5-fluorouracil (5-FU). Co-administration of this agent with 5-FC and upon local activation of 5-FU in the brain tumor, 5-FU disrupts DNA synthesis in tumor cells thereby impeding cellular proliferation with minimal systemic exposure and toxicity.
  • E-101 solution An oxidant-generating coupled-enzyme system-based, topical solution comprised of two enzymes, Aspergillus niger-derived glucose oxidase (GO) and porcine myeloperoxidase (p-MPO), as well as glucose, sodium chloride and stabilizing amino acids, with potential broad-spectrum microbicidal activity. Following direct administration of E-101 solution into the surgical incisional wound via microspray, the enzyme GO converts oxygen into hydrogen peroxide (H2O2). In turn, p-MPO catalyzes the reaction of H2O2 with hypochlorous acid (HOCl), which is formed through oxidation of the chloride ion, to generate singlet oxygen (O2*). As p-MPO binds to microorganisms, O2* is able to exert direct oxidative damage to microorganisms, resulting in potent antimicrobial activity. E-101 may act as an anti-bactericidal agent against a variety of microorganisms, including multidrug-resistant strains. This may prevent infection at the surgical site.
  • E2F1 pathway activator ARQ 171 A second-generation E2F1 pathway activator with potential antineoplastic activity. ARQ 171 induces the expression of E2F transcription factor 1, thereby activating the E2F1-mediated checkpoint process. As a result, this agent exerts anti-tumor activity through checkpoint activation independent of p53 mediated tumor suppression. E2F1, down-regulated in cancer cells, regulates expression of genes involved in the cell cycle progression from G1 into S phase. The G1/S checkpoint process selectively induces cell cycle arrest in cancer cells with irreparable DNA damages and triggers subsequent apoptosis, while allowing cell division to proceed in cells without or with minor reparable DNA damage.
  • E7820 A small molecule and aromatic sulfonamide derivative with potential antiangiogenic and antitumor activities. E7820 inhibits angiogenesis by suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells. Inhibition of integrin alpha 2 leads to an inhibition of cell-cell interactions, endothelial cell-matrix interactions, vascular endothelial cell proliferation and angiogenesis.
  • East Indian sandalwood oil cream A cream containing an essential oil derived from the East Indian sandalwood tree (Santalum album), containing alpha- and beta-santalols, with potential anti-inflammatory, anti-proliferative, anti-bacterial, anti-viral and immunomodulating activities. Upon topical application of the East Indian sandalwood oil (EISO) cream to an affected area of skin, the active ingredients in the cream may suppress various enzymes, such as cyclooxygenase (COX) and cyclic adenosine monophosphate (cAMP) phosphodiesterases (PDEs), prevent the production of pro-inflammatory cytokines and chemokines and directly cause apoptosis in susceptible cell types, including certain cancer cells and virally-infected cells.
  • East Indian sandalwood oil mouth rinse A mouth rinse containing 0.25% East Indian sandalwood oil, which is derived from the heartwood of Santalum album, a tree native to southern Asia, with potential anti-inflammatory, anti-infective and anti-mucositis activities. East Indian sandalwood oil (EISO) is primarily comprised of the sesquiterpene alcohols alpha- and beta-santalol. Although the exact mechanisms of action through which EISO exerts its effects have yet to be fully elucidated, upon rinsing the oral cavity with the EISO mouth rinse, the active ingredients in the oil may inhibit the production of pro-inflammatory cytokines and chemokines, most likely through the inhibition of the activity of key inflammatory enzymes, including the cyclooxygenases. This prevents inflammation of the mucosal membranes and may prevent or decrease chemotherapy- and/or radiation-induced oral mucositis.
  • EBNA-1 inhibitor VK-2019 An orally available, small molecule inhibitor of Epstein-Barr nuclear antigen 1 (EBNA-1) with potential antineoplastic activity. Upon administration, EBNA-1 inhibitor VK-2019 binds to EBNA-1 and inhibits EBNA-1 DNA binding activity. This disrupts the replication, maintenance and segregation of the Epstein-Barr virus (EBV) genome, which may lead to tumor cell death in EBV-associated malignancies. EBNA1, a sequence-specific DNA binding protein, plays an important role in EBV episomal genome maintenance and gene transactivation.
  • ebselen-containing oral capsule SPI-1005 An oral capsule containing a proprietary formulation of the organoselenium compound ebselen, with potential anti-oxidant, anti-inflammatory and cytoprotective activity. Upon oral administration of SPI-1005, this agent mimics the activity of glutathione peroxidase (GPx) and can utilize glutathione to reduce other unstable molecules, thus preventing the formation of reactive oxygen species (ROS) and reducing oxidative stress on the cell. In the cochlea, this agent may prevent drug-induced injury to the auditory hair cells thereby preventing hearing loss. GPx is the main antioxidant enzyme in the cochlea and protects the inner ear from loud sounds and biochemical damage. In addition, ebselen is able to inhibit the activity of many enzymes involved in inflammation.
  • EBV LMP-2A-specific autologous CD8+ T cells A preparation of autologous cytotoxic T lymphocytes (CTLs) that are specifically reactive to Epstein-Barr virus (EBV) latent membrane protein-2A (LMP-2A) and expressing the co-stimulatory domain 4-1BB (CD137), with potential antineoplastic activity. Upon administration of the EBV/LMP-2A-specific autologous CD8+ T cells to patients with EBV-positive tumors, these cells bind to and cause cell death in EBV-infected cells. This inhibits proliferation of EBV LMP-2A-expressing tumor cells. EBV LMP-2A is expressed in various malignancies and plays a key role in tumor cell proliferation and survival. 4-1BB, an inducible costimulatory member of the tumor-necrosis factor receptor (TNFR) family, is expressed on activated T cells. It activates additional CD8+ T cells, prevents activation-induced cell death of CD8+ T cells, and selectively induces T-helper 1 (Th1)-type cytokines such as interferon (IFN)-gamma and tumor-necrosis factor-alpha (TNF-alpha).
  • echinomycin A polypeptide quinoxaline antineoplastic antibiotic isolated from the bacterium Streptomyces echinatus. Echinomycin intercalates into DNA at two locations simultaneously in a sequence-specific fashion, thereby inhibiting DNA replication and RNA synthesis.
  • Ecotrin Brand name for acetylsalicylic acid
  • ecromeximab A low-fucose, human-mouse chimeric IgG1 monoclonal antibody directed against the ganglioside GD3, a surface antigen expressed on many malignant melanoma cells, with potential antineoplastic activity. Ecromeximab binds to GD3-positive cells, thereby initiating antibody-dependent cytotoxicity against GD3-positive cells. This agent is prepared by fusing murine immunoglobulin (Ig) light and heavy variable regions derived from the murine IgG3 antibody KM-641 to a human constant (Fc) region. The low fucose content of the oligosaccharide side chains of this antibody may enhance binding of the antibody Fc region to lymphocyte Fc receptors.
  • eculizumab A human monoclonal antibody directed against terminal complement protein C5. Eculizumab binds to terminal complement protein C5, thereby blocking C5 cleavage into pro-inflammatory components and blocking the complement-mediated destruction of paroxysmal nocturnal hemoglobinuria (PNH) red blood cells.
  • edatrexate A polyglutamatable folate antagonist analogue of methotrexate with antineoplastic activity. Edatrexate inhibits dihydrofolate reductase, thereby increasing cellular levels of polyglutamates, inhibiting thymidylate synthase and glycinamide ribonucleotide formyl transferase, impairing synthesis of purine nucleotides and amino acids, and resulting in tumor cell death. Edatrexate may overcome tumor resistance to methotrexate, which loses its activity after it is polyglutamated.
  • Edecrin Brand name for ethacrynic acid
  • edotecarin A synthetic indolocarbazole with antineoplastic activity. Edotecarin inhibits the enzyme topoisomerase I through stabilization of the DNA-enzyme complex and enhanced single-strand DNA cleavage, resulting in inhibition of DNA replication and decreased tumor cell proliferation.
  • edoxaban tosylate The tosylate salt form of edoxaban, an orally active inhibitor of coagulation factor Xa (activated factor X) with anticoagulant activity. Edoxaban is administered as edoxaban tosylate. This agent has an elimination half-life of 9-11 hours and undergoes renal excretion.
  • edrecolomab A murine monoclonal IgG2a antibody to tumor-associated epithelial cell adhesion molecule (EpCAM, or 17-1A) antigen. Edrecolomab attaches to EpCAM, a human cell surface glycoprotein that is found on normal epithelial cells and some tumor cells, such as those of colon and breast carcinomas. Upon binding, this agent recruits the body's immune effector cells, which may exhibit antitumor cytotoxicity.
  • EED inhibitor MAK683 An inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. Upon administration, MAK683 selectively binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), which leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2). Disruption of the EED-EZH2 protein-protein interaction (PPI) results in a loss of H3K27me3-stimulated PRC2 activity and prevents H3K27 trimethylation. This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2-mutated and PRC2-dependent cancer cells. PRC2, a histone H3 lysine 27 methyltransferase and multi-protein complex comprised of EZH2, EED and suppressor of zeste 12 (SUZ12), plays a key role in gene regulation, especially during embryonic development. EZH2, the catalytic subunit of PRC2, is overexpressed or mutated in a variety of cancer cells. EED is essential for the histone methyltransferase activity of PRC2 because EED directly binds to H3K27me3.
  • EF5 A fluorinated derivative of the 2-nitroimidazole etanidazole. EF5 is effective in accessing oxygen levels in tumor tissue through its adduct formation to intracellular macromolecules in the absence of oxygen. Reduction of this agent is carried out by a diverse group of enzymes in the cytoplasm, microsomes and mitochondria. Tissue hypoxia detection via EF5 has been reported in several cancers, including squamous cell carcinoma of the cervix and the head and neck, and in sarcoma.
  • efalizumab A humanized IgG1 monoclonal antibody directed against CD11a, the alpha subunit of human leukocyte-function-associated antigen type 1 (LFA-1), with immunosuppressant activity. Efalizumab binds to CD11a, which is expressed on all leukocytes, resulting in a reduction in the cell surface expression of CD11a. In addition, this agent inhibits the binding of LFA-1 to intercellular adhesion molecule-1 (ICAM-1), resulting in the inhibition of leukocyte adherence and the suppression of cell-mediated immunity. LFA-1 binding to ICAM-1 is involved in the activation of T lymphocytes, adhesion of T lymphocytes to endothelial cells, and migration of T lymphocytes to sites of inflammation.
  • efaproxiral A synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity. Increasing tumor oxygenation reduces tumor radioresistance.
  • efatutazone dihydrochloride The dihydrochloride salt of efatutazone, an orally bioavailable agonist of peroxisome proliferator-activated receptor gamma (PPAR-gamma) with potential antineoplastic activity. Efatutazone binds to and activates PPAR-gamma, a nuclear hormone receptor and a ligand-activated transcription factor controling gene expression involved in macromolecule metabolism and cell differentiation, specifically adipocyte differentiation. Mediated through activation of PPAR-gamma, this agent is capable of inducing cell differentiation and apoptosis, thereby leading to a reduction in cellular proliferation.
  • efavirenz A synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity. Efavirenz binds directly to the human immunodeficiency virus type 1 (HIV-1) RT, an RNA-dependent DNA polymerase, blocking its function in viral DNA replication. In combination with other antiretroviral drugs, this agent has been shown to significantly reduce HIV viral load, retarding or preventing damage to the immune system and reducing the risk of developing AIDS. Efavirenz induces activity of the cytochrome P450 system, accelerating its own metabolism.
  • Effexor Brand name for venlafaxine
  • Effexor XR Brand name for venlafaxine hydrochloride extended release
  • eflapegrastim A long-acting, recombinant analog of the endogenous human granulocyte colony-stimulating factor (G-CSF) with hematopoietic activity. Similar to G-CSF, eflapegrastim binds to and activates specific cell surface receptors and stimulates neutrophil progenitor proliferation and differentiation, as well as selected neutrophil functions. Therefore, this agent may decrease the duration and incidence of chemotherapy-induced neutropenia. Eflapegrastim extends the half-life of G-CSF, allowing for administration once every 3 weeks.
  • eflornithine hydrochloride A difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. This agent has been shown to induce apoptosis in leiomyoma cells.
  • eflornithine hydrochloride ointment An ointment formulation of the hydrochloride salt of an ornithine decarboxylase (ODC) inhibitor with hair-growth inhibitory and potential chemopreventive activities. When administered topically, eflornithine irreversibly inhibits skin ODC activity, thereby inhibiting the synthesis of polyamines; inhibition of polyamine synthesis may result in diminished hair growth and epidermal cell turnover.
