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• Cancer Drugs

- A -

• A-007

The phenylhydrazone 4,4'-dihydroxybenzophenone-2,4-dinitrophenylhydrazone formulated as a topical agent with immunomodulating and potential antineoplastic activities. Applied topically as a 0.25% gel, A-007 may stimulate a local immune response against human papillomavirus (HPV)-induced cervical intraepithelial neoplasia (CIN).



• Abegrin

(Other name for: monoclonal antibody anti-alpha V beta 3 integrin)



• Aberel

(Other name for: tretinoin)



• Abitrexate

(Other name for: methotrexate)



• Abraxane

(Other name for: paclitaxel albumin-stabilized nanoparticle formulation)



• ABT-510

A synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).



• ABT-751

An orally bioavailable antimitotic sulfonamide. ABT-751 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication. This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect.



• ABT-888

A poly(ADP-ribose) polymerase (PARP) -1 and -2 inhibitor with chemosensitizing and antitumor activities. With no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents. PARP nuclear enzymes are activated by DNA single or double strand breaks, resulting in the poly(ADP-ribosyl)ation of other nuclear DNA binding proteins involved in DNA repair; poly(ADP-ribosyl)ation contributes to efficient DNA repair and to survival of proliferating cells exposed to mild genotoxic stresses as induced by as oxidants, alkylating agents or ionizing radiation.



• Accutane

(Other name for: isotretinoin)



• acetylsalicyclic acid

An orally administered non-steroidal antiinflammatory agent. Acetylsalicylic acid binds to and acetylates serine residues in cyclooxygenases, resulting in decreased synthesis of prostaglandin, platelet aggregation, and inflammation. This agent exhibits analgesic, antipyretic, and anticoagulant properties.



• Achromycin

(Other name for: tetracycline hydrochloride)



• ACNU 50

(Other name for: nimustine)



• Actigall

(Other name for: ursodiol)



• Actimmune

(Other name for: interferon gamma)



• Actinex

(Other name for: nordihydroguaiaretic acid)



• Actiq

(Other name for: fentanyl citrate)



• Activase

(Other name for: recombinant tissue plasminogen activator)



• ActiVin

(Other name for: IH636 grape seed proanthocyanidin extract)



• Actonel

(Other name for: risedronate)



• Actos

(Other name for: pioglitazone hydrochloride)



• Ad5CMV-p53 gene

A replication-defective adenoviral-CMV vector that encodes a wild-type p53 gene. Ad5CMV-p53 induces tumor cells that have been transfected with the vector to produce wild-type p53, a tumor suppressor gene that is deleted or mutated in a significant number of cancers. In transfected tumor cells, the wild-type p-53 gene product exerts an antitumor effect by blocking cell cycle progression at the G1/S regulation point, activating DNA repair proteins in the presence of DNA damage, and initiating apoptosis when DNA damage is irreparable.



• Adderall XR

(Other name for: dextroamphetamine-amphetamine)



• adenovector encoding MDA7

A nonreplicating adenoviral vector (adenovector) encoding the melanoma differentiation-associated 7 gene (MDA7) with potential antineoplastic activity. After intratumoral injection and adenovector-mediated gene transfer of MDA7 into tumor cells, the expressed MDA7 transgene may inhibit tumor cell proliferation and induce tumor cell apoptosis.



• adenovirus

One of a number of genetically-engineered adenoviruses designed to insert a gene of interest into a eukaryotic cell where the gene of interest is subsequently expressed. Unlike most other vectors, adenovirus vectors have the ability to infect post-mitotic cells. Thus, these agents are especially useful for gene transfer into neuronal cells.



• adenovirus 5-tumor necrosis factor alpha

A recombinant agent consisting of a genetically-modified adenovirus 5 vector encoding the protein cytokine tumor necrosis factor (TNF) alpha. TNF exhibits potent anti-tumor cytolytic properties; the adenovirus 5 vector efficiently infects tumor cells, delivering tumor-specific TNF.



• ADH-1

A small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and anti-angiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, a transmembrane glycoprotein of the cadherin superfamily of proteins. Inhibition of N-cadherin-mediated cell-cell binding may lead to disruption of tumor vasculature, inhibition of tumor cell growth, and induction of apoptosis. Involved in calcium- mediated cell-cell adhesion and signaling mechanisms, N-cadherin is found on the surfaces of liver and colorectal tumor cells, and the endothelial cells and pericytes of tumor blood vessels.



