Drug Dictionary


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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Ecotrin

(Other 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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Edecrin

(Other 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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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 ofT lymphocytes to endothelial cells, and migration of T lymphocytes to sites of inflammation. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Effexor

(Other name for: venlafaxine)

eflornithine

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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 patients 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. Check for active clinical trials using this agent. (NCI Thesaurus)

Efudex

(Other name for: topical fluorouracil)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

EGFR inhibitor HM61713

An orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. EGFR inhibitor HM61713 binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. 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 the EGFR wild type form. Check for active clinical trials using this agent. (NCI Thesaurus)

EGFR mutation-selective inhibitor AC0010MA

An orally available, third generation, selective inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), including the second-site resistance mutation T790M, with potential antineoplastic activity. EGFR mutant-selective inhibitor AC0010MA specifically and irreversibly binds to and inhibits the activity of mutant forms of EGFR, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared to some other EGFR inhibitors, AC0010MA may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent does not inhibit wild-type EGFR (EGFRwt), and does not cause dose-limiting toxicities that occur during the use of non-selective EGFR inhibitors, which also inhibit EGFRwt. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent.

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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