  • EFS-ADA lentiviral vector-transduced CD34-positive autologous lymphocytes A preparation of autologous, CD34-positive stem/progenitor cells transduced with a lentrivral vector encoding the human adenosine deaminase (ADA) gene under the control of the human elongation factor alpha short promoter (EFS), with potential to restore ADA expression and function. Autologous hematopoietic CD34+ cells are isolated from the patient’s own bone marrow, peripheral blood or cord blood, and transduced with the EFS-ADA lentiviral vector ex vivo. Upon re-infusion of the EFS-ADA vector-transduced lymphocytes back into the patient, these cells may both restore ADA activity and prevent severe combined immunodeficiency (SCID) due to ADA deficiency. ADA, an enzyme that catalyzes the deamination of adenosine to inosine, plays a key role in the development and functioning of the immune system.
  • Efudex Brand name for topical fluorouracil
  • Efudex Brand name for fluorouracil injection
  • Eg5 kinesin-related motor protein inhibitor 4SC-205 A small-molecule inhibitor of the human kinesin-related motor protein Eg5 with potential antineoplastic activity. Eg5 kinesin-related motor protein inhibitor 4SC-205 selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and cell death. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein essential for the regulation of spindle dynamics, including assembly and maintenance, during mitosis.
  • Eg5 kinesin-related motor protein inhibitor ARQ 621 A small-molecule inhibitor of the kinesin-related motor protein Eg5 with potential antineoplastic activity. Eg5 kinesin-related motor protein inhibitor ARQ 621 selectively inhibits the activity of Eg5, which may result in mitotic disruption, apoptosis and cell death. The ATP-dependent Eg5 kinesin-related motor protein (also known as KIF11 or kinesin spindle protein-5) is a plus-end directed kinesin motor protein involved in the regulation of spindle dynamics, including assembly and maintenance, during mitosis.
  • EGb761 A standardized ginkgo biloba extract with antioxidant and neuroprotective activities. EGb761 has been shown to inhibit the proliferation of certain tumor cells in vitro.
  • EGFR antagonist Hemay022 An orally available, irreversible inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, Hemay022 covalently binds to and inhibits the activity of EGFR, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR antisense DNA A synthetic sequence of DNA constructed in the antisense orientation to a sequence of DNA in epidermal growth factor receptor (EGFR), a member of the erbB gene family. EGFR antisense DNA suppresses the expression of EGFR by tumor cells, thereby inhibiting tumor cell proliferation and decreasing tumor growth. This agent also appears to reduce the invasiveness of certain breast cancer cells. Members of the erbB gene family are overexpressed in many cancers and play roles in carcinogenesis and the regulation of cell proliferation.
  • EGFR CAR-CD3zeta-4-1BB-expressing autologous T-lymphocytes Autologous human T-lymphocytes transduced with a retroviral vector encoding an anti-epidermal growth factor receptor (EGFR) chimeric T cell receptor (chimeric antigen receptor or CAR) gene coupled to the signaling domains from both CD3 zeta and CD137 (4-1BB), with potential immunostimulatory and antineoplastic activities. Upon administration, the chimeric EGFR antigen receptor-modified autologous T lymphocytes bind to the EGFR antigen on tumor cell surfaces; subsequently, EGFR-expressing tumor cells may be lysed. Following binding to EGFR, the 4-1BB co-stimulatory molecule signaling domain enhances both activation and signaling. Inclusion of the 4-1BB signaling domain may also increase the antitumor activity when compared to the inclusion of the CD3-zeta chain alone. EGFR, a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, plays key roles in tumor cell proliferation and tumor angiogenesis.
  • EGFR inhibitor ABT-414 An epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon intravenous infusion, ABT-414 inhibits the activity of EGFR, thereby preventing EGFR-mediated signaling. This may inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase overexpressed in certain tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR inhibitor ASP8273 An orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, ASP8273 covalently binds to and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. ASP8273 preferentially inhibits mutated forms of EGFR including T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase inhibitors. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.
  • EGFR inhibitor AZD3759 An orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR inhibitor DBPR112 An orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, DBPR112 binds to and inhibits the activity of EGFR as well certain mutant forms of EGFR, including EGFR L858R and EGFR T790M. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR inhibitor EGF816 An orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGF816 covalently binds to and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. EGF816 preferentially inhibits mutated forms of EGFR including T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase inhibitors. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.
  • EGFR mutant-specific inhibitor BPI-7711 An orally available third-generation and selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations, including the resistance mutations T790M and L858R, as well as exon 19 deletion, with potential antineoplastic activity. Upon administration, the EGFR mutant-specific inhibitor BPI-7711 specifically and covalently binds to and inhibits selective EGFR mutations, with particularly high selectivity against the T790M mutation, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, BPI-7711 may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity against wild-type EGFR (wt EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit wt EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR mutant-specific inhibitor CK-101 An orally available third-generation and selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations, including the resistance mutation T790M, and the L858R and exon 19 deletion (del 19) mutations, with potential antineoplastic activity. Upon administration, the EGFR mutant-specific inhibitor CK-101 specifically and covalently binds to and inhibits specific EGFR mutations, with particularly high selectivity against the T790M mutation; this prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, CK-101 may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity against wild-type EGFR (WT EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit WT EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR mutant-specific inhibitor D-0316 An orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, the EGFR mutant-specific inhibitor D-0316 specifically binds to and inhibits EGFR T790M, a secondarily acquired resistance mutation, which prevents EGFR-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. Compared to some other EGFR inhibitors, D-0316 may have therapeutic benefits in tumors with T790M-mediated drug resistance. EGFR, a receptor tyrosine kinase that is mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR mutant-specific inhibitor ZN-e4 An orally available selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations, including the resistance mutation T790M, with potential antineoplastic activity. Upon administration, the EGFR mutant-specific inhibitor ZN-e4 specifically binds to and inhibits selective EGFR mutations, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to other EGFR inhibitors, ZN-e4 may offer therapeutic benefits in tumors with T790M-mediated drug resistance and may limit toxicities associated with non-selective EGFR inhibitors. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR T790M antagonist BPI-15086 An orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. EGFR T790M antagonist BPI-15086 specifically binds to and inhibits EGFR T790M, a secondarily acquired resistance mutation, which prevents EGFR-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.
  • EGFR T790M inhibitor PF-06747775 An orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. EGFR T790M inhibitor PF-06747775 specifically binds to and inhibits EGFR T790M, a secondarily acquired resistance mutation, which prevents EGFR-mediated signaling and leads to cell death in EGFR T790M-expressing tumor cells. Compared to some other EGFR inhibitors, PF-06747775 may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity against wild-type EGFR (WT EGFR), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which can inhibit WT EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
  • EGFR tyrosine kinase inhibitor HS-10296 An orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity. Upon administration, HS-10296 binds to and inhibits EGFR T790M, a secondarily acquired resistance mutation, inhibits the tyrosine kinase activity of EGFR T790M, 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.
  • EGFR/FLT3/Abl inhibitor SKLB1028 An orally available inhibitor of epidermal growth factor receptor (EGFR), FMS-related tyrosine kinase 3 (FLT3, STK1, CD135 or FLK2), and the non-receptor tyrosine kinase ABL (Abl), with potential antineoplastic activity. Upon administration, the EGFR/FLT3/Abl inhibitor SKLB1028 specifically binds to and inhibits EGFR, FLT3 and Abl, which interferes with the activation of EGFR-, FLT3- and Abl-mediated signal transduction pathways and reduces cell proliferation in cancer cells that overexpress EGFR, FLT3 and/or Abl. EGFR, EGFR and Abl are all overexpressed in a variety of cancers and play key roles in tumor cell proliferation.
  • EGFR/HER2 inhibitor AP32788 An orally available inhibitor of specific mutant forms of both human epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2; ERBB2), with potential antineoplastic activity. Upon oral administration, EGFR/HER2 inhibitor AP32788 specifically and irreversibly binds to and inhibits certain mutant forms of EGFR and HER2. This prevents EGFR- and HER2-mediated signaling and leads to cell death in EGFR mutant- and HER2 mutant-expressing tumor cells. EGFR and HER2, receptor tyrosine kinases mutated in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization.
  • EGFR/HER2 inhibitor AV-412 A second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. This agent may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization.
  • EGFRBi-armed autologous activated T cells Autologous activated T cells, loaded with a bispecific antibody produced by heteroconjugation of anti-CD3 and anti-epidermal growth factor receptor (EGFR) monoclonal antibodies, with potential antineoplastic activity. Binding of EGFRBi-armed autologous activated T cells to EGFR-positive tumor cells may result in increased T cell-mediated cytotoxicity towards tumor cells expressing EGFR. Arming activated T cells with this bispecific antibody may significantly increase T cell secretion of anti-tumor associated cytokines such as IL2, RANTES, IFN-gamma, and TNF-alpha.
  • eicosapentaenoic acid An essential, polyunsaturated, 20-carbon omega-3 fatty acid with anti-inflammatory and potential antineoplastic and chemopreventive activities. Eicosapentaenoic acid (EPA) may activate caspase 3, resulting in apoptosis in susceptible tumor cell populations. In addition, this agent may inhibit cyclooxygenase-2 (COX-2), resulting in inhibition of prostaglandin synthesis and prostaglandin-mediated inflammatory processes.
  • eicosapentaenoic acid monoacylglyceride An eicosapentaenoic acid derivative with potential antineoplastic activities. Upon oral administration, eicosapentaenoic acid monoacylglyceride (MAG-EPA) may inhibit epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR) and serine/threonine protein kinase AKT (protein kinase B)-mediated signaling pathways and reduce vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1-alpha (HIF1-alpha) expression levels in tumor cells. This may promote apoptosis and inhibit tumor cell growth in cells expressing EGFR, AKT, and VEGFR. MAG-EPA may also inhibit androgen-stimulated tumor cell growth and repress androgenic induction of prostate-specific antigen (PSA) expression. PSA, a tumor associated antigen (TAA), is expressed by prostate epithelial cells and is overexpressed in prostate cancer. The AKT signaling pathway is often dysregulated in cancer and is associated with tumor cell proliferation, survival and migration. EGFR and VGFR are receptor tyrosine kinases that are mutated or upregulated in many tumor cell types and play a key role in tumor cell proliferation and tumor vascularization.
  • eicosapentaenoic acid-enriched nutritional supplement A nutritional supplement enriched with eicosapentaenoic acid (EPA), which is an essential, polyunsaturated, 20-carbon omega-3 fatty acid found in fish oil, with potential anti-inflammatory and anti-cachectic activities. Upon oral intake of the EPA-enriched nutritional supplement, EPA is incorporated in cell membrane phospholipids and replaces arachidonic acid. This affects the production of pro-inflammatory mediators, such as tumor necrosis factor-alpha (TNF-a), interleukin-1 (IL-1) and IL-6, through the inhibition of nuclear factor kappa B (NF-kB) activity. This inhibits inflammation and may abrogate the cachexia-mediated decrease of lean body mass (LBM), which may lead to increased body weight. Pro-inflammatory mediators, such as TNF-a, interferon-gamma, and certain interleukins, such as IL-6 and IL-1b, play a key role in cachexia.