• Adriamycin

(Other name for: doxorubicin hydrochloride)



• Adrucil

(Other name for: fluorouracil)



• ADVEXIN

(Other name for: Ad5CMV-p53 gene)



• AEE788

An orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and vascular endothelial growth factor receptor 2 (VEGF2), resulting in receptor inhibition, the inhibition of cellular proliferation, and induction of tumor cell and tumor-associated endothelial cell apoptosis.



• AEG35156

A second-generation synthetic antisense oligonucleotide with potential antineoplastic activity. AEG35156 selectively blocks the cellular expression of X-linked inhibitor of apoptosis protein (XIAP), a pivotal inhibitor of apoptosis that is overexpressed in many tumors. This agent reduces total levels of XIAP in tumor cells, working synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. XIAP interferes with both the intrinsic and extrinsic program-death signaling pathways, which may render tumor cells resistant to apoptosis.



• Aeroseb-Dex

(Other name for: dexamethasone)



• Aeroseb-HC

(Other name for: hydrocortisone)



• aerosolized liposomal 9-nitro-20 (S) camptothecin

An aerosolized liposomal preparation of a water-insoluble derivative of camptothecin with potential antineoplastic activity. 9-nitro-20 (S)-camptothecin and its active metabolite 9-aminocamptothecin (9-AC) selectively stabilize topoisomerase I-DNA covalent complexes during S-phase, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. This agent is formulated with dilauroylphosphatidylcholine and nebulized in particle sizes of 1.2-1.6 micrometer mass median aerodynamic diameter.



• Aflodac

(Other name for: sulindac)



• AFP gene hepatocellular carcinoma vaccine

A cancer vaccine composed of naked plasmid DNA of the gene for the tumor-associated antigen alpha-fetoprotein (AFP), a macromolecule that acts as a specific immunologic target for hepatocellular carcinoma. This agent exerts an antitumor effect by inducing cytotoxic T-lymphocytes to attack AFP-expressing tumor cells.



• AFP464

A synthetic, lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and anti-tumor activity. AFP464 is rapidly converted to the aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in CYP1A1 enzyme activity and, to a lesser extent, an increase in CYP1B1 enzyme activity and gene expression. Subsequently, aminoflavone is metabolized by the CYP1A1 and CYP1B1 enzymes that it induces. Toxic metabolites of aminoflavone covalently bind to DNA, thereby inhibiting cell proliferation and inducing apoptosis. Pulmonary toxicity may be a dose-limiting toxicity.



• AG-013736

An orally bioavailable tyrosine kinase inhibitor. AG-013736 inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platelet-derived growth factor receptor (PDGF), thereby exerting an anti-angiogenic effect.



• AG-024322

A cyclin-dependent kinase (CDK) inhibitor with antineoplastic activity. AG-024322 selectively inhibits cyclin-dependent kinases (particularly CDK1,2 and 4), enzymes that regulate cell cycle progression. Inhibition of CDK may result in cell cycle arrest, induction of apoptosis, and inhibition of DNA replication and tumor cell proliferation.



• AG-858

A recombinant cancer vaccine made with tumor-derived heat shock protein 70 (HSP70) peptide complexes. HSP70 associates with antigenic peptides, transporting them into antigen presenting cells (APC) for processing. Tumor-derived HSP70-peptide complexes used in vaccine preparations have been shown to prime tumor immunity and tumor-specific T cells in animal models.



• Aknoten

(Other name for: tretinoin)



• alanosine

An amino acid analog derived from Streptomyces alanosinicus, a purine antagonist, and an adenylosuccinate synthetase inhibitor with antineoplastic properties. L-alanosine deprives MTAP-deficient (salvage pathway) tumor cells of de novo synthesized adenosine and is probably responsible for diminished DNA synthesis. The clinical use of L-alanosine may be narrow due to its toxicity profile.



• Alba-Dex

(Other name for: dexamethasone)



• Aldara

(Other name for: imiquimod)



• aldesleukin

A recombinant analog of endogenous interleukin-2 (IL-2), a cytokine involved in intercellular communication related to cell differentiation, proliferation, inflammation, hematopoiesis, neuronal functions, and release of hormones. Aldesleukin binds to and activates specific receptors, triggering expression of specific genes, and may induce T cell-mediated tumor regression in some tumor types.



• alemtuzumab

A recombinant DNA-derived humanized monoclonal antibody directed against the cell surface glycoprotein, CD52. Alemtuzumab is an IgG1 kappa with human variable framework and constant regions, and complementarity-determining regions derived from a rat monoclonal antibody. This agent selectively binds to CD52, thereby triggering a host immune response that results in lysis of CD52 + cells. CD52 is a glycoprotein expressed on the surface of essentially all normal and malignant B and T cells, a majority of monocytes, macrophages and natural killer (NK) cells, a subpopulation of granulocytes, and tissues of the male reproductive system.