  • eIF4E antisense oligonucleotide ISIS 183750 A second-generation antisense oligonucleotide targeting the eukaryotic translation initiation factor 4E (eIF4E) with potential antitumor activity. Antisense oligonucleotide ISIS EIF4ERx suppresses the expression of eIF4E in fast dividing tumor cells. Blocking the expression of eIF4E results in inhibition of the synthesis of tumor angiogenic factors, thereby leading to the inhibition of cellular proliferation and apoptosis in tumor cells. eIF4E is overexpressed in a variety of cancers, is involved in the mRNA-ribosome binding step of eukaryotic protein synthesis and is the rate-limiting component of the eukaryotic translation apparatus.
  • elacestrant An orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration of higher doses of elacestrant, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, elacestrant is able to cross the blood-brain barrier (BBB).
  • elacytarabine The lipophilic 5'-elaidic acid ester of the deoxycytidine analog cytosine arabinoside (cytarabine; Ara-C) with potential antineoplastic activity. As a prodrug, CP-4055 is converted intracellularly into cytarabine triphosphate by deoxycytidine kinase and subsequently competes with cytidine for incorporation into DNA, thereby inhibiting DNA synthesis. Compared to cytarabine, CP-4055 shows increased cellular uptake and retention, resulting in increased activation by deoxycytidine kinase to cytarabine triphosphate, decreased deamination and deactivation by deoxycytidine deaminase, and increased inhibition of DNA synthesis. This agent also inhibits RNA synthesis, an effect not seen with cytarabine.
  • elagolix An orally bioavailable, second-generation, non-peptide based, small molecule compound and selective gonadotropin-releasing hormone (GnRH; LHRH) receptor antagonist, with potential hormone production inhibitory activity. Upon oral administration, elagolix competes with GnRH for receptor binding and inhibits GnRH receptor signaling in the anterior pituitary gland. This inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. In women, inhibition of FSH and LH prevents the production of estrogen by the ovaries. Inhibition of GnRH signaling may treat or prevent symptoms of sex hormone-dependent disease states.
  • elbasvir/grazoprevir A fixed dose combination of elbasvir, an inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A), and grazoprevir, a second-generation inhibitor of the HCV NS3/4A serine protease, with activity against certain HCV genotypes. Upon oral administration of elbasvir/grazoprevir, elbasvir inhibits the activity of the NS5A protein, leading to disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. Grazoprevir inhibits the NS3/4A serine protease enzyme, thereby disrupting the cleavage of the virally encoded polyprotein into mature proteins and preventing the formation of the viral replication complex. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of certain cancers.
  • Eldecort Brand name for therapeutic hydrocortisone
  • Eldisine Brand name for vindesine sulfate
  • Eldopar Brand name for levodopa
  • electrokinetically modified water Orally available, nanobubble-based, electrokinetically modified water (EMW) composed of reverse osmosis water where the minerals calcium chloride, magnesium chloride, and potassium bicarbonate have been added and with an increased oxygen concentration compared to normal water. Upon consumption, the EMW may have a beneficial effect on fatigue. This water may protect muscle cells against damage and may improve skeletal muscle function. The water is pretreated with strong, controlled turbulence to create charge-stabilized nanostructures.
  • electrolyte-free parenteral nutrition emulsion An electrolyte-free emulsion for infusion consisting of a three chamber bag system containing glucose, amino acids and lipids that can be used to provide parenteral nutritional supplementation. The lipid emulsion portion contains soybean oil, medium-chain triglycerides, olive oil and fish oil; the amino acid solution contains alanine, arginine, glycine, histidine, leucine, isoleucine, lysine, methionine, phenylalanine, proline, serine, taurine, threonine, tryptophan, tyrosine, and valine. The electrolyte-free parenteral nutrition emulsion contains no electrolytes, trace elements and vitamins. The three separate bags containing glucose, amino acids and lipids are mixed together before infusion.
  • elesclomol A small-molecule bis(thio-hydrazide amide) with oxidative stress induction, pro-apoptotic, and potential antineoplastic activities. Elesclomol induces oxidative stress, creating high levels of reactive oxygen species (ROS), such as hydrogen peroxide, in both cancer cells and normal cells. Because tumor cells have elevated levels of ROS compared to normal cells, the increase in oxidative stress beyond baseline levels elevates ROS beyond sustainable levels, exhausting tumor cell antioxidant capacity, which may result in the induction of the mitochondrial apoptosis pathway. Normal cells are spared because the increase in the level of oxidative stress induced by this agent is below the threshold at which apoptosis is induced.
  • elesclomol sodium The water soluble sodium salt of a small-molecule bis(thio-hydrazide amide) with oxidative stress induction, pro-apoptotic, and potential antineoplastic activities. Elesclomol induces oxidative stress, creating high levels of reactive oxygen species (ROS), such as hydrogen peroxide, in both cancer cells and normal cells. Because tumor cells have elevated levels of ROS compared to normal cells, the increase in oxidative stress beyond baseline levels elevates ROS beyond sustainable levels, exhausting tumor cell antioxidant capacity, which may result in the induction of the mitochondrial apoptosis pathway. Normal cells are spared because the increase in the level of oxidative stress induced by this agent is below the threshold at which apoptosis is induced.
  • Elidel Brand name for pimecrolimus cream
  • Eligard Brand name for leuprolide acetate
  • Eliquis Brand name for apixaban
  • elisidepsin A marine-derived, synthetic cyclic depsipeptide with potential antineoplastic activity. Elisidepsin is a derivative of a natural marine compound that belongs to a family of dehydro aminobutyric acid-containing peptides (kahalalides) isolated from the herbivorous marine mollusk Elysia rufescens. Although the primary mechanism of action has yet to be elucidated, this agent exhibits anti-proliferative activity in a wide variety of cancer cell types, including breast, colon, pancreas, lung, and prostate; it appears to induce oncolytic rather than apoptotic cell death.
  • Elitek Brand name for rasburicase
  • Elixophyllin Brand name for theophylline
  • ellagic acid/Annona muricata supplement A nutritional supplement containing the phytochemical polyphenol, ellagic acid, and an extract of Annona muricata, with potential chemopreventive activity. Although the exact mechanism of action for ellagic acid has yet to be fully elucidated, this agent acts as an anti-oxidant and reduces oxidative stress. This agent also appears to protect the body against certain carcinogens, either through preventing DNA binding or by increasing the rate of their metabolism and deactivation. Certain extracts of Annona muricata, a member of the custard apple plants and belonging to the Annonaceae family, may have antiviral activity, potential targets include human papilloma virus (HPV), and may be cytotoxic against various types of cancer cells.
  • Ellence Brand name for epirubicin hydrochloride
  • elliptinium acetate Acetate salt of elliptinium, a derivative of the alkaloid ellipticine isolated from species of the plant family Apocynaceae, including Bleekeria vitensis, a plant with anti-cancer properties. As a topoisomerase II inhibitor and intercalating agent, elliptinium stabilizes the cleavable complex of topoisomerase II and induces DNA breakages, thereby inhibiting DNA replication and RNA and protein synthesis.
  • Elmiron Brand name for pentosan polysulfate sodium
  • Elocon Brand name for mometasone furoate
  • elotuzumab A humanized monoclonal antibody directed against the human CS1 (CD2 subset 1, CRACC, SLAMF7) antigen with potential antineoplastic activity. Elotuzumab binds to the CS1 antigen, which may trigger antibody-dependent cellular cytotoxicity (ADCC) in cells expressing CS1. CS1 is a cell surface glycoprotein belonging to the CD2 subset of the immunoglobulin superfamily (IgSF) and is highly expressed by multiple myeloma cells, but minimally expressed by normal cells.
  • Eloxatin Brand name for oxaliplatin
  • elsamitrucin A heterocyclic antineoplastic antibiotic isolated from the bacterium Actinomycete strain J907-21. Elsamitrucin intercalates into DNA at guanine-cytosine (G-C)-rich sequences and inhibits topoisomerase I and II, resulting in single-strand breaks and inhibition of DNA replication.
  • elsiglutide A synthetic glucagon-like peptide-2 (GLP-2) analogue with potential antidiarrheal and intestinotrophic activities. Upon subcutaneous administration, elsiglutide, a 39 amino acid polypeptide, binds to GLP-2 receptors and thereby promotes proliferation of epithelial cells. Regeneration of endothelial cells damaged during chemotherapy may prevent or decrease chemotherapy-induced diarrhea. In addition, elsiglutide may prevent chemotherapy-induced intestinal injury. GLP-2, a peptide hormone primarily produced in the small intestines in response to food, plays a key role in intestinal epithelial growth, metabolism and regeneration of epithelial cells.
  • Elspar Brand name for asparaginase
  • eltrombopag olamine The orally active ethanolamine salt of eltrombopag, a small-molecule, nonpeptide thrombopoietin receptor agonist with megakaryopoiesis-stimulating activity. Eltrombopag binds to and stimulates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), a member of the hematopoietin receptor superfamily. Activation of TPO-R leads to the proliferation and differentiation of cells in the megakaryocytic lineage and an increase in platelet production.
  • Elzonris Brand name for tagraxofusp-erzs
  • emactuzumab A humanized monoclonal antibody directed against the tyrosine kinase receptor colony stimulating factor 1 receptor (CSF1R; CSF-1R; CD115), also known as macrophage colony-stimulating factor receptor (M-CSFR), with potential antineoplastic and immunomodulating activities. Upon administration, emactuzumab binds to CSF1R expressed on macrophages and inhibits the binding of colony-stimulating factor-1 (CSF-1) to CSF1R. This prevents CSF1R activation and CSF1R-mediated signaling in these cells, which blocks the production of inflammatory mediators by macrophages and reduces inflammation. By blocking both the activity of CSF1R-dependent tumor-associated macrophages (TAMs) and the recruitment of TAMs to the tumor microenvironment, emactuzumab enhances T-cell infiltration and antitumor T-cell immune responses, which inhibits the proliferation of tumor cells. TAMs play key roles in immune suppression and promoting inflammation, tumor cell proliferation and survival.
  • emapalumab-lzsg A human monoclonal antibody against the cytokine interferon-gamma (IFN-gamma; IFNg), with potential immunomodulating activity. Upon administration, emapalumab binds to and neutralizes IFNg. This inhibits IFNg-mediated signaling pathways and suppresses the activation of the immune system. IFNg, a cell-signaling protein, plays a key role in the regulation and activation of the immune system; its upregulation is associated with certain auto-immune and auto-inflammatory diseases in which the immune system is abnormally activated.
  • Emcyt Brand name for estramustine phosphate sodium
  • Emend Brand name for aprepitant
  • emepepimut-S 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.
  • Emergent-EZ Brand name for hydrocortisone sodium succinate
  • Empirin Brand name for acetylsalicylic acid
  • Empliciti Brand name for elotuzumab
  • emtricitabine 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).
  • Emtriva Brand name for emtricitabine
  • E-Mycin Brand name for erythromycin
  • Enacard Brand name for enalapril maleate
  • enadenotucirev A complex, replication-selective, E1B and partial E3 gene deleted, adenovirus type 11p (Ad11p)/Ad3 chimeric oncolytic virus with potential antineoplastic activity. Upon intralesional injection of enadenotucirev, the adenovirus selectively and rapidly replicates in cancer cells; however, it is unable to replicate in normal, healthy cells. This induces a selective adenovirus-mediated cytotoxicity in cancer cells, which leads to cancer cell lysis. Following the lysis of infected cells, the replicated virus is released and can infect adjacent cells, which both induces further tumor cell oncolysis and may activate the immune system to kill the infected tumor cells. The E1B protein causes p53 inactivation in host cells, which promotes viral replication. Deletion of E1B prevents replication in normal, healthy cells that express wild-type p53. The mutation and subsequent inactivation of p53 in cancer cells enables the E1B-deleted adenovirus to selectively replicate in cancer cells. Partial deletion of the E3 gene, which encodes the adenovirus death protein, enhances the safety profile of the administered adenovirus.
  • enadenotucirev-expressing anti-CD40 agonistic monoclonal antibody NG-350 An oncolytic adenoviral vector, enadenotucirev (EnAd), that expresses a full-length agonistic anti-CD40 monoclonal antibody, with potential immunomodulating and antineoplastic activities. Upon intratumoral administration of NG-350A, enadenotucirev specifically infects and replicates in tumor cells and not in normal, noncancerous tissue, and selectively expresses the agonistic anti-CD40 antibody. The locally expressed anti-CD40 antibody targets and binds to CD40 on a variety of immune cells, including B cells, T cells and dendritic cells (DCs) in the tumor microenvironment (TME). This induces CD40-dependent signaling pathways, which activates these immune cells and induces a cytotoxic T-lymphocyte (CTL)-mediated antitumor immune response and leads to tumor cell death. CD40, a cell surface receptor and member of the tumor necrosis factor receptor superfamily (TNFRSF), is expressed on various immune cells and plays a key role in the activation of the immune system.
  • 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.
  • enasidenib mesylate The mesylate salt form of enasidenib, an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, enasidenib specifically inhibits various mutant forms of IDH2, including the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by blocking differentiation and the production of the oncometabolite 2HG.
  • enavatuzumab 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.
  • Enbrel Brand name for etanercept
  • enclomiphene citrate 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.
  • encochleated amphotericin B A proprietary, orally bioavailable, nanoparticle-based encochleated formulation composed of amphotericin B, a polyene antifungal antibiotic produced by Streptomyces nodosus, encochleated within lipid-based crystals, which are composed of multi-layered, rolled-up sheets of soy-derived phosphatidylserine (PS) bilayers and calcium, with broad-spectrum antifungal activity. Upon oral administration, the cochleate crystal structure protects amphotericin B from degradation within the gastrointestinal (GI) tract. The lipid structure facilitates uptake into the bloodstream where the nanoparticles are taken up by macrophages and fungal cells though phagocytosis. Amphotericin B is released from the cochleate due to the calcium differential between the inside of the cell, which has low calcium levels, and the outside of the cell, which has high calcium levels. This delivers amphotericin B directly to the fungal-infected site and to its target cells. In turn, amphotericin B binds to ergosterol, an essential component of the fungal cell membrane. This results in depolarization of the cell membrane, alterations in cell membrane permeability, leakage of important intracellular components, and cell rupture. This causes fungal cell death and prevents fungal infections. Compared to amphotericin B alone, which can only be administered intravenously (IV), this formulation permits oral administration and reduces treatment-limiting side effects that are seen with IV amphotericin B, particularly nephro- and hepato-toxicity.
  • encorafenib An orally available Raf kinase inhibitor with potential antineoplastic activity. Encorafenib specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of encorafenib may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival.
  • EndoClot Brand name for absorbable modified polymer hemostatic powder
  • Endometrin Brand 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.
  • enfortumab vedotin An antibody drug conjugate (ADC) containing a human monoclonal antibody AGS-22 targeting the cell adhesion molecule nectin-4 and conjugated to the cytotoxic agent monomethyl auristatin E (MMAE), via a proprietary enzyme-cleavable linker (AGS-22CE), with potential antineoplastic activity. The monoclonal antibody moiety of AGS-22CE selectively binds to nectin-4. After internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in nectin-4 overexpressing tumor cells. Nectin-4, a tumor associated antigen belonging to the nectin family, is overexpressed in a variety of cancers, including breast, bladder, lung and pancreatic cancer.
  • Engerix-B Brand name for hepatitis B vaccine (recombinant)
  • Enhanzyn Brand name for Detox-B adjuvant
  • eniluracil An orally-active fluoropyrimidine analogue. Eniluracil inhibits dihydropyrimidine dehydrogenase, the rate-limiting enzyme that catabolizes and inactivates 5-fluorouracil (5-FU) in the liver. Co-administration of ethynyluracil permits the oral administration of 5-FU.
  • enoblituzumab An Fc-domain optimized, humanized monoclonal antibody directed against cancer stem cells (CSCs), with potential immunomodulating and antineoplastic activities. After binding of enoblituzumab to an as of yet not elucidated target expressed on CSCs and differentiated tumor cells, this agent may induce an antibody-dependent cell-mediated cytotoxicity (ADCC) against CSCs. CSCs are tumor initiating cells that are able to self-renew and are responsible for tumor cell growth and resistance.
  • enobosarm A non-steroidal agent with anabolic activity. Enobosarm is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.
  • enoxaparin sodium The sodium salt of a low molecular weight, synthetic heparin. As an anticoagulant/antithrombotic agent, enoxaprin's mechanism of action is similar to that of heparin, although it exhibits a higher ratio of anti-Factor Xa to anti-Factor IIa activity. This agent also has anti-inflammatory properties, inhibiting monocyte adhesion to tumor necrosis factor alpha- or lipopolysaccharide-activated endothelial cells. Compared to unfractionated heparins, the use of enoxaparin is associated with lower incidences of osteoporosis and heparin-induced thrombocytopenia.
  • Enpresse Brand name for ethinyl estradiol/levonorgestrel
  • ensartinib An orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, ensartinib binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK is not expressed in healthy adult human tissue but ALK dysregulation and gene rearrangements are associated with a series of tumors; ALK mutations are associated with acquired resistance to small molecule tyrosine kinase inhibitors.
  • ensituximab 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.
  • Ensure Brand name for nutritional supplement drink
  • entecavir 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.
  • Enterade Brand name for amino acid/electrolyte mixture-based dietary supplement
  • EnteraGam Brand name for serum-derived bovine immunoglobulin protein isolate
  • Entereg Brand name for alvimopan
  • Enterex Glutapak-10 Brand name for glutamine
  • 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.
  • Entericin Brand name for acetylsalicylic acid
  • Enterococcus gallinarum strain MRx0518 A live strain of the flagellin-producing Gram-positive bacterium Enterococcus (E.) gallinarum that is isolated from a healthy human gut , with potential immunomodulating and antineoplastic activities. Upon oral administration, MRx0518 modulates the intestinal microbiota and targets both intestinal epithelial cells (IECs), and various immune cells, such as macrophages and dendritic cells (DCs) and is able to induce the production of both pro- and anti-inflammatory mediators, such as interleukin-8 (IL-8), tumor necrosis factor-alpha (TNF-a), IL-1beta, IL-6, IL-23, in these cells and activates the innate immune system. The flagellin produced by MRx0518 interacts with and activates toll-like receptor 5 (TLR5), thereby activating the adaptive immune system and modulating the tumor microenvironment (TME). This activates the immune system to mount a cytotoxic T-lymphocyte (CTL) immune response against tumor cells.
  • entinostat A synthetic benzamide derivative with potential antineoplastic activity. Entinostat binds to and inhibits histone deacetylase, an enzyme that regulates chromatin structure and gene transcription. This agent appears to exert dose-dependent effects in human leukemia cells including cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1)-dependent growth arrest and differentiation at low drug concentrations; a marked induction of reactive oxygen species (ROS); mitochondrial damage; caspase activation; and, at higher concentrations, apoptosis. In normal cells, cyclin-dependent kinase inhibitor 1A expression has been associated with cell-cycle exit and differentiation.
  • entolimod A polypeptide derived from the Salmonella filament protein flagellin with potential radioprotective and anticancer activities. As a toll-like receptor 5 (TLR5) agonist, entolimod binds to and activates TLR5 thereby stimulating tumor necrosis factor production and activating nuclear factor kappa B (NF-kB). This induces NF-kB-mediated signaling pathways and inhibits the induction of apoptosis. This may prevent apoptosis in normal, healthy cells during radiotherapy of cancerous cells and may allow for increased doses of ionizing radiation. In addition, entolimod may inhibit radiation-independent proliferation in TLR5-expressing tumor cells.
  • entospletinib An orally available inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. Upon oral administration of entospletinib, this agent may inhibit the activity of Syk, which inhibits B-cell receptor (BCR) signaling and leads to an inhibition of tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoeitic malignancies.
  • entrectinib An orally bioavailable inhibitor of the tyrosine kinases tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon administration, entrectinib binds to and inhibits TrkA, TrkB, TrkC, ROS1 and ALK. Inhibition of these kinases may result in a disruption of TrkA-, TrkB-, TrkC-, ROS1-, and ALK-mediated signaling. This leads to an induction of apoptosis and an inhibition of tumor cell proliferation in tumor cells that express these kinases. TrkA, TrkB, TrkC, ROS1 and ALK are overexpressed in a variety of cancer cell types.
  • Entyvio Brand name for vedolizumab
  • enzalutamide An orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Through a mechanism that is reported to be different from other approved AR antagonists, enzalutamide inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. AR over-expression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance.
  • enzastaurin hydrochloride The hydrochloride salt of enzastaurin, a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
  • enzymatically hydrolyzed whey protein-based nutritional supplement An orally available, gluten-free, enzymatically hydrolyzed cysteine-rich whey-protein based nutritional supplement containing essential vitamins, minerals, and trace elements, as well as fat and carbohydrates. Upon oral intake of the nutritional supplement, the whey protein may improve gastric functioning and gastrointestinal health, thereby reducing vomiting and diarrhea. The whey-based hydrolyzed protein helps to alleviate the digestive burden for the pancreas and may be beneficial for patients with a pancreas-associated disease, such as pancreatitis or pancreatic cancer. Due to the high levels of cysteine in the whey protein, this supplement increases levels of the antioxidant glutathione (GSH). The polyunsaturated fatty acids in this supplement are incorporated in cell membranes and affect the production of pro-inflammatory mediators, eliciting an anti-inflammatory effect. Medium chain triglycerides (MCT) in this supplement enhance fat absorption and may aid in the prevention of fat malabsorption. Altogether, this supplement may prevent both malnutrition and weight loss.
  • Eoquin Brand name for apaziquone
  • Eovist Brand name for gadoxetate disodium
  • EP4 antagonist ONO-4578 An orally bioavailable antagonist of the prostaglandin E2 receptor subtype 4 (PTGER4; EP4), with potential analgesic, immunomodulating and antineoplastic activities. Upon administration, the EP4 antagonist ONO-4578 selectively targets and binds to EP4, inhibiting the binding of the immunosuppressive prostaglandin E2 (PGE2) to EP4. This prevents the activation of EP4 and inhibits PGE2-EP4-mediated signaling, thereby inhibiting proliferation of tumor cells in which the PGE2-EP4 signaling pathway is over-activated. In addition, EP4 inhibition prevents the activity of tumor-associated myeloid cells (TAMCs) in the tumor microenvironment (TME) by inhibiting interleukin-23 (IL-23) production and the IL-23-mediated expansion of Th17 cells. EP4, a prostanoid receptor, is a G protein-coupled receptor that is expressed in certain types of cancers; it promotes tumor cell proliferation and invasion.
  • epacadostat An orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. epacadostat targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, epacadostat increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs.
  • EpCAM-specific CAR-expressing autologous T lymphocytes A preparation of autologous T lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) specific for the antigen epithelial cell adhesion molecule (EpCAM), with potential immunostimulating and antineoplastic activities. Upon administration, the EpCAM-specific CAR-expressing autologous T lymphocytes specifically recognize and bind to EpCAM-expressing tumor cells, resulting in tumor cell lysis. EpCAM, a cell surface protein, is expressed by a variety of tumor cells.
  • EphA2-targeting DOPC-encapsulated siRNA A liposomal formulation consisting of short-interfering RNAs (siRNAs) directed against ephrin type-A receptor 2 (EphA2) and encapsulated into 1,2-dioleoyl-sn-glycero-3-phosphatidylcholine (DOPC) neutral liposomes, with potential antineoplastic activity. Upon internalization, EphA2-targeting DOPC-encapsulated siRNA can hybridize to EphA2 DNA and mRNA, thereby interfering with both the transcription and translation of EphA2, and thus inhibiting tumor cell growth. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types and plays an important role in tumor growth.