• Alferon

(Other name for: recombinant interferon alpha-2a)



• Alferon N

(Other name for: interferon alfa)



• alfuzosin hydrochloride

The hydrochloride salt of alfuzosin, a quinazoline compound with smooth muscle-relaxing activity. Alfuzosin selectively binds to and antagonizes post-synaptic alpha1-adrenoreceptors in smooth muscle of the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra, initiating relaxation of smooth muscle and resulting in improvement of urine flow and the symptoms of benign prostatic hyperplasia (BPH). This agent also blocks alpha1-adrenoreceptors in peripheral vascular smooth muscle, resulting in vasodilatation and a decrease in peripheral vascular resistance.



• ALIMTA

(Other name for: pemetrexed disodium)



• Alkeran

(Other name for: melphalan)



• allogeneic dendritic cell-myeloma idiotype vaccine

A cell-based vaccine composed of allogeneic dendritic cells pulsed ex -vivo with an autologous myeloma idiotype with potential antineoplastic activity. Upon administration, allogeneic dendritic cell-myeloma idiotype vaccine may stimulate the host immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against myeloma cells, resulting in cell lysis.



• allogeneic GM-CSF-secreting breast cancer vaccine

An allogenic vaccine consisting of irradiated breast cancer cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene. Upon vaccination, the genetically modified cells secrete GM-CSF, thereby potentiating a tumor-specific T cell response against breast cancer cell-asociated antigens.



• allogeneic lymphocytes

A population of lymphocytes therapeutically administered to a recipient individual who is genetically distinct from a donor of the same species.



• allogeneic tumor cell vaccine

A vaccine composed of tumor cells isolated from the tumor of one patient, killed and processed, and administered to another patient in order to stimulate cytotoxic immune responses to a similar tumor cell type. The cells found in this type of whole-cell vaccine express many cell-surface tumor-associated antigens. This vaccine is frequently administered with an adjuvant immunostimulant.



• allopurinol

A structural isomer of hypoxanthine. Allopurinol inhibits xanthine oxidase, an enzyme that converts oxypurines to uric acid. By blocking the production of uric acid, this agent decreases serum and urine concentrations of uric acid, thereby providing protection against uric acid-mediated end organ damage in conditions associated with excessive production of uric acid, i.e. the massive cell lysis associated with the treatment of some malignancies.



• Aloxi

(Other name for: palonosetron hydrochloride)



• alpha fetoprotein adenoviral vector vaccine

A vaccine consisting of a recombinant adenoviral vector encoding alpha fetoprotein. After vaccination, expressed alpha fetoprotein may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein, resulting in tumor cell lysis.



• alpha fetoprotein plasmid DNA vaccine

A vaccine consisting of plasmid DNA encoding alpha fetoprotein. After vaccination, expressed alpha fetoprotein may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein, resulting in tumor cell lysis.



• alpha-1,3-galactosyltransferase-expressing allogeneic pancreatic tumor cell vaccine

A cancer vaccine comprised of irradiated allogeneic pancreatic cancer cells transfected to express murine alpha-1,3-galactosyltransferase with antitumor activity. Vaccination results in murine alpha-1,3-galactosyltransferase-mediated expression of foreign alpha-1,3-galactosyl (alpha-gal) carbohydrate residues on cell membrane glycoproteins and glycolipids of the vaccine pancreatic cancer cell "xenograft"; these foreign alpha-gal epitopes, not present on human cells, then induce a hyperacute rejection of the vaccine pancreatic cancer cell xenograft. The hyperacute rejection involves pre-existing human anti-alpha-gal antibodies (naturally occur against gut flora) that bind the foreign alpha-gal epitopes, resulting in the rapid activation of complement and antibody-dependent cell-mediated cytotoxicity (ADCC). The host immune system then attacks pancreatic cancer cells, preexistent to vaccination and with cell membrane epitopes unmodified by alpha-gal, resulting in ADCC and tumor growth inhibition or reduction.



• alprostadil

The naturally occuring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Alprostadil is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.



• alum adjuvant

An inorganic compound containing aluminum. Used in various immunologic preparations to improve immunogenicity, alum adjuvant consists of aluminium sulfate. In vaccines, this agent binds to the protein conjugate, resulting in improved antigen processing by the immune system.



• alvimopan

A synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opiod-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.