  • EpiCept NP-1 Brand name for ketamine/amitriptyline NP-H cream
  • epidermal growth factor ointment A topical ointment containing a recombinant form of human epidermal growth factor (EGF) with potential protective activity against EGF receptor (EGFR/HER1) inhibitor-induced cutaneous toxicities. Upon topical application of the EGF ointment, EGF locally activates EGFR, thereby abrogating EGFR inhibition in the skin caused by systemic EGFR inhibiting agents. This may help inhibit the skin rash induced by EGFR antagonists. EGFR, a tyrosine kinase, plays a key role in maintaining epidermal integrity.
  • epigallocatechin gallate A phenolic antioxidant found in a number of plants such as green and black tea. It inhibits cellular oxidation and prevents free radical damage to cells. It is under study as a potential cancer chemopreventive agent.
  • Epilex Brand name for divalproex sodium
  • epirubicin hydrochloride The hydrochloride salt of the 4'-epi-isomer of the anthracycline antineoplastic antibiotic doxorubicin. Epirubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also produces toxic free-radical intermediates and interacts with cell membrane lipids causing lipid peroxidation.
  • epitinib succinate The succinate salt form of epitinib, an orally available epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon administration, epitinib inhibits the activity of EGFR, thereby preventing EGFR-mediated signaling. This may lead to induction of cell death and inhibition of tumor growth in EGFR-overexpressing tumor cells. EGFR is a receptor tyrosine kinase (RTK) that is overexpressed in certain tumor types and plays a key role in tumor cell proliferation and vascularization.
  • Epitol Brand name for carbamazepine
  • Epival Brand name for divalproex sodium
  • Epivir Brand name for lamivudine
  • eplerenone A selective aldosterone receptor antagonist. Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreasing sodium resorption and subsequently increasing water outflow. This leads to a decrease in blood pressure. Eplerenone is used in the treatment of hypertension and congestive heart failure.
  • EPOCH regimen A chemotherapy regimen consisting of etoposide, prednisone, vincristine (Oncovin), cyclophosphamide and doxorubicin hydrochloride (hydroxydaunorubicin hydrochloride), which may be used in combination with rituximab (R-EPOCH) for the treatment of various aggressive B-cell and T-cell non-Hodgkin lymphomas.
  • EPOCH-O regimen An immune-chemotherapy regimen consisting of etoposide, prednisone, vincristine (Oncovin), cyclophosphamide, doxorubicin (hydroxydaunorubicin) and ofatumumab, which may be used for the treatment of various aggressive non-Hodgkin lymphomas.
  • epoetin alfa A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine human erythropoietin (EPO). Produced primarily by cells of the peritubular capillary endothelium of the kidney in response to hypoxia, circulating EPO binds to EPO receptors on the surface of committed erythroid progenitors in the bone marrow resulting in their replication and maturation into functional erythrocytes.
  • epoetin beta A recombinant therapeutic agent that is chemically identical to or similar to the endogenous cytokine human erythropoietin (EPO). Produced primarily by cells of the peritubular capillary endothelium of the kidney in response to hypoxia, circulating EPO binds to EPO receptors on the surface of committed erythroid progenitors in the bone marrow resulting in their replication and maturation into functional erythrocytes.
  • epoetin zeta A recombinant form of the endogenous human cytokine erythropoietin (EPO) with erythropoiesis-stimulating activity. Similar to EPO, epoetin zeta binds to and activates erythropoietin receptors on the surface of committed erythroid progenitors in the bone marrow resulting in their proliferation and differentiation into functional erythrocytes. This may enhance red blood cell counts and hemoglobin levels. Epoetin zeta differs from other epoetins in its glycosylation profile. EPO is a glycosylated polypeptide primarily produced by renal peritubular cells and its synthesis is regulated by a serum oxygenation feedback mechanism.
  • Epogen Brand name for epoetin alfa
  • epothilone analog UTD1 A genetically engineered epothilone analog with potential antineoplastic activity. Upon administration, epothilone analog UTD1 binds to tubulin, 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 enhanced activity against certain multidrug-resistant (MDR) tumors.
  • epothilone D A natural polyketide compound isolated from the myxobacterium Sorangium cellulosum. Also known as desoxyepothilone B, epothilone D binds to tubulin and inhibits the disassembly of microtubules, resulting in the inhibition of mitosis, cellular proliferation, and cell motility.
  • epothilone KOS-1584 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.
  • epratuzumab A recombinant, humanized monoclonal antibody directed against CD22, a cell surface glycoprotein present on mature B-cells and on many types of malignant B-cells. After binding to CD22, epratuzumab's predominant antitumor activity appears to be mediated through antibody-dependent cellular cytotoxicity (ADCC).
  • epratuzumab-cys-tesirine An antibody-drug conjugate (ADC) composed of a cysteine-engineered version of epratuzumab (hLL2), a humanized anti-CD22 monoclonal antibody derived from the murine immunoglobulin (Ig) G2a monoclonal antibody LL2 (EPB-2), site-specifically conjugated to the cross-linking cytotoxic agent tesirine (SG3249), a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine dimer (PBD), with potential antineoplastic activity. Upon administration of epratuzumab-cys-tesirine, the epratuzumab moiety targets and binds to the B-cell-specific CD22 receptor and is rapidly internalized. Upon cleavage, the imine groups of tesirine target and bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA and inhibits DNA replication, which inhibits the proliferation of CD22-overexpressing tumor cells. CD22, a cell surface glycoprotein, is expressed on mature B-cells and on most malignant B cells.
  • eprodisate disodium The orally available disodium salt form of eprodisate, a negatively charged sulfonated inhibitor of fibrillogenesis, that can be used in the treatment of amyloid A (AA) amyloidosis. Upon administration, eprodisate competitively binds to the glycosaminoglycan binding sites on serum amyloid A (SAA), which inhibits the formation of the glycosaminoglycan-amyloid fibril aggregate. This prevents the formation of amyloid deposits in certain organs, especially the kidneys, in AA amyloidosis.
  • EPS8 peptide-specific dendritic cells A preparation of dendritic cells (DCs) pulsed with peptides derived from epidermal growth factor receptor (EGFR) pathway substrate 8 (EPS8), with potential immunostimulating and antineoplastic activities. Upon administration of the EPS8 peptide-specific DCs, the immune system is exposed to the EPS8 antigens. This results in the induction of a specific cytotoxic T-lymphocyte (CTL) response against EPS8-expressing tumor cells and tumor cell lysis. EPS8, a tumor-associated antigen (TAA), is overexpressed in a variety of tumor cell types but rarely in normal tissues. As a substrate for the EGFR kinase, it plays a key role in tumor progression through the EGFR-dependent pathway. Its expression is correlated with a poor prognosis.
  • 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.
  • Eraxis Brand name for anidulafungin
  • erb-38 immunotoxin A bivalent fusion protein consisting of disulfide-stabilized Fv fragments of an anti-HER2 (erbB2) monoclonal antibody (e23) and a truncated version of the M(r) 38 fragment of Pseudomonas exotoxin that lacks the toxin's cell binding domain. ERB-38 immunotoxin binds specifically to cells that overexpress HER2, the antigenic target of the monoclonal antibody; the exotoxin portion of the immunotoxin then lyses the cells bound by the antibody portion.
  • Erbitux Brand name for cetuximab
  • erdafitinib An orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, erdafitinib binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumor cell proliferation and tumor cell death in FGFR-overexpressing tumor cells. FGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival.
  • Ergamisol Brand name for levamisole hydrochloride
  • ergocalciferol Vitamin D2, a fat-soluble vitamin important for many biochemical processes including the absorption and metabolism of calcium and phosphorus. In vivo, ergocalciferol is formed after sun (ultraviolet) irradiation of plant-derived ergosterol, another form of vitamin D. Ergocalciferol is the form of vitamin D usually found in vitamin supplements.
  • eribulin mesylate 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.
  • eritoran tetrasodium 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.
  • Erivedge Brand name for vismodegib
  • ERK 1/2 inhibitor ASTX029 An orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. Upon administration, ASTX029 specifically binds to and inhibits both ERK 1 and 2, thereby preventing the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The MAPK/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in the proliferation, differentiation and survival of tumor cells.
  • ERK inhibitor CC-90003 An orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, CC-90003 inhibits ERK activity, and prevents the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
  • ERK inhibitor GDC-0994 An orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
  • ERK inhibitor LTT462 An orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, LTT462 binds to and inhibits ERK, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in numerous tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
  • ERK1/2 inhibitor KO-947 An inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. Upon intravenous administration, KO-947 specifically binds to and inhibits both ERK 1 and 2, thereby preventing the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The MAPK/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in the proliferation, differentiation and survival of tumor cells.
  • ERK1/2 inhibitor LY3214996 An orally available inhibitor of extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity. Upon oral administration, LY3214996 inhibits both ERK 1 and 2, thereby preventing the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The MAPK/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.
  • Erleada Brand name for apalutamide
  • erlotinib hydrochloride The hydrochloride salt of a quinazoline derivative with antineoplastic properties. Competing with adenosine triphosphate, erlotinib reversibly binds to the intracellular catalytic domain of epidermal growth factor receptor (EGFR) tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation.
  • ertapenem sodium 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.
  • ertumaxomab 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.
  • Erwinaze Brand name for asparaginase Erwinia chrysanthemi
  • ERYC Brand name for erythromycin
  • Ery-Tab Brand name for erythromycin
  • erythrocyte-encapsulated L-asparaginase suspension A suspension of erythrocytes encapsulating L-asparaginase with potential antineoplastic activity. Upon administration of erythrocyte-encapsulated L-asparaginase suspension, L-asparagine is hydrolyzed to L-aspartic acid and ammonia in plasma, thereby depleting tumor cells of asparagine. Due to low asparagine synthetase activity in tumor cells, de novo synthesis of asparagine is suppressed within tumor cells. Shortage of asparagine prevents synthesis of important proteins necessary for tumor cell growth. Encapsulation of asparaginase in erythrocytes decreases the immunogenicity of exogenous protein, enhances its circulation time and may limit toxicity.
  • 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.
  • escitalopram oxalate 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.
  • Eskalith Brand name for lithium carbonate
  • esmolol The hydrochloride salt form of esmolol, a short, rapid-acting, selective beta-adrenergic receptor blocker, devoid of intrinsic sympathomimetic activity, and with anti-arrhythmic, antihypertensive and potential analgesic activities. Upon intravenous administration, esmolol binds to and blocks the beta-1 receptor in the myocardium thereby preventing the action of epinephrine and norepinephrine. This leads to a reduction in the force and rate of cardiac contractions and thereby preventing tachycardia, arrythmias and/or hypertension. At higher doses, esmolol also blocks beta-2 receptors located in bronchial and vascular smooth muscle, thereby leading to smooth muscle relaxation. In addition, esmolol exerts a peripheral analgesic effect and intraoperative use of this agent may decrease the amount of opioid administration postoperatively. As the ester moiety in esmolol is rapidly hydrolyzed byplasma esterases, this agent has a very short half-life.
  • esomeprazole magnesium The magnesium salt of esomeprazole, the S-isomer of omeprazole, with gastric proton pump inhibitor activity. In the acidic compartment of parietal cells, esomeprazole is protonated and converted into the active achiral sulphenamide; the active sulphenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. H+/K+ ATPase is an integral membrane protein of the gastric parietal cell.
  • esorubicin 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.