• amantadine hydrochloride

The hydrochloride salt of amantadine, a synthetic tricyclic amine with antiviral, antiparkinsonian, and antihyperalgesic activities. Amantadine appears to exert its antiviral effect against the influenza A virus by interfering with the function of the transmembrane domain of the viral M2 protein, thereby preventing the release of infectious viral nucleic acids into host cells; furthermore, this agent prevents virus assembly during virus replication. Amantadine exerts its antiparkinsonian effects by stimulating the release of dopamine from striatal dopaminergic nerve terminals and inhibiting its pre-synaptic reuptake. This agent may also exert some anticholinergic effect through inhibition of N-methyl-D-aspartic acid (NMDA) receptor-mediated stimulation of acetylcholine, resulting in antihyperalgesia.



• Ambien

(Other name for: zolpidem tartrate)



• Amboclorin

(Other name for: chlorambucil)



• AMD3100

A bicyclam with hematopoietic stem cell-mobilizing properties. AMD3100 blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation.



• Amdray

(Other name for: PSC 833)



• Amfebutamone

(Other name for: bupropion hydrochloride)



• AMG 531

A recombinant protein with megakarypoiesis stimulating activity. AMG 531 mimics endogenous thrombopoietin (TPO), directly binding to and activating the platelet thrombopoietin receptor (TpoR, Mpl, or CD110 antigen), a cytokine receptor belonging to the hematopoietin receptor superfamily. Activation of TPO-R stimulates the proliferation and differentiation of megakaryocytes, resulting in an increase in the production of blood platelets.



• AMG 706

An orally bioavailable multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation.



• amifostine trihydrate

The trihydrate form of a phosphorylated aminosulfhydryl compound. After dephosphorylation of amifostine by alkaline phosphatase to an active free sulfhydryl (thiol) metabolite, the thiol metabolite binds to and detoxifies cytotoxic platinum-containing metabolites of cisplatin and scavenges free radicals induced by cisplatin and ionizing radiation. The elevated activity of this agent in normal tissues results from both the relative abundance of alkaline phosphatase in normal tissues and the greater vascularity of normal tissues compared to tumor tissues.



• aminolevulinic acid

A topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid (ALA) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect.



• amiodarone hydrochloride

The hydrochloride salt of an iodine-rich benzofuran derivative with antiarrhythmic and vasodilatory activities. As a class III antiarrhythmic agent, amiodarone blocks the myocardial calcium, potassium and sodium channels in cardiac tissue, resulting in prolongation of the cardiac action potential and refractory period. In addition, this agent inhibits alpha- and beta-adrenergic receptors, resulting in a reduction in sympathetic stimulation of the heart, a negative chronotropic effect, and a decrease in myocardial oxygen demands. Amiodarone may cause vasodilation by stimulation of the release of nitric oxide and cyclooxygenase-dependent relaxing endothelial factors.



• Ammoidin

(Other name for: methoxsalen)



• amonafide dihydrochloride

The dihydrochloride salt of amonafide, an imide derivative of naphthalic acid. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis.



• amonafide L-malate

The malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis.



• amoxicillin-clavulanate potassium

A combination of the semisynthetic broad-spectrum antibiotic amoxicillin and the beta-lactamase enzyme inhibitor clavulanate potassium. Clavulanate potassium increases the serum half-life of amoxicillin by inhibiting beta-lactamase-mediated metabolism of amoxicillin. Amoxicillin inhibits bacterial cell wall synthesis by binding to penicillin binding proteins and inhibiting peptidoglycan synthesis, a critical component of bacterial cell walls.



• amphotericin B deoxycholate

The deoxycholate salt of amphotericin B, a polyene antifungal antibiotic produced by Streptomyces nodosus, with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, resulting in depolarization of the membrane; alterations in cell membrane permeability and leakage of important intracellular components; and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells.



• ampicillin sodium/sulbactam sodium

A combination formulation of the sodium salts of the antibiotic ampicillin and the beta-lactamase inhibitor sulbactam with antibacterial activity. Ampicillin, a broad-spectrum, semisynthetic penicillin, binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall, thereby interfering with the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. As a result, the cell wall is weakened and the cell lyses. The sulbactam component irreversibly binds to bacterial beta-lactamase at or near its active site, thereby interfering with substrate binding and inhibiting bacterial metabolism of penicillin and cephalosporin beta-lactam antibiotics, effectively extending their antibiotic spectrum to include many beta-lactam-resistant bacteria.



• Ampligen

(Other name for: atvogen)



• Amplimexon

(Other name for: imexon)



• amrubicin hydrochloride

The hydrochloride salt of a third-generation synthetic 9-amino-anthracycline with antineoplastic activity. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds.



• amsacrine

An aminoacridine derivative with potent antineoplastic properties. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest.



• anakinra

A recombinant human nonglycosylated interleukin-1 (IL-1) receptor antagonist with potential antineoplastic activity. Anakinra binds to the IL-1 receptor, thereby blocking the binding of the IL-1 to and activation of its receptor. Blockade of IL-1 activity may inhibit the cascade of downstream pro-angiogenic factors such as vascular endothelial cell growth factor, tumor necrosis factor-alpha, and IL-6, resulting in inhibition of tumor angiogenesis.



• anastrozole

A nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth.



• Android-F

(Other name for: fluoxymesterone)



• Android-F

(Other name for: fluoxymesterone)



• Angelica sinensis extract

An herbal extract derived from the root of the plant Angelica sinensis with possible antiinflammatory, antispasmodic, vasodilatory, estrogenic, and antitumor activities. Angelica sinensis contains volatile oils, including safrole, isosafrole, and n-butylphthalide; coumarin derivatives, including psoralens, bergapten, osthol, imperatorin, and oxypeucedanin; and ferulic acid. The coumarin derivatives in this agent may vasodilate and relax smooth muscle and may exhibit additive anticoagulant effects. Ferulic acid, a phenolic phytochemical present in plant cell walls, may neutralize free radicals such as reactive oxygen species.\'c2\~In addition, Angelica sinensis extract has been shown to inhibit the growth and induce apoptosis of glioblastoma mutltiforme brain tumor cells through p53-dependent and p53-independent pathways.



• anidulafungin

A cyclic lipopeptide echinocandin derivative with antifungal activity. Anidulafungin inhibits 1,3 beta-D-glucan synthase, an enzyme involved in fungal cell wall synthesis, resulting in cell lysis and death. This agent is active against Candida species and Aspergillus.



• anti-EpCAM-Pseudomonas-exotoxin fusion protein

A fusion protein consisting of a human monoclonal antibody fragment specific for the epithelial cell adhesion molecule (EpCAM) conjugated with a truncated form of Pseudomonas exotoxin A with potential antineoplastic activity. Anti-EpCAM-Pseudomonas-exotoxin fusion protein binds to Ep-CAM-positive tumor cells, thereby delivering the Pseudomonas exotoxin A moiety specifically; the Pseudomonas exotoxin A moiety then inactivates elongation factor 2 (EF-2) through ADP ribosylation, resulting in inhibition of protein synthesis in target cells. EpCAM, a cell surface protein, is expressed by a variety of tumor cells and is frequently found in head and neck cancers.



• anti-IL-6 chimeric monoclonal antibody

A human-mouse chimeric antibody, constructed from a murine antiinterleukin 6 (IL-6) monoclonal antibody, with antitumor and antiinflammatory activities. Containing the antigen-binding variable region of the murine antibody, CLB-IL-6-8, and the constant region of a human IgG1kappa immunoglobulin, anti-IL-6 chimeric monoclonal antibody has high affinity for recombinant as well as native IL-6 and inhibits the binding of IL-6 to the IL-6 receptor (IL-6R), resulting in the blockade of the IL-6/IL-6R/gp130 signal transduction pathway, and, subsequently, antitumor and antiinflammatory activities.



• antineoplaston A10

A piperidinedione antineoplaston with potential antineoplastic activity. Antineoplaston A10 was originally isolated from human urine but is now synthetically derived. This agent intercalates into DNA, resulting in cell cycle arrest in G1 phase, reduction of mitosis, and decreased protein synthesis. Antineoplaston A10 may also inhibit ras-oncogene expression and activate tumor suppressor gene p53, leading to cell differentiation and apoptosis.



• antineoplaston AS2-1

A 4:1 mixture of phenylacetate and phenylacetylgluatmine, degradation products of the antineoplaston agent A10. Antineoplaston AS2-1 inhibits the incorporation of L-glutamine into tumor-cell proteins, leading to cell cycle arrest in the G1 phase and inhibition of mitosis. This agent may also inhibit RAS oncogene expression and activate tumor suppressor gene p53, resulting in cell differentiation and apoptosis.



• anti-thymocyte globulin

A purified gamma immunoglobulin with immunosuppressive properties. Obtained from rabbits that have been immunized with human thymocytes, antithymocyte globulin specifically recognizes and destroys T lymphocytes. Although the exact mechanism of action is not completely understood, it appears to involve T lymphocyte clearance from the circulation and modulation of T lymphocyte activity. Administering antithymocyte globulin with chemotherapy prior to stem cell transplantation may reduce the risk of graft-versus-host disease.