An herbal formula containing burdock root (Arctium lappa), Turkey rhubarb root (Rheum palmatum), sheep sorrel (Rumex acetosella), and slippery elm bark (Ulmus fulva) with potential immunostimulating, anti-inflammatory and anti-tumor activities. The exact chemical profile, their respective concentrations and the mechanism of action of Essiac are largely unknown due to the proprietary nature of the formula and product inconsistency. Several chemical classes in Essiac are consistently represented and may attribute to its therapeutic effect, including anthraquinone derivatives such as rhein and emodin, high molecular polysaccharides, and lignans such as arctigenin. However, all these chemicals are unlikely to occur in high concentrations in Essiac, and its potential therapeutic effect may be attributed to a potential synergistic effect of these various compounds.

Brand name for ethinyl estradiol

Brand name for therapeutic estradiol

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.

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.

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.

Brand name for estradiol vaginal ring

A vaginal gel formulation containing a very low concentration of the estrogen estriol, that can be used for hormone replacement. Upon topical application to the vagina, estriol maintains adequate levels of estrogen in the vagina, and decreases vaginal atrophy and its associated symptoms, such as vaginal dryness and itching.

Brand name for diethylstilbestrol

Brand name for transdermal estrogen

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.

Brand name for diethylstilbestrol

Brand name for rigosertib sodium

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.

A recombinant soluble dimeric fusion protein consisting of the extracellular ligand-binding region of recombinant human tumor necrosis factor (rhTNF) receptor attached to the constant (Fc) region of human immunoglobulin G (FcIgG). The receptor moiety of etanercept binds to circulating TNF (2 molecules of TNF per receptor) and inhibits its attachment to endogenous TNF cell surface receptors, thereby rendering TNF inactive and inhibiting TNF-mediated mechanisms of inflammation.

A 2-nitroimidazole with radiosensitizing properties. Etanidazole depletes glutathione and inhibits glutathione transferase, thereby enhancing the cytotoxicity of ionizing radiation. This agent may also be useful as an imaging agent for identifying hypoxic, drug-resistant regions of primary tumors or metastases.

A humanized monoclonal IgG1 antibody directed against the vitronectin receptor alpha v beta 3 integrin. Etaracizumab blocks the binding of ligands, such as vitronectin, to alpha v beta 3 integrin, resulting in inhibition of angiogenesis and metastasis. Alpha v beta 3 integrin is a cell adhesion and signaling receptor that is expressed on the surface of tumor vessel endothelial cells, some tumor cells, and a number of other cell types.

A calcimimetic and calcium-sensing receptor (CaSR) agonist composed of a synthetic peptide comprised of seven D-amino acids that can be used to treat secondary hyperparathyroidism (sHPT) in hemodialysis patients with chronic kidney disease (CKD). Upon intravenous administration, etelcalcetide mimics calcium and allosterically binds to and activates the CaSR expressed by the parathyroid gland. This suppresses the synthesis and secretion of parathyroid hormone (PTH), thereby reducing PTH levels and lowering serum calcium and phosphorus levels. Elevated PTH is often observed in patients with CKD and is associated with dysregulated calcium-phosphate homeostasis.

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.

An orally bioavailable organoselenium inhibitor of thioredoxin reductase 1 (TrxR1), with potential antineoplastic activity. Upon oral administration, ethaselen specifically binds to the selenocysteine-cysteine redox pair in the C-terminal active site of TrxR1 and inhibits its activity, which may result in growth inhibition and the induction of apoptosis in TrxR1-overexpressing tumor cells. TrxR1, upregulated in many cancer cell types, plays a key role in various redox-dependent cellular pathways, regulates transcription factor activity, inhibits apoptosis, and promotes cell growth and survival.

Brand 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 combination of two steroid sex hormones, an estrogen and a progestin, used for contraceptive purposes. Estradiol, the endogenous counterpart of ethinyl estradiol (EE), is the principal, most potent estrogen hormone produced by the ovaries and is vital to the maintenance of fertility and secondary sexual characteristics in females. Levonorgestrel is a synthetic progestogen. This drug combination prevents or delays ovulation and causes a variety of hormonal changes. Ethinyl estradiol inhibits the release of follicle stimulating hormone (FSH), thus suppressing the development of ovarian follicle; levonorgestrel inhibits the release of luteinizing hormone (LH), thus preventing ovulation. This combination of agents alters the endometrium in such a way as to discourage implantation.

An oral contraceptive formulation containing the semisynthetic estrogen, ethinyl estradiol, combined with the synthetic progestin, norethindrone, with estrogenic and progestogenic activities, respectively. Ethinyl 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, activates the transcription of genes involved in the maintenance of the female reproductive system, inhibits the release of follicle stimulating hormone (FSH) from the anterior pituitary, and suppresses the development of the ovarian follicle. Norethindrone binds to intracellular progesterone receptors in progesterone-responsive tissues, such as the pituitary and those found in the reproductive system, and the activated ligand/receptor complex interacts with specific progesterone response elements on DNA, which results in the alteration in protein synthesis, the inhibition of ovulation, an increase in cervical mucus production, the induction of the secretory phase of the endometrial cycle, and the inhibition of luteinizing hormone (LH) release. The combination of an estrogen with a progestin suppresses the hypothalamic-pituitary system and alters the structure of the endometrium to discourage implantation.

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.

A mouthwash containing ethyl alcohol, with topical antibacterial activity. Upon rinsing the oral cavity with the ethyl alcohol mouthwash, ethyl alcohol denatures bacterial proteins, and dissolves and disrupts the bacterial lipid membrane, thereby killing the bacteria. This reduces oral colonization with harmful bacteria and may prevent oral mucositis.

A highly purified omega-3 fatty acid that can decrease serum triglyceride levels. Ethyl icosapentate reduces serum triglycerides without an increase in LDL cholesterol, but increases the cholesterol and triglyceride content in skeletal muscle.

A non-adhesive, non-absorbable, permanent liquid embolic agent comprised of ethylene vinyl alcohol (EVOH) copolymer dissolved in dimethyl sulfoxide (DMSO), and of micronized tantalum powder that can be used to occlude blood vessels. Upon administration of the EVOH-based embolic agent, contact with fluids, such as blood, induces the solidification of EVOH into a sponge-like material. This causes occlusion of blood vessels and prevents blood flow to the treated area.

Brand name for amifostine

A synthetic conjugate composed of the bisphosphonate etidronate linked to the cytostatic agent and antimetabolite cytarabine, with potential antineoplastic and antiresorptive activities. Upon intravenous administration of the etidronate-cytarabine conjugate MBC-11, the etidronate moiety targets bone and the two moieties are released upon hydrolysis of the phospho-ester bond locally. Etidronate binds to hydroxyapatite crystals in bone tissues and prevents its resorption. This prevents bone destruction and induces bone cell mineralization. In addition, the bone-targeting nature of this agent allows for the accumulation of cytarabine in bone tissue, where it is able to exert its antitumor effect locally by competing with cytidine for incorporation into DNA, thereby inhibiting DNA synthesis, while reducing systemic exposure. This leads to a destruction of bone-associated tumor cells, an inhibition of tumor cell proliferation and bone metastasis, and prevents tumor-mediated bone destruction.

Brand name for buserelin

An extended-release (ER) formulation composed of irinotecan, which is a semisynthetic derivative of camptothecin and a topoisomerase I-inhibitor prodrug, that is conjugated, via a proprietary biodegradable ester-based linker, to polyethylene glycol (PEG), with antineoplastic activity. Upon administration of etirinotecan pegol (EP), the agent penetrates into the leaky tumor vasculature and accumulates in the tumor. The linker slowly hydrolyzes and releases irinotecan, which leads to sustained exposure of the tumor to irinotecan. In turn, irinotecan is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN38) by a carboxylesterase. SN38 inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA; this results in DNA breaks that inhibit DNA replication and trigger apoptosis. Pegylation provides improved systemic exposure, increases drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile.

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.

Brand name for etoposide phosphate

A semisynthetic derivative of podophyllotoxin, a substance extracted from the mandrake root Podophyllum peltatum. Possessing potent antineoplastic properties, etoposide binds to and inhibits topoisomerase II and its function in ligating cleaved DNA molecules, resulting in the accumulation of single- or double-strand DNA breaks, the inhibition of DNA replication and transcription, and apoptotic cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle.

A phosphate salt of a semisynthetic derivative of podophyllotoxin. Etoposide binds to the enzyme topoisomerase II, inducing double-strand DNA breaks, inhibiting DNA repair, and resulting in decreased DNA synthesis and tumor cell proliferation. Cells in the S and G2 phases of the cell cycle are most sensitive to this agent.

A prodrug of etoposide, a semisynthetic derivative of podophyllotoxin extracted from the mandrake root Podophyllum peltatum, with potential antineoplastic activity. Upon intravenous administration of the etoposide prodrug CAP7.1, etoposide is released after enzymatic cleavage of CAP7.1 by specific carboxylesterases (CE) 1 and 2, which are upregulated in certain tumor cell types. Etoposide acts primarily in the G2 and S phases of the cell cycle. This drug binds to and inhibits topoisomerase II, an enzyme elevated in tumor cells. This results in the accumulation of double-strand DNA breaks, the inhibition of DNA replication and transcription and the induction of apoptotic cell death. The tumor-specific activation of etoposide increases its efficacy while lowering its systemic toxicity.

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.

Brand name for hycanthone

Brand name for acitretin

A proprietary biologic that inhibits the transcriptional-promoting activity of E26 transformation-specific (Ets, E-twenty-six) family transcription factors, with potential antineoplastic activity. Although the exact mechanism(s) of action through which this agent exerts its effect has yet to be fully elucidated, upon administration, Ets-family transcription factor inhibitor TK216 inhibits transcriptional activation mediated by Ets family proteins, including the oncogenic Ewing sarcoma breakpoint region 1/Friend leukemia virus integration 1 (EWSR1/FLI1; EWS/FLI1) fusion protein. This agent may both inhibit the malignant downstream effects mediated by genomic rearrangements that result in the overexpression of Ets family transcription factors and decrease tumor cell growth and proliferation. A chromosomal translocation t(11;22)(q24;q12) fuses the EWSR1 gene and the FLI1 gene and encodes the EWSR1/FLI1 fusion protein, which is an oncoprotein expressed by peripheral primitive neuroectodermal (pPNET) tumors.

Brand name for therapeutic lotion

A cream containing Evaux thermal spring water, with potential moisturizing and skin protecting activities. Upon application to the skin, Evaux spring water-based cream forms a protective barrier, which prevents water loss, provides moisture to the skin, protects the skin from damage, and soothes irritated skin. The Evaux thermal spring water contains the trace elements lithium and manganese which may help heal the skin.

A skin spray composed of Evaux thermal spring water, the emulsifier polysorbate 20, the preservatives phenoxyethanol and chlorphenesin, zinc gluconate, and the moisturizer caprylyl glycol with prophylactic and calming activity. Evaux thermal spring water is rich in mineral elements particularly of lithium, strontium and manganese. When sprayed directly onto the skin or scalp, this topical spray may have a calming, moisturizing, healing and nurturing effect. This agent may prevent or decrease skin rashes associated with the administration of EGFR inhibitors or with radiochemotherapy-induced skin reactions.

A topical solution containing Evaux thermal spring water, with potential moisturizing and skin protecting activities. Upon application to the nails and surrounding skin, Evaux spring water-based solution forms a film on the nails that serves as a protective barrier. This prevents water loss from, provides moisture to, and strengthens the nails, and protects them from damage. The solution also relieves pain caused by cracked, peeled, thinning or soft nails. Evaux thermal spring water contains the elements lithium, manganese and strontium which may help heal the nails and prevent onycholysis. It also contains chlorphenesin and piroctone olamine, both of which have antifungal activity. Some chemotherapy and/or radiation therapy can induce damage to the nails.

A derivative of the natural macrocyclic lactone sirolimus with immunosuppressant and anti-angiogenic properties. In cells, everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. Inhibition of mTOR activation results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2, IL-4, and IL-15) stimulation and the inhibition of antibody production.

Tablets for oral suspension containing everolimus, a derivative of the natural macrocyclic lactone sirolimus, with immunosuppressive and antineoplastic activities. After suspension of the everolimus tablets in water and oral administration, this agent inhibits the activation of the serine/threonine kinase mammalian target of rapamycin (mTOR) by binding to mTOR's cytosolic receptor immunophilin FK Binding Protein-12 (FKBP-12). Inhibition of the mTOR complex may result in the inhibition of the phosphatidylinositol 3 kinase/Akt/mTOR pathway and an inhibition in the expression of vascular endothelial cell growth factor (VEGF) and hypoxia-inducible factor. Ultimately, this may result in decreased tumor cell proliferation and tumor angiogenesis. This pediatric formulation can dissolve easily in a small volume of water making it easier to swallow and is available in smaller dose increments thereby allowing for greater dosing flexibility.

A chemotherapy regimen consisting of everolimus and exemestane that is used as a treatment for hormone receptor (HR)-positive and HER-2/neu-negative metastatic or advanced breast cancer.

Brand name for testosterone enanthate

Brand name for raloxifene hydrochloride

A cancer vaccine composed of enveloped virus-like particles (eVLPs) containing the human cytomegalovirus (CMV) antigens glycoprotein B (gB) and phosphoprotein 65 (pp65; UL83) that are combined with the immunoadjuvant granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulatory and antineoplastic activities. Upon intradermal administration of VBI-1901, the eVLPs are taken up by and activate immune cells, such as dendritic cells (DCs), thereby stimulating the immune system to exert a cytotoxic T-lymphocyte (CTL) immune response against CMV gB and pp65-expressing tumor cells. This may lyse and inhibit the proliferation of CMV-infected cancer cells. eVLPs, derived from viral structural proteins, stimulate the immune system and promote CTL responses. CMV gB and pp65 are expressed in certain tumor cell types, such as glioblastoma multiforme (GBM). GM-CSF stimulates the immune system and potentiates the antitumor immune response.

An orally available calcium receptor (CaR) modulator, with potential calcimimetic activity. Upon administration, evocalcet allosterically binds to and inhibits the activity of CaR, thereby suppressing the production of serum parathyroid hormone (PTH) and prevents the PTH-mediated efflux of calcium from bone and normalizes calcium levels.

A hypoxia-activated prodrug of the cytotoxin bromo-isophosphoramide mustard (Br-IPM) conjugated with 2-nitroimidazole, with potential antineoplastic activity. When exposed to hypoxic conditions, such as those found in hypoxic tumors, the 2-nitroimidazole moiety of evofosfamide is reduced. This releases the DNA-alkylating Br-IPM moiety, which introduces intra- and inter-strand DNA crosslinks in nearby cells; the crosslinks inhibit both DNA replication and cell division, and may lead to apoptosis of cells in the tumor. The inactive form of the prodrug is stable under normoxic conditions, which may limit systemic toxicity. Check for active clinical trialsusing this agent.

Brand name for melphalan hydrochloride

Brand name for Evaux thermal spring water-based solution

Brand name for Evaux spring water-based cream

Brand name for cevimeline hydrochloride

Autologous human lymph node T-lymphocytes, with potential immunostimulatory and antineoplastic activity. Upon collection of immune cells from the tumor-draining lymph node, the human lymph node lymphocytes are activated with anti-CD3/anti-CD28 microbeads, cultured with recombinant, human interleukin-2 (IL-2), expanded and isolated ex vivo. Upon reintroduction into the patient, the ex vivo-activated autologous lymph node lymphocytes recognize and lyse the tumor cells.