• Antrin

(Other name for: motexafin lutetium)



• Anzemet

(Other name for: dolasetron mesylate)



• apaziquone

A bioreductive prodrug and novel analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone alkylates DNA after actvation to its active metabolite in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. This agent may selectively sensitize hypoxic tumor cells to radiocytotoxicity.



• APC8015 vaccine

A cell-based vaccine composed of autologous antigen-presenting peripheral blood mononuclear cells (enriched for a dendritic cell fraction) that have been exposed to a recombinant protein consisting of granulocyte-macrophage colony-stimulating factor (GM-CSF) fused to prostatic-acid phosphatase (PAP), a protein expressed by prostate cancer cells. Upon administration, the vaccine may stimulate an antitumor T-cell response against tumor cells expressing PAP.



• APC8015F

A cell-based vaccine composed of previously frozen autologous antigen-presenting peripheral blood mononuclear cells (enriched for a dendritic cell fraction) that have been exposed to a recombinant protein consisting of granulocyte-macrophage colony-stimulating factor (GM-CSF) fused to prostatic-acid phosphatase (PAP), a protein expressed by prostate cancer cells. Upon administration, the vaccine may stimulate an antitumor T-cell response against tumor cells expressing PAP.



• apixaban

An orally active inhibitor of coagulation factor Xa with anticoagulant activity. Apixaban directly inhibits factor Xa, thereby interfering with the conversion of prothrombin to thrombin and preventing formation of cross-linked fibrin clots.



• Aplidin

(Other name for: plitidepsin)



• apolizumab

A humanized monoclonal antibody directed against 1D10, a polymorphic determinant on the HLA-DR beta chain that is expressed on normal and neoplastic B cells. Apolizumab induces complement-mediated cytotoxicity, antibody-dependent cell-mediated cytotoxicity, and apoptosis of 1D10 antigen-positive B cells in vitro.



• aprepitant

A small molecule, high-affinity substance P antagonist (SPA) with antiemetic activity. Crossing the blood brain barrier, aprepitant binds selectively to the human substance P/neurokinin 1 receptor in the central nervous system (CNS), thereby inhibiting receptor binding of endogenous substance P and substance P-induced emesis. This agent has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors.



• aprotinin bovine

A single chain polypeptide isolated from bovine lung with antifibrinolytic and anti-inflammatory activities. As a broad-spectrum serine protease inhibitor, aprotinin bovine competitively and reversibly inhibits the activity of a number of different esterases and proteases, including trypsin, chymotrypsin, kallikrein, plasmin, tissue plasminogen activator, and tissue and leukocytic proteinases, resulting in attenuation of the systemic inflammatory response (SIR), fibrinolysis, and thrombin generation. This agent also inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis.



• Aptosyn

(Other name for: exisulind)



• Aquadiol

(Other name for: estradiol)



• Aranesp

(Other name for: darbepoetin alfa)



• Arcoxia

(Other name for: etoricoxib)



• Aredia

(Other name for: pamidronate)



• arginine butyrate

The butyric acid salt of the amino acid arginine. In EBV-related lymphomas, arginine butyrate induces EBV thymidine kinase transcription and may act synergistically with the antiviral agent ganciclovir to inhibit cell proliferation and decrease cell viability. In addition, the butyrate moiety inhibits histone deacetylase, which results in hyperacetylation of histones H3 and H4. Acetylated histones have a reduced affinity for chromatin; this reduced histone-chromatin affinity may allow chromosomal unfolding, potentially enhancing the expression of genes related to tumor cell growth arrest and apoptosis.



• Aricept

(Other name for: donepezil hydrochloride)



• Arimidex

(Other name for: anastrozole)



• Arixtra

(Other name for: fondaparinux sodium)



• Aromasin

(Other name for: exemestane)



• Arranon

(Other name for: nelarabine)



• arsenic trioxide

A small-molecule arsenic compound with antineoplastic activity. The mechanism of action of arsenic trioxide is not completely understood. This agent causes damage to or degradation of the promyelocytic leukemia protein/retinoic acid receptor-alpha (PML/RARa) fusion protein; induces apoptosis in acute promyelocytic leukemia (APL) cells and in many other tumor cell types; promotes cell differentiation and suppresses cell proliferation in many different tumor cell types; and is pro-angiogenic.



• arzoxifene hydrochloride

The hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist. In comparison to other selective estrogen receptor modulators (SERMs), arzoxifene exhibits greater bioavailability and higher anti-estrogenic potency in the breast than raloxifene; it exhibits reduced estrogenicity in the uterus compared with either tamoxifen or raloxifene. This agent may have beneficial effects on bone and the cardiovascular system.