A preparation of autologous cytotoxic T lymphocytes, specifically recognizing certain tumor-associated antigens (TAAs), with potential antineoplastic activity. The endogenous T cells are isolated, expanded ex vivo, and reintroduced back into the patient. Upon administration, the ex vivo-expanded autologous T cells IMA101 target and kill tumor cells. The T cells are analyzed beforehand for their ability to specifically recognize certain TAAs, based on a proprietary antigen warehouse.

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.

A semisynthetic, water-soluble derivative of camptothecin with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues.

Brand name for rivastigmine tartrate

A synthetic androgen analogue. Exemestane 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.

A 39 amino acid peptide and synthetic version of exendin-4, a hormone found in the saliva of the venomous lizard Gila monster, with insulin secretagogue and antihyperglycemic activity. Exenatide is administered subcutaneously and mimics human glucagon-like peptide-1 (GLP-1). Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.

A truncated form of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 peptide, with GLP-1 receptor (GLP-1R) antagonistic and GLP-1R-mediated signaling inhibiting activities. Upon administration, exendin 9-39 competitively binds to and inhibits the activity of GLP-1R, thereby inhibiting GLP-1/GLP-1R-mediated signaling. This antagonizes the glucagonostatic and the insulinotropic effects of GLP-1. By abrogating GLP-1-mediated simulation of insulin release and reduction of glucagon secretion after food intake, exendin 9-39 may be used to help study the potential effects of overproduction of GLP-1 on food intake, weight loss and glucose levels. GLP-1R, located on pancreatic beta cells, is overexpressed on certain tumor cell types. GLP-1 is a gastrointestinal (GI) and insulinotropic hormone that is released after a meal and plays a key role in the regulation of blood glucose levels.

Brand name for ADH-1

An inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac. After oral administration, sulindac undergoes extensive biotransformation including irreversible oxidation to sulindac sulfone. Approximately, one half of an administered dose of sulindac is eliminated through the urine, mostly as the conjugated sulfone metabolite.

Brand name for deferasirox

A preparation of umbilical cord blood (UCB) co-cultured and expanded in an optimized culture system with a small molecule agonist of hematopoietic stem cell (HSC) renewal, with potential use in hematopoietic cell transplantation (HCT). Upon administration, the ECT-001 expanded cord blood cells increase and restore the number of hematopoietic stem and progenitor cells (HSPCs) that can differentiate into a variety of cell types and promote blood cell recovery. Compared to untreated UBCs, ECT-001 expanded UCB cells may exhibit enhanced stem cell proliferation and engraftment.

A population of ex vivo expanded, CD34-positive-enriched hematopoietic progenitor cells (HPCs), which are derived from allogeneic human umbilical cord blood (UCB), and are co-cultured and expanded with a proprietary preparation of human endothelial cells (ECs), which are genetically modified with an adenovirus (Ad) vector that includes the Ad E4 region that encodes the ORF1 (E4ORF1) gene, that can be used for transplantation. Upon transplantation of the expanded cord blood stem cells mixed with engineered human ECs AB-110, the UCB-derived cells can differentiate into a variety of cell types and promote blood cell recovery. Compared to bone marrow transplants, these HPCs demonstrate a decreased risk of causing graft-versus-host disease (GvHD), increase survival and enhance the potential for transplant and engraftment in any given patient as there is no need for a matched donor. Compared to HPCs alone, inclusion of the ECs increases blood stem cell count, enhances engraftment potential and increases the chances for blood cell recovery, thereby further increasing the potential for a successful cord blood transplantation. Insertion of the Ad E4ORF1 gene enhances survival and replication of the ECs ex vivo, preserves the ECs' vascular functions and improves the ability of the ECs to secrete angiocrines, which promotes stem cell proliferation and increases engraftment.

A preparation of gamma delta T lymphocytes derived from donor T cells that have been expanded and activated ex-vivo and further depleted of alpha and beta T-cell receptors (TCRs), with potential immunomodulating and antineoplastic activities. Upon administration, these expanded/activated gamma delta (EAGD) T cells secrete interferon-gamma (IFN-g) and exert direct killing of tumor cells. In addition, these cells activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against tumor cells. Gamma delta T lymphocytes play a key role in the activation of the immune system and do not require major histocompatibility complex (MHC)-mediated antigen presentation to exert their cytotoxic effect.

Brand name for bupivacaine hydrochloride liposome injectable suspension

An extended release (ER) injectable formulation composed of the hydrochloride salt form of bupivacaine, an amide-type, long-acting local anesthetic, in a resorbable sucrose acetate isobutyrate-based matrix, with analgesic activity. Following administration in or around a specific site, ER bupivacaine is released from the matrix over an extended period of time. Upon release, bupivacaine reversibly binds to specific voltage-gated sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions, membrane destabilization, and depolarization inhibition thus disrupting nerve impulse conduction. This eventually leads to a reversible loss of sensation. This formulation may provide pain relief up to 72 hours.

An extended release (ER) oral tablet that contains flucytosine (5-FC), a fluorinated cytosine analog, with antifungal activity and potential anti-cancer activity. Following oral administration of ER 5-FC, the 5-FC is deaminated to its active metabolite 5-fluorouracil (5-FU). 5-FU replaces uracil during RNA synthesis, which consequently inhibits downstream protein synthesis. In addition, 5-FU is metabolized further to 5-fluorodeoxyuridylic acid monophosphate, which inhibits thymidylate synthetase. Inhibition of this enzyme interrupts nucleotide synthesis, DNA replication and cell proliferation. Negative regulation of protein synthesis, DNA replication and cell proliferation can lead to cell death. Following ingestion of ER 5-FC, intravenous injection of a retroviral vector encoding cytosine deaminase (TC 511) at a tumor site may result in higher local concentrations of 5-FU and its metabolites, and increased tumor cell death than other 5-FU treatment regimens.

An extended-release (ER) formulation of the hydrobromide salt form of galantamine, a tertiary alkaloid obtained synthetically or naturally from the bulbs and flowers of Narcissus and several other genera of the Amaryllidaceae family, with anticholinesterase and neurocognitive-enhancing activities. Upon administration, galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). In addition, galantamine is a ligand for nicotinic acetylcholine receptors, which may increase the presynaptic release of Ach and activate postsynaptic receptors. This agent may improve neurocognitive function in mild and moderate Alzheimer's disease and may, through its Ach stimulating effect on nicotinic receptors, help quit smoking and reduce abstinence-induced cognitive symptoms that promote smoking relapse.

An extended-release (ER), polymer-based injectable formulation containing the indazole derivative granisetron, a selective serotonin (5-hydroxytryptamine; 5-HT) receptor type 3 (5-HT3) antagonist, with anti-emetic activity. Upon subcutaneous administration, granisetron is released from the polymer in a sustained manner, which is based upon the controlled hydrolysis of the polymers, and selectively binds to and inhibits the activity of the 5-HT3 receptors located peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema. By preventing stimulation of 5-HT3 receptors, granisetron is able to suppress chemotherapy-induced nausea and vomiting (CINV). Compared to the injection of granisetron alone, injection of the polymer-based formulation allows for therapeutic levels of granisetron over an extended period of time.

A wax microsphere capsule formulation of oxycodone, a semi-synthetic, morphine-like opioid alkaloid, with analgesic activity. Upon administration, oxycodone exerts its analgesic activity by binding to the mu-receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opioids. Due to the unique formulation, extended-release microsphere capsule-based oxycodone may provide an identical pharmacokinetic profile regardless of whether the capsule is intact when ingested or if ingested via enteral feeding tube, leading to a predictable level of analgesia in patients that must be transitioned from oral to enteral administration.

An extended-release (ER) formulation of onapristone, an orally bioavailable progesterone receptor (PR) antagonist, with antineoplastic activity. Onapristone binds to the PR and inhibits both PR activation and the associated expression of PR-responsive genes. This may inhibit PR-mediated proliferative effects in cancer cells overexpressing PR. PR is expressed on certain cancer cell types and plays a key role in proliferation and survival.

Brand name for acetylsalicylic acid

Brand name for povidone-iodine solution

Brand name for povidone-iodine solution

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.

An azetidinone derivative and a cholesterol absorption inhibitor with lipid-lowering activity. Ezetimibe appears to interact physically with cholesterol transporters at the brush border of the small intestine and inhibits the intestinal absorption of cholesterol and related phytosterols. As a result, ezetimibe causes a decrease in the level of blood cholesterol or an increase in the clearance of cholesterol from the bloodstream. Overall, the following effects observed are a reduction of hepatic cholesterol stores and a reduction of total cholesterol, LDL cholesterol, and other triglycerides in the blood.

An orally bioavailable combination agent containing the cholesterol absorption inhibitor ezetimibe and the hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitor simvastatin, with lipid-lowering activity. Upon oral administration, ezetimibe binds to the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1) at the brush border of the small intestine and inhibits the intestinal absorption of biliary and dietary cholesterol and related phytosterols. This decreases blood cholesterol levels, decreases the delivery of intestinal cholesterol to the liver, reduces hepatic cholesterol stores and enhances the clearance of cholesterol from the bloodstream. Upon administration of simvastatin and subsequent hydrolyzation to its active beta-hydroxyacid form, this statin competitively inhibits HMG-CoA reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, which is an essential step in cholesterol synthesis. Ezetimibe and simvastatin together reduce blood levels of total cholesterol, low-density lipoprotein cholesterol (LDL-C), triglycerides (TGs), very-low-density lipoproteins (VLDL), and apolipoprotein B (Apo B), and increase the plasma concentration of high-density lipoprotein cholesterol (HDL-C). Higher cholesterol blood levels appear to be associated with an increased risk in the proliferation of certain cancer cells, such as prostate cancer cells.

An orally available selective inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and 2 (EZH2), with potential antineoplastic activity. Upon oral administration, DS-3201 selectively inhibits the activity of both wild-type and mutated forms of EZH1 and EZH2. Inhibition of EZH1/2 specifically prevents the methylation of lysine 27 on histone H3 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways, enhances transcription of certain target genes, and results in decreased proliferation of EZH1/2-expressing cancer cells. EZH1/2, histone lysine methyltransferase (HMT) class enzymes and catalytic subunits of the polycomb repressive complex 2 (PRC2), are overexpressed or mutated in a variety of cancer cells and play key roles in tumor cell proliferation, progression, stem cell self-renewal and migration.

An orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity. Upon oral administration, CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, a histone lysine methyltransferase (HMT) class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis.

An orally available selective inhibitor of the histone lysine methyltransferase (HMT) enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral administration, EZH2 inhibitor PF-06821497 selectively targets, binds to and inhibits the activity of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, an HMT class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis.

An orally available selective inhibitor of the histone lysine methyltransferase (HMT) enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral administration, EZH2 inhibitor SHR2554 selectively targets, binds to and inhibits the activity of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, an HMT class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis.  

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