• Asorbicap

(Other name for: ascorbic acid)



• asparaginase

An enzyme isolated from the bacterium Escherichia coli or the bacterium Erwinia carotovora. Asparagine is critical to protein synthesis in leukemic cells, which cannot synthesize this amino acid due to the absence of the enzyme asparagine synthase. Asparaginase hydrolyzes L-asparagine to L-aspartic acid and ammonia, thereby depleting leukemic cells of asparagine and blocking protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle. This agent also induces apoptosis in tumor cells. The E. carotovora-derived form of asparaginase is typically reserved for cases of asparaginase hypersensitivity.



• Aspergum

(Other name for: acetylsalicyclic acid)



• ATGAM

(Other name for: anti-thymocyte globulin)



• Athrombin-K

(Other name for: warfarin)



• atiprimod

An orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.



• ATN-161

A small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration.



• atomoxetine hydrochloride

The hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft; the effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.



• Atragen

(Other name for: tretinoin liposome)



• atrasentan hydrochloride

The orally available hydrochloride salt of pyrrolidine-3-carboxylic acid with potential antineoplastic activity. As a selective antagonist of the endothelin-A (ETA) receptor, atrasentan binds selectively to the ETA receptor, which may result in inhibition of endothelin-induced angiogenesis and tumor cell proliferation.



• atvogen

A synthetic derivative of inosinic acid with antiretroviral and immunomodulatory properties. Atvogen acts through a number of pathways to stimulate intracellular antiviral activity of the immune system: it stimulates interferon production; activates the oligoadenylate synthase-RNase L pathway; stimulates natural killer cell activity; and acts as a non-mitogenic stimulator of the immune system. This agent also inhibits replication of human immunodeficiency virus (HIV) in vitro.



• Augmentin

(Other name for: amoxicillin-clavulanate potassium)



• Aurora kinase inhibitor MK-0457

A synthetic, small-molecule Aurora kinase inhibitor with potential antitumor activity. Aurora kinase inhibitor MK-0457 binds to and inhibits Aurora kinases (AKs), thereby inducing apoptosis in tumor cells in which AKs are overexpressed. AKs, a family of serine-threonine kinases, are essential for mitotic progression, spindle formation, centrosome maturation, chromosomal segregation, and cytokinesis.



• Aurora kinase inhibitor MLN8054

An orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers.



• autologous dendritic cell/adenovirus HER-2 vaccine

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) transduced with a replication-deficient adenovirus vector encoding HER-2 with potential antineoplastic activity. Upon administration, autologous dendritic cell/adenovirus HER-2 vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against HER-2-positive tumor cells, which may result in tumor cell death and decreased tumor growth. HER-2, a tyrosine kinase receptor for epidermal growth factor (EGF) (also known as neu and ErbB2), is overexpressed by some breast, ovarian, and gastric cancers.



• autologous dendritic cell-adenovirus p53 vaccine

An autologous vaccine composed of dendritic cells (DC) that have been transduced with a p53 tumor suppressor gene-modified virus. When the autologous dendritic cell-adenovirus p53 vaccine is administered, the host cytotoxic T lymphocytes (CTL) are directed against p53-positive tumor cells, which may result in tumor cell death and decreased tumor growth.



• autologous dendritic cell-allogeneic melanoma tumor cell lysate vaccine

A cell-based vaccine composed of autologous dendritic cells (DCs) pulsed with lysates from heat-treated allogeneic melanoma tumor cells. Upon administration, this vaccine may stimulate anti-tumoral cytotoxic T-cell and antibody responses to melanoma cells bearing shared melanoma antigens such as MelanA/MART-1, gp100, MAGE3, resulting in tumor cell lysis.



• autologous dendritic cell-autologous tumor mRNA-human CD40L vaccine

A cancer vaccine consisting of autologous dendritic cells transfected with autologous tumor mRNA and the human CD40 ligand (CD40L) gene with immunostimulatory and antitumor activities. Vaccination with autologous dendritic cell-autologous tumor mRNA-human CD40L vaccine may elicit a cytotoxic T cell response against tumor cells from which the autologous tumor mRNA was derived. When expressed by dendritic cells, tumor antigens and the co-stimulatory molecule CD40L, which binds to CD40 receptors on antigen presenting cells (APC), facilitate both humoral and cellular immune responses against tumor cells.



• autologous EBV-transformed B lymphoblastoid-tumor fusion cell vaccine

A cell-based vaccine composed of autologous tumor cells fused with Epstein-Barr virus-transformed B-lymphoblastoid cells. Upon administration, this vaccine may stimulate a cytotoxic T cell response against tumor cells, resulting in tumor cell lysis.



• autologous Epstein-Barr virus-specific cytotoxic T lymphocytes

A preparation of lymphocytes harvested from a patient with an Epstein-Barr virus (EBV)-positive tumor. Ex vivo, the lymphocytes are activated against EBV-specific antigens and then returned to the patient, where they mount a specific immune response against EBV-positive tumor cells.



• autologous Epstein-Barr virus-transformed B-lymphoblastoid cell vaccine

A cell-based vaccine composed of autologous lymphoblastoid B cells activated against Epstein-Barr virus (EBV) in vitro with potential immunoprotective activity. Upon prophylactic administration, this vaccine may stimulate specific cytotoxic T-lymphocyte (CTL) and antibody responses against EBV-transformed B cells, thereby preventing an EBV-induced post-transplantation lymphoproliferative disorder.



• autologous immunoglobulin idiotype-KLH conjugate vaccine

A cancer vaccine composed of tumor-specific idiotype determinants derived from an individual's tumor cells which are conjugated to keyhole limpet hemocyanin, an immunostimulant carrier protein. When injected into the individual from whom the tumor cells were isolated, this vaccine may stimulate an antitumoral cytotoxic T-lymphocytic immune response.



• autologous tumor cell vaccine

A therapeutic agent produced by isolating tumor cells from an individual and processing these tumor cells into a vaccine formulation in vitro; the vaccine is then administered to the individual from whom the tumor cells were isolated. Typically combined with an adjuvant immunostimulant, an autologous cell vaccine may elicit a cytotoxic T-lymphocytic immune response to cell surface-expressed tumor-associated antigens (TAAs), resulting in tumor cell death.



• Avandia

(Other name for: rosiglitazone)



• Avastin

(Other name for: bevacizumab)



• Avelox

(Other name for: moxifloxacin hydrochloride)



• Avita

(Other name for: tretinoin)



• Avlosulfon

(Other name for: dapsone)



• AVN944

An orally available, synthetic small molecule with potential antineoplastic activity. AVN944 inhibits inosine monosphosphate dehydrogenase (IMPDH), an enzyme involved in the de novo synthesis of guanosine triphosphate (GTP), a purine molecule required for DNA and RNA synthesis. Inhibition of IMPDH deprives cancer cells of GTP, resulting in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 appears to have a selective effect on cancer cells in that deprivation of GTP in normal cells results in a temporary slowing of cell growth only. IMPDH is overexpressed in some cancer cells, particularly in hematological malignancies.



• Avodart

(Other name for: dutasteride)



• AVR118

A peptide-nucleic acid immunomodulator with proinflammatory, broad-spectrum antiviral, and potential antineoplastic activities. AVR118 stimulates the peripheral blood mononuclear cell (PBMC) production of the proinflammatory cytokines IFN-y, IL-1b, IL-6 and TNF-a. This agent may reduce HIV-1 p24 antigen; viral reverse transcriptase activity; syncitial cell formation; and viral mRNA in infected PBMCs and human CD4+ lymphocyte H9 cells, and may decrease viral loads and increase CD4+ and CD8+ T-cell counts in HIV patients. In vitro, AVR118 has been shown to induce the maturation of HL60 leukemic cells and to inhibit the invasive and metastatic properties of a highly malignant breast cancer cell line.



• azacitidine

A pyrimidine nucleoside analogue of cytidine with antineoplastic activity. Azacitidine is incorporated into DNA, where it reversibly inhibits DNA methyltransferase, thereby blocking DNA methylation. Hypomethylation of DNA by azacitidine may activate tumor suppressor genes silenced by hypermethylation, resulting in an antitumor effect. This agent is also incorporated into RNA, thereby disrupting normal RNA function and impairing tRNA cytosine-5-methyltransferase activity.



• AZD0530

An orally available 5-, 7-substituted anilinoquinazoline with anti-invasive and anti-tumor activities. AZD0530 is a dual-specific inhibitor of Src and Abl, protein tyrosine kinases that are overexpressed in chronic myeloid leukemia cells. This agent binds to and inhibits these tyrosine kinases and their effects on cell motility, cell migration, adhesion, invasion, proliferation, differentiation, and survival. Specifically, AZD0530 inhibits Src kinase-mediated osteoclast bone resorption.



• AZD2171

An indole ether quinazoline derivative with antineoplastic properties. Competing with adenosine triphosphate, AZD2171 binds to and inhibits all three vascular endothelial growth factor receptor (VEGF-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth.