lunes, 26 de junio de 2017

NCI Drug Dictionary - National Cancer Institute | A-2

NCI Drug Dictionary - National Cancer Institute



National Cancer Institute



Alkeran

(Other name for: melphalan)

ALK-FAK inhibitor CEP-37440

An orally available dual kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and focal adhesion kinase (FAK), with potential antineoplastic activity. Upon administration, ALK-FAK inhibitor CEP-37440 selectively binds to and inhibits ALK kinase and FAK kinase. The inhibition leads to disruption of ALK- and FAK-mediated signal transduction pathways and eventually inhibits tumor cell growth in ALK- and FAK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; its dysregulation and gene rearrangements are associated with a variety of tumors. The cytoplasmic tyrosine kinase FAK, a signal transducer for integrins, is upregulated and constitutively activated in various tumor types; it plays a key role in tumor cell migration, proliferation, survival, and tumor angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)

Allegra

(Other name for: fexofenadine hydrochloride)

AllerNaze

(Other name for: triamcinolone acetonide)

alloantigen-specific allogeneic type 1 regulatory T cells T-allo10

A preparation of allogeneic CD4+ cells that were ex vivo stimulated with alloantigens, which involves exposing the cells to host antigen-presenting cells (APCs), in the presence of the immunomodulatory cytokine interleukin-10 (IL-10), with potential to prevent graft-versus-host disease (GvHD). The stimulation of the CD4+ cells by exposure to alloantigens plus IL-10 induces the differentiation of alloantigen-specific type 1 T regulatory (TR1) cells, which are hyporesponsive to the alloantigens. Upon infusion of T-allo10 and prior to donor hematopoietic stem cell transplantation (HSCT), the alloantigen-specific type 1 regulatory T cells are tolerant to the alloantigens and suppress alloreactive immune responses by donor CD4+ and CD8+ T cells. This may ultimately prevent GvHD. IL-10 plays a key role in controlling inflammation, down-regulating immune responses, and inducing immunological tolerance. IL-10 induces both a long lasting antigen specific T-cell anergy and the differentiation of TR1 cells. Check for active clinical trials using this agent. (NCI Thesaurus)

allodepleted haploidentical T cells expressing inducible Caspase 9

Allodepleted haploidentical T-lymphocytes transduced with the Gal-V pseudotyped retrovirus vector encoding SFG.iCasp9-2A-deltaCD19, with potential immune reconstitution property. SFG.iCasp9-2A-deltaCD19 contains the suicide gene inducible caspase 9 (iCasp9) linked with a 2A-like cleavable peptide to the selectable marker, truncated human CD19 (deltaCD19). iCasp9 consists of a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V) linked to human caspase 9 using a short linker (SGGGS). Donor T cell therapy may help control transplant-related viral infections following allogeneic hematopoietic stem cell transplantation. However, even the addition of allodepleted donor T cells can lead to graft-versus-host disease (GVHD). In the event that GVHD begins to develop, the chemical homodimerizer AP1903 can be administered, which binds to the FKBP12-F36V domain activating caspase 9. This results in the death of T cells causing GVHD while sparing the virus reactive T-cells. Check for active clinical trials using this agent. (NCI Thesaurus)

allodepleted T cell immunotherapeutic ATIR101

A cell-based immunotherapeutic product containing T-lymphocyte-enriched leukocytes that are devoid of alloreactive T-lymphocytes, that can potentially be used to restore lymphocyte levels after stem cell transplantations and are derived from partially matched (haploidentical) family donors for blood cancer patients who do not have a matching stem cell donor available. Host alloreactive T-cells, which can cause graft-versus-host disease (GVHD), are eliminated from the donor lymphocytes ex vivo using photodynamic therapy. After allogeneic hematopoietic stem cell transplantation (HSCT), allodepleted T cell immunotherapeutic ATIR101 is administered. This maintains a T-cell-mediated immune response against tumor cells and the donor T-cells can prevent opportunistic infections. ATIR101 does not cause severe, acute GVHD. In addition, administration of ATIR101 eliminates the need for immunosuppressants. Check for active clinical trials using this agent. (NCI Thesaurus)

Allodepleted T-cell ImmunotheRapeutics

(Other name for: allodepleted T cell immunotherapeutic ATIR101)

AlloDerm

(Other name for: acelullar cadaveric dermal matrix)

allogeneic acute myeloid leukemia antigen-expressing dendritic cell vaccine

A cancer vaccine consisting of allogeneic, immortalized dendritic precursor cells derived from a patient with acute myelogenous leukemia (AML), with potential immunostimulatory and antineoplastic activities. Upon ex vivo stimulation and expansion of the precursor cells into mature, fully functional dendritic cells (DCs) and subsequent administration, the allogeneic AML antigen-expressing DC vaccine may elicit a potent cytotoxic T-cell (CTL) and antibody response against AML antigen-expressing cells, resulting in tumor cell death. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic adenovirus-specific cytotoxic T lymphocytes

A population of allogeneic cytotoxic T-lymphocytes (CTLs) specifically reactive to human adenovirus (Ad) with potential immunomodulating and anti-adenoviral activities. Upon immunoprophylactic adoptive cell therapy, infusion of allogeneic Ad-specific CTLs may help reconstitute Ad-specific CTL responses in patients at risk of developing Ad infections after allogeneic stem cell transplant or in Ad-infected immunocompromised hosts. These allogeneic Ad-specific CTLs are prepared by multiple rounds of stimulation with donor peripheral blood mononuclear cells and lymphoblastoid cell lines that have been transduced with Ad5f35, a recombinant adenoviral vector carrying no transgene. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic B7.1/HLA-A1 transfected tumor cell vaccine

An allogeneic whole cell vaccine, derived from irradiated allogenic tumor cells manipulated to express human B7.1 (CD80 antigen) and human leukocyte antigen (HLA) A1, with potential antitumor activity. Vaccination with allogeneic B7.1/HLA-A1 transfected tumor cell vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic CD19-specific CAR-modified CD8 positive central memory-derived virus-specific T cells

A preparation of allogeneic Epstein-Barr virus (EBV)- and human cytomegalovirus (CMV)-specific CD8+ central memory-derived T effector-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) anti-CD19/CD3 zeta chain fusion protein coupled to the intracellular signal domain of CD28 antigen, with potential immunostimulating, anti-viral and antineoplastic activities. Upon infusion, allogeneic CD19-specific CAR-modified CD8+ central memory-derived virus-specific T cells directs the T-lymphocytes to CD19-expressing tumor cells, stimulating a selective toxicity to tumor cells which may eventually result in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. The viral specific T-cells exert antiviral immunity. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic CD3- CD19- selected natural killer cells

Human leukocyte antigen (HLA)-haploidentical donor-derived natural killer (NK) cells that are activated with the cytokine interleukin-15 (IL-15), with immunomodulating and antineoplastic activities. Upon leukapheresis, the HLA-haploidentical donor peripheral blood mononuclear cells (PBMCs) are treated to remove T lymphocytes (CD3+) and B-lymphocytes (CD19+) cells. In turn, NK cells are expanded and activated with IL-15. Upon infusion of the allogeneic CD3- CD19- selected NK cells, these cells recognize and bind to tumor cells, and secrete perforins, granzymes, and cytokines, which results in cancer cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic CD4+ memory Th1-like T cells/microparticle-bound anti-CD3/anti-CD28

A preparation consisting of allogeneic, differentiated Th1-like T cells bound to T cell-stimulating monoclonal antibodies with potential antitumor activity. More specifically, allogeneic CD4+ memory Th1-like T cells/microparticle-bound anti-CD3/anti-CD28 are composed of a proprietary preparation of mismatched, allogeneic differentiated CD4+ memory Th1-like T cells bound to paramagnetic, epoxy-covered 4.5 micron microparticles with covalently bound anti-CD3/anti-CD28 monoclonal antibodies at a 2:1 bead:cell ratio. The CD4+ memory Th1-like T cells are derived from precursors found in the circulation of a normal donor. Stimulated by the microparticle-bound monoclonal antibodies, the infused T cells produce pro-inflammatory, anti-tumor cytokines such as like IFN-gamma, TNF-beta, and IL-2, disabling tumor immune avoidance mechanisms and stimulating the host immune system to both reject the infused T cells and kill tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic CMV/AdV-specific cytotoxic T lymphocytes

A population of allogeneic cytotoxic T lymphocytes (CTLs) specifically reactive to cytomegalovirus (CMV) and adenovirus (AdV) with potential antiviral activity. Allogeneic CMV/AdV-specific cytotoxic T lymphocytes are prepared by exposing donor-derived CTLs to a lethally irradiated Epstein-Barr virus-positive lymphoblastoid B cell line (EBV-LCL) that has been transduced with a clinical-grade adenoviral vector (Ad5f35CMVpp65) as a source of CMV and AdV antigens. Infusion of these CTLs into stem cell transplant recipients may prevent CMV and AdV viral disease. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic cytomegalovirus-specific cytotoxic T lymphocytes

A population of allogeneic cytotoxic T lymphocytes (CTLs) specifically reactive to the herpes virus cytomegalovirus (CMV) with potential immunomodulating and antiviral activities. Upon immunoprophylactic adoptive cell therapy infusion with allogeneic cytomegalovirus-specific cytotoxic T lymphocytes, these CTLs may help reconstitute CMV-specific CTL responses in CMV-infected immunocompromised hosts after allogeneic hematopoietic stem cell transplant, thereby potentially preventing the occurrence of CMV viral disease or reducing the amount of antiviral drug therapy. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic dendritic cell vaccine COMBIG-DC

A cancer vaccine consisting of allogeneic, immortalized dendritic cells (DCs) loaded with tumor specific antigens and activated, with potential immunostimulatory and antineoplastic activities. Upon intratumoral administration of the allogeneic dendritic cell vaccine COMBIG-DC, these activated DCs attract natural killer (NK) cells, induce an anti-inflammatory response leading to the induction of NK-cell-mediated tumor cell death. Upon release of tumor associated antigens (TAAs) from the lysed tumor cells, these antigens are taken up by antigen presenting cells which activate the immune system to elicit a potent cytotoxic T-cell (CTL) response against the TAAs, resulting in the death of TAAs-expressing tumor cells. Check for active clinical trials using this agent.

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

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

allogeneic glioblastoma stem-like cell line lysate-pulsed autologous dendritic cell vaccine

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with lysates from an allogeneic glioblastoma (GBM) stem-like cell line, with potential immunostimulatory and antineoplastic activities. Upon administration allogeneic glioblastoma stem-like cell line lysate-pulsed autologous dendritic cell vaccine exposes the immune system to GBM stem cell antigens, which may result in cytotoxic T lymphocyte (CTL) and antibody responses against GBM cells. This leads to GBM cell lysis. GBM stem-like cells contain a specific range of antigens that are essential for the neoplastic growth and survival of GBM cells. Check for active clinical trials using this agent. (NCI Thesaurus)

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

allogeneic GM-CSF-secreting lethally irradiated whole melanoma cell vaccine

An allogeneic cancer vaccine composed of lethally irradiated whole melanoma cancer cells that are genetically modified to secrete the immunostimulatory cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Upon intradermal injections, allogeneic GM-CSF-secreting lethally irradiated whole melanoma cell vaccine secretes GM-CSF. In turn, GM-CSF may stimulate the body's immune system against tumor cells by enhancing the activation of dendritic cells (DCs) and promoting antigen presentation to both B- and T-lymphocytes. In addition, GM-CSF promotes antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function. Check for active clinical trials using this agent.

allogeneic GM-CSF-secreting tumor vaccine PANC 10.05 pcDNA-1/GM-Neo

An allogeneic cancer vaccine composed of lethally irradiated, whole pancreatic cancer cells transfected with a plasmid carrying the gene for cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Allogeneic GM-CSF–secreting tumor vaccine PANC 10.05 pcDNA-1/GM-Neo secretes GM-CSF thereby activating dendritic cells, promoting antigen presentation to B- and T-cells, and promoting a cytotoxic T-lymphocyte (CTL) response. This may eventually kill tumor cells. The pancreatic tumor cells are derived from the PANC 10.05 tumor cell line. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic GM-CSF-secreting tumor vaccine PANC 6.03 pcDNA-1/GM-Neo

An allogeneic cancer vaccine composed of lethally irradiated, whole pancreatic cancer cells transfected with a plasmid carrying the gene for cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Allogeneic GM-CSF–secreting tumor vaccine PANC 6.03 pcDNA-1/GM-Neo secretes GM-CSF thereby activating dendritic cells, promoting antigen presentation to B- and T-cells, and promoting a cytotoxic T-lymphocyte (CTL) response. This may eventually kill tumor cells. The pancreatic tumor cells are derived from the PANC 6.03 tumor cell line. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic GM-CSF-transfected myeloma cell vaccine

An allogeneic tumor cell vaccine containing myeloma cancer cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene with potential antineoplastic activity. Upon vaccination, allogeneic GM-CSF-based myeloma cellular vaccine secretes GM-CSF, which may potentiate a tumor-specific cytotoxic T-lymphocyte (CTL) response against myeloma cancer cell-associated antigens. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic HLA A2/4-1BB ligand-expressing melanoma vaccine

An allogeneic melanoma cell vaccine derived from a cell line with high expression of melanoma associated antigens and genetically modified to express both HLA-A2 and 4-1BB ligand, with potential immunostimulating and antineoplastic activities. Upon administration, the 4-1BB ligand of the allogeneic HLA-A2/4-1BB ligand-expressing melanoma vaccine binds to 4-1BB on activated T-lymphocytes, which induces a strong immune response against HLA-A2 positive melanoma cells. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic IL13-zetakine/HyTK-expressing-glucocorticoid resistant cytotoxic T lymphocytes GRm13Z40-2

A preparation of glucocorticoid receptor (GR) negative, allogeneic cytotoxic T-lymphocytes (CTLs) expressing a membrane-tethered interleukin 13 (IL13) cytokine chimeric T-cell antigen receptor (zetakine), with potential antineoplastic activity. Upon transfection of donor T-lymphocytes with a plasmid encoding a fusion protein of the IL13-zetakine and the selection-suicide expression enzyme HyTK, these modified CTLs are expanded and introduced into a patient with glioblastoma multiforme (GBM). This agent specifically targets IL13 receptor alpha2, a glioma-restricted cell-surface epitope; the CTLs exert their cytolytic effect thereby killing IL13Ra2-expressing glioma cells. In addition, IL13-zetakine redirected CTLs induce production of certain cytokines. Furthermore, due to the fact that these CTLs are GR negative, they can be used concomitantly with glucocorticoid therapy. The IL13-zetakine consists of an extracellular IL-13 E13Y mutein-human IgG4 hinge-Fc chimera fused to human cytoplasmic CD3-zeta via the transmembrane domain of human CD4. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic irradiated melanoma cell vaccine CSF470

An allogeneic cancer vaccine composed of a mixture of lethally irradiated whole melanoma cancer cells obtained from four different melanoma cell lines, with potential immunostimulating and antineoplastic activities. Upon intradermal injections, allogeneic irradiated melanoma cell vaccine may stimulate the body's immune system to exert a cytotoxic T-lymphocyte response and antibody-dependent cellular cytotoxicity (ADCC) against the melanoma cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic large multivalent immunogen breast cancer vaccine

A cancer vaccine, containing human-specific large multivalent immunogens (LMIs) isolated from the membrane fraction of cells from a breast cancer cell line, with potential immunostimulatory and antineoplastic activities. Upon administration, allogeneic large multivalent immunogen breast cancer vaccine may stimulate a cytotoxic T lymphocyte (CTL) immune response against tumor cells that express the breast cancer cell-specific LMIs. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic large multivalent immunogen melanoma vaccine LP2307

A cancer vaccine, containing human-specific large multivalent immunogen (LMI) isolated from plasma membrane fractions of the melanoma cell lines MSM-M1 and MSM-M2, with potential immunostimulating and antineoplastic activities. Upon administration, allogeneic large multivalent immunogen melanoma vaccine LP2307 may stimulate a CD8+ cytotoxic T lymphocyte (CTL) response against melanoma tumor cells that express melanoma-specific LMI. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic LMP1-/LMP2- specific cytotoxic T-lymphocytes

A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to the Epstein-Barr virus (EBV) latent membrane proteins (LMP) 1 and 2, with potential antineoplastic activity. Peripheral blood mononuclear cells (PBMC) are collected from a donor and are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP1/2 to generate LMP1/2-specific CTL which are subsequently expanded. Administration of allogeneic LMP1-/LMP2- specific CTL to patients with LMP1/2-positive tumors may result in a specific CTL response against tumor cells expressing LMP1 and LMP2, resulting in cell lysis and inhibition of tumor cell proliferation. As tumor associated antigens (TAAs), LMP1 and LMP2 are expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic melanoma vaccine AGI-101H

A cancer vaccine derived from two gentically modified human melanoma cell lines with potential antineoplastic activity. Allogeneic melanoma vaccine AGI-101H consists of a 1:1 mixture of cells from two genetically modified human melanoma cell lines, designated as Mich1H6 and Mich2H6, that have been gamma-irradiated to render the cells non-proliferative. Upon administration, this vaccine may stimulate a cytotoxic immune response against melanoma tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic mesothelioma tumor lysate-pulsed autologous dendritic cell vaccine

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with a mixture of lysates from five allogeneic mesothelioma tumor cell lines, with potential immunostimulatory and antineoplastic activities. Upon leukapheresis, DCs are loaded with allogeneic mesothelioma tumor cell lysates. Upon re-administration of the allogeneic mesothelioma tumor lysate-pulsed autologous DC vaccine, the immune system is exposed to an undefined amount of mesothelioma-associated antigens, which stimulates the induction of a specific cytotoxic T-lymphocyte (CTL) response against mesothelioma tumor cells and leads to tumor cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic multipotent adult progenitor cells

A biologic product that consists of undifferentiated stem cells, obtained from adult bone marrow or other non-embryonic tissue sources, that are expanded in vitro and deposited in master cell banks for "off-the-shelf" use, with potential hematopoiesis-inducing and immunomodulating activities. Allogeneic multipotent adult progenitor cells (MAPCs) are non-immunogenic due to the lack of major histocompatibility (MHC) molecule expression, and so elicit no immune response upon administration. In vivo, bone marrow-derived adult stem cells are capable of maturing into a broad range of cell types and may help restore the immune system by producing multiple therapeutic molecules in response to inflammation and tissue damage. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic multivirus-specific cytotoxic T lymphocytes

A population of closely human leukocyte antigen (HLA)-matched, donor-derived cytotoxic T lymphocytes (CTLs) that are specifically reactive towards five viruses, Epstein-Barr virus (EBV), cytomegalovirus (CMV), adenovirus (AdV), human herpesvirus 6 (HHV6), and human polyomavirus type I (BKV), with potential antiviral activity. Infusion of the multivirus-specific CTLs into allogeneic hematopoietic stem cell transplant (HSCT) recipients provides virus-specific cellular immunity and causes specific anti-viral effects against active viral infections. The administered CTLs also prevent EBV, CMV, AdV, HHV6, and BKV reactivation and infection as well as inhibiting viral-associated diseases in immunocompromised patients. The allogeneic multivirus-specific CTLs may also provide cellular immunity towards the human polyomavirus type II (JC virus; JCV), which is highly homologous to BKV. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic natural killer cell line MG4101

A population of allogeneic, cytotoxic natural killer (NK) cells with potential antitumor activity. Allogeneic natural killer cell line MG4101 is derived from cells of a normal, healthy donor upon leukapheresis and activation. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic natural killer cell line NK-92

A proprietary, human cytotoxic cell line composed of allogeneic, activated, interleukin-2 (IL-2) dependent-natural killer cells derived from a 50-year old male patient with rapidly progressive non-Hodgkin's lymphoma, with potential antineoplastic activity. As NK-92 cells are devoid of killer inhibitory receptors (KIRs; also called killer cell immunoglobulin-like receptors), which are negative regulators of NK cell activity, cancer cells are unable to suppress the cancer cell killing ability of the NK-92 cells. Upon infusion of the allogeneic NK cell line NK-92, the NKs recognize and bind to tumor cells. This leads to the secretion and release of perforins, granzymes, cytokines and chemokines, which results in cancer cell lysis and apoptosis. In addition, NK-92 cells express high affinity Fc receptors, which bind to therapeutic antibodies; therefore, this agent can enhance antibody dependent cellular cytotoxicity (ADCC) of co-administered therapeutic antibodies. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic renal cell carcinoma vaccine MGN1601

A whole cell vaccine comprised of irradiated allogeneic renal cell carcinoma (RCC) with potential immunostimulating and antineoplastic activities. Allogeneic renal cell carcinoma vaccine MGN1601 contains two active ingredients: 1) genetically modified allogeneic RCC cells that are transiently transfected with four different MIDGE (Minimalistic Immunogenically Defined Gene Expression) vectors encoding IL-7, GM-CSF, CD80 and CD154 and 2) the synthetic DNA-based immunomodulator dSLIM-30L1, a TLR9 agonist. Vaccination results in expression of IL-7, GM-CSF, CD80 and CD154, which all contribute to the activation or enhancement of immune responses. Furthermore, administration of this RCC vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor growth. TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity. Check for active clinical trials using this agent. (NCI Thesaurus)

allogeneic T lymphocytes BPX-501

Allogeneic T lymphocytes with potential immune reconstitution activity. Donor T lymphocytes are transduced with a retroviral vector (BPZ-1001) encoding the inducible suicide gene caspase 9 (iCasp9) and linked to a drug binding domain. Donor T-cell therapy may help control transplant-related infections following allogeneic hematopoietic stem cell transplantation. However, the addition of donor T cells can lead to graft-versus-host disease (GVHD). In the event that GVHD begins to develop, the chemical homodimerizer AP1903 can be administered, which binds to the drug binding domain and induces caspase 9 expression. This activates apoptosis in the T cells causing GVHD. Check for active clinical trials using this agent. (NCI Thesaurus)

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

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

allosteric Bcr-Abl tyrosine kinase inhibitor ABL001

An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, ABL001 binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. The Bcr-Abl fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that contain the Philadelphia chromosome. Check for active clinical trials using this agent. (NCI Thesaurus)

almurtide

A synthetic muramyl dipeptide (MDP) H8analogue with potential immunostimulating and antineoplastic activity. As a derivative of the mycobacterial cell wall component MDP, almurtide activates both monocytes and macrophages. This results in the secretion of cytokines and induces the recruitment and activation of other immune cells, which may result in indirect tumoricidal or cytostatic effects. Check for active clinical trials using this agent. (NCI Thesaurus)

Alocrest

(Other name for: injectable liposomal vinorelbine)

aloe vera gel

A preparation of leaf pulp from the parenchymal tissue of the plant Aloe vera (Liliaceae). Aloe vera gel contains carbohydrate polymers, such as glucomannans or pectic acid, and various vitamins and essential amino acids, as well as other organic and inorganic compounds. This agent has been used internally or externally for sunburn, skin problems, insect bites, ulcers, arthritis, constipation, and as an immune system enhancer. Check for active clinical trials using this agent. (NCI Thesaurus)

aloe/anise/ascorbic acid/clove/glycerin/peppermint/spearmint/thyme-based herbal mouthwash

A herbal-based mouthrinse containing aloe, anise, ascorbic acid, clove, peppermint, spearmint and thyme, with potential anti-mucositic activity. When aloe/anise/ascorbic acid/clove/peppermint/spearmint/thyme-based mouthwash is used as a rinse, the ingredients in this agent may prevent or decrease inflammation and bacterial infections.This may prevent or inhibit radiotherapy- or chemotherapy-induced mucositis and decreases the pain associated with mucositis. Check for active clinical trials using this agent.

alogliptin

A selective, orally bioavailable, pyrimidinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. In addition to its effect on glucose levels, alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines. Check for active clinical trials using this agent. (NCI Thesaurus)

Aloxi

(Other name for: palonosetron hydrochloride)

alpelisib

An orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Alpelisib specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Check for active clinical trials using this agent. (NCI Thesaurus)

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

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

alpha-1,3-galactosyltransferase-expressing allogeneic lung tumor cell vaccine

An allogeneic lung cancer vaccine with potential immunostimulating and antineoplastic activities. Derived from allogeneic lung tumor cells, alpha-1,3-galactosyltransferase-expressing allogeneic lung tumor cell vaccine is engineered to express the murine alpha-1,3-galactosyltransferase (GalT), an enzyme humans lack. GalT catalyzes the expression of foreign alpha-1,3-galactosyl (alpha-gal) carbohydrate epitopes in glycoproteins and in glycolipids on the cell membranes of the allogeneic lung tumor cells present in the vaccine, essentially producing a "xenograft". The hyperacute rejection involves pre-existing human anti-alpha-gal antibodies that bind the foreign alpha-gal epitopes expressed by the vaccine tumor cell “xenograft”, resulting in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) towards endogenous lung tumor cells with unmodified carbohydrate epitopes. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-1,3-galactosyltransferase-expressing allogeneic renal cell carcinoma vaccine

An allogeneic renal cell cancer (RCC) vaccine composed of cell line-derived RCCs that are genetically engineered to express the murine alpha-1,3-galactosyltransferase (GalT), with potential immunostimulatory and antineoplastic activities. Not naturally occurring in humans, GalT catalyzes the expression of foreign alpha-1,3-galactosyl (alpha-gal) carbohydrate epitopes on the cell membranes of the allogeneic RCCs present in the vaccine. This induces a hyperacute rejection reaction involving pre-existing human anti-alpha-gal antibodies, which bind to the foreign alpha-gal epitopes expressed by the allogeneic RCCs. This results in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) towards endogenous RCCs with unmodified carbohydrate epitopes. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-1-proteinase inhibitor human

Human serum-derived alpha-1 proteinase inhibitor (alpha-1-antitrypsin or AAT) with immunomodulating and anti-inflammatory activity. Upon administration, AAT reduces the production of proinflammatory cytokines, such as tumor necrosis factor-alpha, interleukin (IL)-1 beta, IL-32, IL-6, and proteinase 3, and induces the production of anti-inflammatory cytokines, such as IL-10 and the IL-1 receptor antagonist IL-1RN. This agent also downregulates heparan sulfate and reduces the expansion of cytotoxic effector T cells, interferes with the maturation of dendritic cells and increases T regulatory cells. Altogether, AAT may attenuate acute graft-versus-host disease (GvHD) and may facilitate graft acceptance and survival. In addition, AAT enhances levels of cAMP and activation of cAMP-dependent protein kinase A. AAT, a 52kD protein and serine protease inhibitor, belongs to the serpin superfamily. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-fetoprotein peptide-pulsed autologous dendritic cell vaccine

A cell-based cancer vaccine comprising autologous dendritic cells pulsed with four alpha-fetoprotein (AFP) peptides, with potential immunostimulatory and antineoplastic activities. Upon administration, AFP peptide-pulsed autologous dendritic cell vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against AFP-expressing cancer cells, resulting in tumor cell lysis. AFP is overexpressed in a variety of cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-folate receptor-targeting thymidylate synthase inhibitor ONX-0801

An alpha-folate receptor (aFR)-mediated inhibitor of thymidylate synthase (TS), with potential antineoplastic activity. Upon intravenous infusion, ONX-0801 selectively targets and binds to aFR-expressing tumor cells. Upon uptake by aFR, this agent binds to and inhibits TS. This reduces thymine nucleotide synthesis, inhibits both DNA synthesis and cell division, and leads to tumor cell apoptosis. TS catalyzes the conversion of deoxyuridine monophosphate (dUMP) to deoxythymidine monophosphate (dTMP), an essential precursor for DNA synthesis, and plays a key role in cell growth and division. aFR, a cell-surface receptor glycoprotein, is overexpressed on various tumor cell types, but is minimally expressed by normal, healthy tissue. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-Gal glycosphingolipids

A preparation of glycosphingolipids (GSL), containing the disaccharide epitope galactose-alpha-1,3-galactose (alpha-Gal), with potential antineoplastic activity. Upon intratumoral injection, alpha-Gal glycosphingolipids may stimulate the immune system to mount complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against alpha-Gal GSL, which may result in tumor cell death; these responses involve natural anti-alpha-Gal immunoglobulins (Igs). As antibodies that occur naturally due to sensitization to alpha-Gal present on symbiotic bacterial flora, anti-alpha-Gal Igs are present in unusually high amounts in human sera. GSL represent a glycolipid subtype containing the amino alcohol sphingosine; tumor-associated GSL antigens contain various oligosaccharide residues. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-galactosylceramide-pulsed autologous dendritic cells

A cancer vaccine comprised of autologous dendritic cells (DCs) pulsed with the marine sponge glycolipid alpha-galactosylceramide (alpha-GalCer) with potential immunostimulatory and antimetastatic activities. Upon administration, alpha-galactosylceramide-pulsed autologous dendritic cells may result in the activation and proliferation of a subset of endogenous natural killer T ( NKT) cells, B cells, and CD4+ and CD8+ T cells, and the production of interferon-gamma and interleukin-12; these cascade events may result in a T helper-1 cell-biased proinflammatory antitumor immune response. The NKT cell ligand alpha-GalCer was originally isolated from the marine sponge Agelas mauritianusis. Check for active clinical trials using this agent. (NCI Thesaurus)

Alphagan

(Other name for: brimonidine tartrate)

alpha-lipoic acid

A naturally occurring micronutrient, synthesized in small amounts by plants and animals (including humans), with antioxidant and potential chemopreventive activities. Alpha-lipoic acid acts as a free radical scavenger and assists in repairing oxidative damage and regenerates endogenous antioxidants, including vitamins C and E and glutathione. This agent also promotes glutathione synthesis. In addition, alpha-lipoic acid exerts metal chelating capacities and functions as a cofactor in various mitochondrial enzyme complexes involved in the decarboxylation of alpha-keto acids. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-lipoic acid/vitamin/mineral supplement PolyMVA

A proprietary water- and lipid-soluble polymer-based nutritional supplement composed of a complex mixture of alpha-lipoic acid bound to palladium (palladium lipoic acid complex (PdLA)) and other minerals, vitamins and amino acids, including vitamins B1, B2 and B12, formylmethionine, acetyl cysteine, and trace amounts of molybdinum, rhodium, and ruthenium, with potential anti-oxidant and cytoprotective activities. Upon oral administration, the alpha-lipoic acid-palladium/vitamin/mineral supplement acts as a free radical scavenger, crosses the cell membrane and is able to transfer electrons from fatty acids to DNA via the electron transport chain in mitochondria, which protects against DNA damage. This could protect non-cancerous cells from the oxidative damage caused by radiation and chemotherapy. In addition, in the hypoxic conditions found within tumors, the excess electrons can generate free radicals within mitochondria and could induce both cytochrome c release and apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside

A radioconjugate and sodium-dependent glucose transporter (SGLT)-specific tracer that is composed of a glucose analog labeled with the positron-emitting radioactive isotope fluorine F18, and can be used for tumor cell imaging upon positron emission tomography (PET). Upon administration, alpha-methyl-4-deoxy-4-[(18)F]fluoro-D-glucopyranoside (Me4FDG) is specifically taken up by SGLT-expressing tumor cells. The fluorine F 18 moiety can be visualized upon PET imaging and this agent can be used both as a tracer for sugar uptake by and for imaging and staging of certain tumor cell types. Glucose is a major metabolic substrate required for cancer cell survival and growth and is taken up by cancer cells at a much higher rate compared to normal cells. SGLTs, especially SGLT type 2 (SGLT2), are overexpressed on certain tumor cell types and play key roles in glucose transport in these cells. Me4FDG is not transported by glucose uniporter proteins (GLUTs). In contrast, Me4FDG is not transported by glucose transporters (GLUTs). Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-tocopherol

A naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties. Considered essential for the stabilization of biological membranes (especially those with high amounts of polyunsaturated fatty acids), d-alpha-Tocopherol is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, resulting in a decrease in prostaglandin production. Vitamin E also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-tocopheryloxyacetic acid

An orally bioavailable vitamin E derivative with potential antineoplastic and immunostimulating activities. Upon administration, alpha-tocopheryloxyacetic acid (alpha-TEA) induces tumor autophagy; the autophagosomes formed, which carry tumor associated antigens (TAAs), allow for increased cross-presentation of TAAs by professional antigen-presenting cells (APCs). This activates a T-cell-mediated T-helper type 1 (TH1) response, generates a cytotoxic T-lymphocyte (CTL) response against cancer cells, and reduces the frequency of regulatory T-cell (Treg) differentiation. In addition, alpha-TEA modulates the release of various cytokines and chemokines and induces tumor cell apoptosis. Altogether, this results in decreased tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

alpha-type-1 polarized dendritic cells

A population of mature polarized dendritic cells with potent immunostimulating activity. Treating bone marrowed-derived dendritic cells (DCs) with interferon-alpha (IFN-a), polyinosinic:polycytidylic acid (poly I:C) and bacterial CpG-DNA produces mature but not exhausted alpha type-1 polarized DCs (alphaDC1) that are capable of: 1) high responsiveness to other lymphoid chemokines, and 2) producing high levels of interleukin-12p70 (IL-12p70), characteristics found in human type-1 polarized dendritic cells. When pulsed with specific tumor associated antigens (TAAs), alphaDC1 may induce a potent cytotoxic T lymphocyte (CTL) response against TAA-expressing tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

alprazolam

A triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant activities. Alprazolam binds to a specific site distinct from the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) binding site on the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic and hypothalamic regions of the central nervous system (CNS). This binding causes an allosteric modification of the receptor and enhances the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events. This leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential and leads to a decrease in neuronal excitability. Check for active clinical trials using this agent. (NCI Thesaurus)

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

Altace

(Other name for: ramipril)

alteplase

A recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA). tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme. Upon administration, alteplase increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism. Check for active clinical trials using this agent. (NCI Thesaurus)

Althose

(Other name for: methadone hydrochloride)

altiratinib

An orally bioavailable inhibitor of c-Met/hepatocyte growth factor receptor (HGFR), vascular endothelial growth factor receptor type 2 (VEGFR2), Tie2 receptor tyrosine kinase (TIE2), and tropomyosin receptor kinase (Trk), with potential antiangiogenic and antineoplastic activities. Upon administration, altiratinib selectively binds to c-Met, VEGFR2, Tie2 and Trk tyrosine kinases, which may lead to the inhibition of endothelial cell migration, proliferation and survival. This also results in both an inhibition of tumor cell proliferation and increased tumor cell death in c-Met/VEGFR2/Tie2/Trk-expressing cells. These receptor tyrosine kinases (RTKs), frequently overexpressed or mutated by a variety of tumor cell types, play crucial roles in the regulation of angiogenesis, tumor cell growth and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

altretamine

A synthetic cytotoxic s-triazine derivative similar in structure to alkylating agent triethylenemelamin with antineoplastic activity. Although the precise mechanism by which altretamine exerts its cytotoxic effect is unknown, N-demethylation of altretamine may produce reactive intermediates which covalently bind to DNA, resulting in DNA damage. Check for active clinical trials using this agent. (NCI Thesaurus)

alum adjuvant

An aluminum compound with immune adjuvant activity. This agent adsorbs and preciptates protein antigens in solution; the resulting precipitate improves vaccine immunogenicity by faclitating the slow release of antigen from the vaccine depot formed at the site of inoculation. Check for active clinical trials using this agent. (NCI Thesaurus)

Alunbrig

(Other name for: brigatinib)

ALVAC(2) melanoma multi-antigen therapeutic vaccine

A therapeutic cancer vaccine, based on a replication-defective recombinant canarypox virus (ALVAC) encoding multiple melanoma antigens, with potential immunostimulatory and antineoplastic activities. Vaccination with ALVAC(2) melanoma multi-antigen therapeutic vaccine may stimulate the host immune system to mount an immune response against antigen-expressing melanoma cells, resulting in inhibition of tumor growth and/or metastasis. Check for active clinical trials using this agent. (NCI Thesaurus)

ALVAC(2)-NY-ESO-1 (M)/TRICOM vaccine

A cancer vaccine consisting of a replication-defective recombinant canarypox virus [ALVAC(2)] encoding the cancer-testis antigen NY-ESO and the TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3; also called TRICOM), with potential immunostimulatory and antineoplastic activities. Upon administration, ALVAC(2)/NY-ESO (M)/TRICOM vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against NY-ESO-expressing cancer cells, which may result in the inhibition of tumor cell proliferation. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cells, including bladder, breast, hepatocellular, melanoma, and prostate tumor cells. TRICOM may enhance antigen presentation and activate cytotoxic T-cells. In addition, ALVAC(2) encodes the vaccinia virus (vv) E3L ad K3L genes, which may potentiate the translation of the NY-ESO and TRICOM genes. Check for active clinical trials using this agent. (NCI Thesaurus)

ALVAC-CEA vaccine

A cancer vaccine consisting of ALVAC, a highly attenuated poxvirus strain derived from the canarypox virus, encoding for the tumor associated antigen (TAA) carcinoembryonic antigen (CEA), with potential antineoplastic activity. Upon administration, ALVAC-CEA vaccine expresses CEA and may stimulate a host immune response against tumor cells expressing CEA. This may result in the inhibition of tumor growth and/or metastasis. CEA is overexpressed in a variety of tumor cell types. Check for active clinical trials using this agent.

ALVAC-ESO-1 vaccine

A cancer vaccine consisting of a replication-defective recombinant canarypox virus (ALVAC) encoding the cancer-testis antigen NY-ESO-1, with potential immunostimulatory and antineoplastic activities. Upon administration, ALVAC-ESO-1 vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against NY-ESO-1-expressing cancer cells, which may result in the inhibition of tumor cell proliferation. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

ALVAC-hB7.1

A vaccine comprise of a canarypox viral vector that carries the gene for human B7.1 (CD80 antigen) with potential use as an autologous therapeutic cancer vaccine. Tumor cells harvested from a patient are infected with ALVAC-hB7 1, thereby producing an autologous cell line that exhibits increased expression of HLA class I and class II, CD54 (ICAM), and CD80. Increased expression of these proteins by this autologous cell line may activate an antitumor T-cell response when the modified cells are administered to the patient. Check for active clinical trials using this agent. (NCI Thesaurus)

ALVAC-MART-1 vaccine

A cancer vaccine containing a replication-defective recombinant canarypox virus (ALVAC), encoding an epitope of MART-1 (melanoma antigen recognized by T-cells), with potential immunostimulatory and antineoplastic activities. Upon administration, the MART-1 epitope is expressed by the ALVAC vector in ALVAC-MART-1 vaccine; a host cytotoxic T lymphocyte (CTL) response against MART-1-expressing tumor cells may follow, resulting in tumor cell lysis and decreased tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

alvelestat

An orally bioavailable, selective and reversible inhibitor of human neutrophil elastase (NE), with potential anti-inflammatory activity. Upon administration, alvelestat binds to and inhibits the activity of human NE. This inhibits NE-mediated inflammatory responses, which may prevent lung inflammation and injury, and may improve lung function associated with NE-induced respiratory diseases. NE, a serine protease released by neutrophils during inflammation, is upregulated in a number of respiratory diseases. Check for active clinical trials using this agent. (NCI Thesaurus)

alvespimycin hydrochloride

The hydrochloride salt of alvespimycin, an analogue of the antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction. Check for active clinical trials using this agent. (NCI Thesaurus)

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

alvocidib

A synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity. Check for active clinical trials using this agent. (NCI Thesaurus)

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

Amaryl

(Other name for: glimepiride)

amatuximab

A humanized IgG1 monoclonal antibody directed against human mesothelin with potential antineoplastic activity. Amatuximab binds to mesothelin, triggering an antibody dependent cellular cytotoxicity (ADCC)-mediated host immune response against mesothelin-expressing tumor cells, which may result in tumor cell lysis. Mesothelin, a 40kDa cell surface glycoprotein, is overexpressed in several human tumors, including mesothelioma and ovarian and pancreatic adenocarcinomas. Check for active clinical trials using this agent. (NCI Thesaurus)

Ambien

(Other name for: zolpidem tartrate)

AmBisome

(Other name for: liposomal amphotericin B)

Ambochlorin

(Other name for: chlorambucil)

Amboclorin

(Other name for: chlorambucil)

Amdray

(Other name for: valspodar)

American ginseng

The aromatic root of the perennial herb Panax quinquefolius, native to eastern North America. American ginseng, used in Chinese traditional medicine and available as a nutritional supplement, is classified as an adaptogenic herb with multiple effects, many of which are regulatory in nature. It contains a complex mixture of saponin glycosides, also known as ginsenosides or panaxosides. Although the mechanism of action is unclear, this agent is reported to enhance the immune system and reduce fatigue. Check for active clinical trials using this agent. (NCI Thesaurus)

Amevive

(Other name for: alefacept)

Amfebutamone

(Other name for: bupropion hydrochloride)

Amicar

(Other name for: aminocaproic acid)

amifampridine

An organic compound derived from pyridine with potassium channel inhibition activity. Amifampridine inhibits potassium channel efflux, increasing the duration of the action potential, which results in an increase in the duration of calcium channel opening and enhanced acetylcholine (ACh) release. Increased ACh availability at the motor end plate allows muscles to contract. Check for active clinical trials using this agent. (NCI Thesaurus)

amifostine

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

amikacin inhalation solution

A solution for inhalation containing the aminoglycoside antibiotic amikacin, with anti-bacterial activity. Upon aerosolized administration using the Pulmonary Drug Delivery System (PDDS), amikacin irreversibly binds to the 30S ribosomal subunit of susceptible organisms, thereby interfering with the activity of the translation initiation complex, which leads to both the misreading of mRNA and the production of non-functional or toxic peptides, and prevents normal protein synthesis. This kills susceptible bacteria. Check for active clinical trials using this agent. (NCI Thesaurus)

amino acid injection

A concentrated dietary supplement for injection containing the essential amino acids leucine, isoleucine, lysine, valine, phenylalanine, histidine, threonine, methionine and tryptophan as well as the non-essential amino acids alanine, arginine, glycine, proline, serine and tyrosine, with potential anabolic and anti-catabolic activities. Upon dilution and intravenous infusion of the amino acid nutritional supplement, the amino acids serve as protein building blocks, promote protein synthesis in muscle cells and prevent protein breakdown. Check for active clinical trials using this agent. (NCI Thesaurus)

amino acid/electrolyte mixture-based dietary supplement

A nutritional supplement containing a proprietary mix of amino acids and electrolytes, with potential rehydrating and gastrointestinal (GI) supportive activities. Upon oral administration of the amino acid-electrolyte dietary supplement, the electrolytes are transported by amino acid-coupled transporters across the intestinal epithelial barriers. This helps rehydrate the intestinal epithelial cells, helps restore normal bowel function, prevents fluid loss and improves symptoms of diarrhea. In addition, the supplement helps restore the size and functioning of the damaged villi and facilitates the restoration of the intestinal cells, thereby helping to restore and increase nutrient absorption, restoring normal bowel function and supporting healthy immune function. Check for active clinical trials using this agent. (NCI Thesaurus)

aminobenzoate potassium

The potassium salt form of aminobenzoate, with anti-inflammatory and antifibrotic activities. Aminobenzoate potassium increases oxygen uptake at the tissue level and may enhance monoamine oxidase (MAO) activity, which requires oxygen as a substrate. Enhanced MAO activity maybe accountable for the prevention or regression of fibrosis, which may occur due to too much serotonin or too little MAO activity. Check for active clinical trials using this agent. (NCI Thesaurus)

aminocamptothecin

A water-insoluble camptothecin derivative. Aminocamptothecin binds to the nuclear enzyme topoisomerase I, thereby inhibiting repair of single-strand DNA breakages. Because the terminal lactone ring of aminocamptothecin required for the agent's antitumor activity spontaneously opens under physiological conditions to an inactive carboxy form, the drug must be administered over an extended period of time to achieve effective cytotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)

aminocaproic acid

A synthetic lysine derivative with antifibrinolytic activity. Aminocaproic acid competitively inhibits activation of plasminogen, thereby reducing conversion of plasminogen to plasmin (fibrinolysin), an enzyme that degrades fibrin clots as well as fibrinogen and other plasma proteins including the procoagulant factors V and VIII. Aminocaproic acid competitively reduces the conversion of plasminogen to plasmin by plasminogen activators. It directly inhibits proteolytic activity of plasmin, but higher doses are required than are needed to reduce plasmin formation. Aminocaproic acid is used in the treatment of hemorrhage and prophylactically against hemorrhage, including hyperfibrinolysis-induced hemorrhage and postsurgical hemorrhage. Check for active clinical trials using this agent. (NCI Thesaurus)

aminolevulinic acid hydrochloride

A topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid hydrochloride (ALA HCl) 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. Check for active clinical trials using this agent. (NCI Thesaurus)

aminophylline

A methylxanthine and derivative of theophylline. Aminophylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Aminophylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart. Check for active clinical trials using this agent. (NCI Thesaurus)

aminopterin

A synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analogue, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synthesis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. Check for active clinical trials using this agent. (NCI Thesaurus)

aminothiadiazole

A synthetic derivative of nicotinamide adenine dinucleotide (NAD). Aminothiadiazole competitively inhibits inosine 5-monophosphate dehydrogenase, thereby disrupting the regulation of cell proliferation and differentiation in a number of cells. This agent is also a selective human adenosine A3 receptor antagonist. Check for active clinical trials using this agent. (NCI Thesaurus)

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

Amitiza

(Other name for: lubiprostone)

amitriptyline hydrochloride

The hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities. Amitriptyline inhibits the re-uptake of norepinephrine and serotonin by the presynaptic neuronal membrane in the central nervous system (CNS), thereby increasing the synaptic concentration of norepinephrine and serotonin. Due to constant stimulation to these receptors, amitriptyline may produce a downregulation of adrenergic and serotonin receptors, which may contribute to the antidepressant activity. In the CNS the antinociceptive activity of this agent may involve high affinity binding to and inhibition of N-methyl-D-aspartate (NMDA) receptors and/or the enhancement of the action of serotonin at the spinal terminals of an opioid-mediated intrinsic analgesia system. Check for active clinical trials using this agent. (NCI Thesaurus)

AML mRNA plus lysate loaded autologous dendritic cell vaccine

A cancer vaccine consisting of autologous dendritic cells loaded with separate preparations of acute myelogenous leukemia (AML) cell lysate and AML-specific messenger RNA (mRNA) with potential immunostimulatory and antineoplastic activities. Upon administration, AML mRNA plus lysate loaded autologous dendritic cell vaccine may elicit a potent cytotoxic T-cell (CTL) response against AML cells, resulting in tumor cell death. Autologous dendritic cells doubly-loaded with AML cell lysate and AML-specific mRNA may elicit superior primary, recall, and effector lytic immune responses compared to autologous dendritic cells loaded with tumor lysate or tumor mRNA alone. Check for active clinical trials using this agent. (NCI Thesaurus)

Ammoidin

(Other name for: methoxsalen)

ammonia N-13

A radiopharmaceutical composed of ammonia labeled with the radioisotope nitrogen N 13 that can be used, during positron emission tomography (PET), as a blood flow imaging agent and potentially as a tumor imaging agent. Upon intravenous administration, ammonia N 13 distributes to various organs in the body, such as the myocardium, liver, kidneys and brain. This agent is taken up by cells and is retained following conversion to glutamine N 13 by glutamine synthetase (GS). Upon PET, organ perfusion and the presence of cancer cells can be assessed. GS, an enzyme that catalyzes the synthesis of glutamine from glutamate and ammonia, is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

ammonium trichlorotellurate

A synthetic non-toxic tellurium derivative, structurally similar to cisplatin, with immuno-modulating, antiviral, and hair growth-promoting activities. Ammonium trichlorotellurate may inhibit the inflammatory cytokine interleukin-10 (IL-10) and may induce hematopoietic cells to express interleukin-2 (IL-2), IL-2 receptors, granulocyte-macrophage colony-stimulating factor (GM-CSF), IL-3, tumor necrosis factor (TNF) and interferons (INFs). This agent is also a potent inducer of IL-1 and IL-6. Accordingly, ammonium trichlorotellurate may protect against chemotherapy-induced myelosuppression. In addition, this agent exhibits hair growth-promoting activity by inducing anagen production and inhibiting catagen production, resulting in the promotion of follicular keratinocyte proliferation and interference with follicular keratinocyte terminal differentiation, respectively. Accordingly, ammonium trichlorotellurate may protect against chemotherapy-induced alopecia. Check for active clinical trials using this agent. (NCI Thesaurus)

Amnesteem

(Other name for: isotretinoin)

AmnioFix

(Other name for: dehydrated human amnion/chorion membrane)

amnion-derived cellular cytokine solution

A topical cellular cytokine solution containing a distinct combination of growth factors and cytokines secreted by and released from amnion-derived multipotent progenitor (AMP) cells, with potential immunomodulating and skin healing activities. The amnion-derived cellular cytokine solution (ACCS) contains near physiological levels of transforming growth factor beta, tissue inhibitor of metalloproteinase-1 (TIMP-1) and TIMP-2, as well as the angiogenesis factors platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF) and angiogenin that are normally found in healing wounds. Upon spraying the solution onto affected areas, the cytokines and growth factors in ACCS appear to increase the migration, proliferation and differentiation of both keratinocytes and fibroblasts; enhance the migration and phagocytosis of macrophages in wounds; and increase epithelialization. Together these processes may accelerate skin healing and tissue repair. Also, ACCS may be beneficial in the treatment of radiation burns of the skin. Check for active clinical trials using this agent. (NCI Thesaurus)

Amoban

(Other name for: zopiclone)

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

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

amoxicillin

A broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Amoxicillin binds to and inactivates penicillin-binding protein (PBP) 1A located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)

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

Amoxil

(Other name for: amoxicillin)

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

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

Ampligen

(Other name for: rintatolimod)

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

Amsa P-D

(Other name for: amsacrine)

amsacrine

An aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)

amsilarotene

A retinobenzoic acid with potential antineoplastic activity. Amsilarotene inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression. Check for active clinical trials using this agent. (NCI Thesaurus)

amuvatinib

An orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Amuvatinib binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, amuvatinib inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors. This agent also suppresses the induction of DNA repair protein Rad51, thereby potentiating the activities of DNA damage-inducing agents. Mutant forms of c-Kit are often associated with tumor chemoresistance. Check for active clinical trials using this agent. (NCI Thesaurus)

anagrelide hydrochloride

The hydrochloride salt of a synthetic quinazoline derivative, anagrelide hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. Check for active clinical trials using this agent. (NCI Thesaurus)

anagrelide prolonged-release formulation

A prolonged-release tablet formulation containing the quinazoline anagrelide, with antiplatelet activity. Although the exact mechanism of action through which anagrelide exerts its effect has yet to be fully elucidated, this agent inhibits the maturation of megakaryocytes into platelets, which reduces platelet production. Anagrelide also inhibits cyclic AMP phosphodiesterase III (PDEIII), which prevents PDEIII-mediated platelet aggregation. This may prevent essential thrombocythemia and thrombosis. Check for active clinical trials using this agent. (NCI Thesaurus)

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

anamorelin hydrochloride

The orally bioavailable hydrochloride salt of a synthetic, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite. Check for active clinical trials using this agent. (NCI Thesaurus)

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

anaxirone

A synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis. This agent has been shown to exhibit a broad spectrum of antineoplastic activity against experimental tumors, including those resistant to other alkylating agents. Check for active clinical trials using this agent. (NCI Thesaurus)

Ancef

(Other name for: cefazolin sodium)

Ancestim

(Other name for: recombinant human stem cell factor)

ancitabine hydrochloride

The hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine. Check for active clinical trials using this agent. (NCI Thesaurus)

Ancobon

(Other name for: flucytosine)

AndroGel

(Other name for: testosterone gel)

androgen antagonist APC-100

An orally available, vitamin E derivative and androgen receptor (AR) antagonist with potential anti-oxidant, chemopreventative and antineoplastic activity. APC-100 binds to ARs in target tissues thereby inhibiting androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. By inhibiting the formation of the complex between androgen activated AR- and the AP1 transcription factor JunD, the expression of androgen-responsive genes is blocked. One such gene is spermidine/spermine N1-acetyl transferase gene (SSAT) which is responsible for the breakdown of polyamines, which are produced in high levels by prostatic epithelial cells, into reactive oxygen species (ROS) that cause cellular damage. APC-100 may ultimately lead to an inhibition of growth in both AR-dependent and AR-independent prostate tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

androgen receptor antagonist SHR3680

An orally bioavailable androgen receptor (AR) antagonist with potential antineoplastic activity. Upon administration, SHR3680 competitively binds to AR in target tissues, which both prevents androgen-induced receptor activation and facilitates the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes, inhibits the expression of genes that regulate prostate cancer cell proliferation, and may lead to an inhibition of cell growth of AR-expressing tumor cells. ARs are overexpressed in prostate cancer and play a key role in prostate cancer cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

androgen receptor antagonist TRC253

An orally bioavailable androgen receptor (AR) antagonist, with potential antineoplastic activity. Upon oral administration, AR antagonist TRC253 specifically binds to both wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus. This prevents binding to and transcription of AR-responsive genes, inhibits the expression of genes that regulate prostate cancer cell proliferation, and may lead to an inhibition of growth of tumor cells in which AR is overexpressed and/or mutated. AR is often overexpressed and/or mutated in prostate cancers and plays a key role in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trialsusing this agent.

androgen receptor antisense oligonucleotide AZD5312

An antisense oligonucleotide targeting the androgen receptor (AR) mRNA, with potential antineoplastic activity. Upon intravenous administration, AZD5312 hybridizes with AR mRNA, which blocks translation of the AR protein. This both inhibits AR-induced tumor cell growth and promotes apoptosis in AR-overexpressing tumor cells. AR is overexpressed in certain breast and prostate cancers and is involved in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

androgen receptor antisense oligonucleotide EZN-4176

A locked nucleic acid (LNA)-based antisense oligonucleotide targeting the androgen receptor (AR) mRNA, with potential antineoplastic activity. Upon administration, EZN-4176 is hybridized and releases the complementary sequences of AR mRNA, thereby blocking translation of the AR protein and inhibiting AR-induced tumor cell growth and promoting tumor cell apoptosis in AR-overexpressing tumor cells. AR is overexpressed in certain breast and prostate cancers and is involved in tumor cell proliferation and survival. LNAs contain a methylene bridge linking 2'-oxygen and 4'-carbon of ribose sugar rings, thereby increasing their thermal stability and decreasing degradation. Check for active clinical trialsusing this agent.

androgen receptor inhibitor EPI-506

An orally bioavailable, small molecule inhibitor of the N-terminal domain (NTD) of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR inhibitor EPI-506 specifically binds to the NTD of AR, thereby inhibiting both AR activation and the AR-mediated signaling pathway. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

androgen receptor ligand-binding domain-encoding plasmid DNA vaccine MVI-118

A cancer vaccine containing pTVG4 plasmid DNA encoding the human androgen receptor (AR) ligand-binding domain (LBD) (pTVG-AR), with potential immunostimulating and antineoplastic activities. Upon intradermal administration of AR LBD-encoding plasmid DNA vaccine MVI-118, the plasmid DNA vaccine expresses AR LBD and may stimulate the host immune system to generate a cytotoxic T-lymphocyte (CTL) response against AR LBD-expressing prostate cancer cells. This reduces proliferation of AR-expressing tumor cells. AR, a tumor-associated antigen (TAA) overexpressed in prostate cancer cells, plays a key role in the development and progression of prostate cancer; its expression is correlated with poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)

Android-F

(Other name for: fluoxymesterone)

androstane steroid HE3235

An orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agent inhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2. Check for active clinical trials using this agent. (NCI Thesaurus)

anetumab ravtansine

A fully human IgG1 monoclonal antibody directed against the cell surface glycoprotein mesothelin and conjugated to the maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody moiety of anetumab ravtansine targets and binds to the tumor associated antigen mesothelin; upon internalization, the DM4 moiety binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of mesothelin-expressing tumor cells. Mesothelin is overexpressed on all mesotheliomas as well as many ovarian and pancreatic cancers while minimally expressed on normal tissue. Check for active clinical trials using this agent. (NCI Thesaurus)

Aneustat

(Other name for: multifunctional/multitargeted anticancer agent OMN54)

ANF-Rho

(Other name for: pegfilgrastim anti-neutropenic factor)

Ang2/VEGF-binding peptides-antibody fusion protein CVX-241

A fusion protein containing angiopoietin-2 (Ang2) and vascular endothelial growth factor (VEGF) derived peptides covalently attached, via a proprietary diketone linker, to a proprietary humanized catalytic aldolase monoclonal antibody, with potential antiangiogenic and antineoplastic activities. The Ang2/VEGF peptide moieties of Ang2/VEGF-binding peptides-antibody fusion protein CVX-241 bind to Ang2 and VEGF receptors, which may inhibit tumor angiogenesis and tumor cell proliferation. The proprietary humanized catalytic IgG1 monoclonal aldolase antibody contains reactive lysine residues in its binding sites, which react covalently with compounds having a diketone function; the Ang2 and VEGFR peptide moieties are then covalently attached to the diketone linkers via a proprietary spacer. Both VEGF and Ang2 are upregulated in a variety of cancer cell types and play a crucial role in angiogenesis. This agent possesses an enhanced half-life compared to the naked peptides. Check for active clinical trials using this agent. (NCI Thesaurus)

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

Angiocal

(Other name for: anti-VEGF anticalin PRS-050-PEG40)

Angiocept

(Other name for: pegdinetanib)

angiogenesis inhibitor GT-111

An adenovirus encoding an endothelial cell-specific, murine pre-proendothelin-1 (PPE-1) promoter and a Fas-based chimeric death receptor with potential anti-angiogenic activity. Endothelial cell-specific transcriptional control of the adenoviral vector is achieved by the use of a modified murine PPE-1 promoter that is specifically activated in PPE-1-expressing angiogenic endothelial cells residing in the tumor microvasculature. Subsequently, the Fas-c (Fas-chimeric) death receptor, containing Fas and tumor necrosis factor (TNF) receptor 1 (TNFR1) moieties, is expressed in angiogenic endothelial cells; endothelial cell-specific Fas-mediated apoptosis is initiated by the binding of TNF-alpha, abundant in the tumor microenvironment, to the TNFR1 moiety of the expressed Fas-c death receptor. Check for active clinical trials using this agent. (NCI Thesaurus)

angiogenesis inhibitor JI-101

An orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101 binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so, cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. The receptor tyrosine kinases VEGFR2, PDGFRb and EphB4 may be overexpressed in a number of different cancer cell types and may play crucial roles in tumor angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)

angiogenesis/heparanase inhibitor PG545

A synthetic heparan sulfate mimetic with potential anti-angiogenic and antineoplastic activity. PG545 inhibits the cleavage of heparan sulfate from cell surface proteoglycan by heparanase and thus inhibits the neovascularization induced by interaction between heparan sulfate and other extracellular matrix proteins. In this manner, this agent may have the potential to slow the progression of growth of solid tumors. Check for active clinical trials using this agent. (NCI Thesaurus)

angiostatin

Encoded by human PLG Gene (Plasminogen Family) and expressed in the kidney, angiostatin is an angiogenesis inhibitor present in plasma and other extracellular fluids that blocks neovascularization and mediates suppression of metastases. Containing at least three kringles, angiostatin is a 38-kD internal (serine protease) proteolytic fragment of plasminogen. Check for active clinical trials using this agent. (NCI Thesaurus)

Angiozyme

(Other name for: anti-FLT-1 ribozyme)

anguidine

A trichothecene mycotoxin and potent teratogen. Anguidine inhibits initiation of protein synthesis, resulting in the death of rapidly proliferating cells. Anguidine also has been shown to both potentiate and protect against the cytotoxic effects of other drugs. Check for active clinical trials using this agent. (NCI Thesaurus)

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

aniline mustard

An alkylating mustard with antineoplastic activity. Aniline mustard forms covalent linkages with nucleophilic centers, resulting in depurination, base miscoding and strand scission, and crosslinking of DNA strands, all of which contribute to its cytotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)

anlotinib hydrochloride

The hydrochloride salt form of anlotinib, a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth. Check for active clinical trials using this agent. (NCI Thesaurus)

Annonaceous acetogenins

A family of naturally occurring polyketides that consist of C32 or C34 long chain fatty acids and combined with a propan-2-ol unit at C-2 to form a gamma-lactone, which are isolated from various species of the plant family Annonaceae, with potential antineoplastic and antimicrobial activity. Annonaceous acetogenins bind to the ubiquinone catalytic site(s) within the mitochondrial NADH:ubiquinone oxidoreductase (complex I), and block the electron transport chain in mitochondria. In addition, the acetogenins bind to and block the activity of ubiquinone-linked NADH oxidase, an enzyme overexpressed in the plasma membranes of cancer cells. This inhibits adenosine triphosphate (ATP) production, decreases intracellular ATP levels, and induces tumor cell apoptosis. Compared to normal cells, cancer cells have higher ATP demands. The Annonaceous acetogenins also inhibit microbial glucose dehydrogenase 6. Check for active clinical trials using this agent. (NCI Thesaurus)

Ansaid

(Other name for: flurbiprofen)

Antabuse

(Other name for: disulfiram)

anthocyanin-rich corn extract

A corn-based, water-soluble extract rich in the polyphenol anthocyanin, with potential antioxidant, anti-inflammatory and chemoprotective activities. Upon administration of the anthocyanin-rich corn extract, the anthocyanins scavenge reactive oxygen species (ROS), which protects healthy cells from radiation-induced oxidative stress and DNA damage. In addition, anthocyanins modulate the expression of various genes and proteins involved in inflammation, tumor cell proliferation, angiogenesis, tumor cell invasion and differentiation. This agent also chelates metals and induces the expression of enzymes involved in Phase II antioxidant and detoxification pathways, which may further protect cells against oxidative stress induced by toxins and carcinogens. Check for active clinical trials using this agent. (NCI Thesaurus)

anthracycline analogue GPX-150

A synthetic non-cardiotoxic analogue of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Anthracycline analogue GPX-150 intercalates DNA and impedes the activity of topoisomerase II, inducing single and double-stranded breaks in DNA; inhibiting DNA replication and/or repair, transcription, and protein synthesis; and activating tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)

anti c-KIT antibody-drug conjugate LOP628

An antibody-drug conjugate (ADC) consisting of a humanized monoclonal antibody against the stem cell factor receptor c-Kit (SCFR) and conjugated, via a non-cleavable linker, to the cytotoxic agent maytansine, with potential antineoplastic activity. The monoclonal antibody moiety of anti c-KIT ADC LOP628 targets and binds to the cell surface antigen c-Kit. After antibody-antigen interaction followed by internalization, the maytansine moiety binds to tubulin, inhibits microtubule assembly, and induces microtubule disassembly. This leads to a disruption of mitosis and the inhibition of cell proliferation in cancer cells expressing c-Kit. c-Kit, a transmembrane protein and receptor tyrosine kinase, is overexpressed in solid tumors and hematological malignancies; it plays a key role in the regulation of cell differentiation and proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-5T4 antibody-drug conjugate PF-06263507

An antibody-drug conjugate composed of an antibody directed against 5T4 and conjugated, via the stable linker maleimidocaproyl (mc), to the microtubule inhibitor monomethyl auristatin phenylalanine (MMAF), with potential antineoplastic activity. Upon administration, the antibody moiety of PF-06263507 selectively binds to cells expressing the 5T4 oncofetal antigen. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAF binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. 5T4, a transmembrane glycoprotein, is overexpressed by a variety of cancer cell types; its expression is correlated with increased invasiveness. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-A33 monoclonal antibody KRN330

A recombinant fully human monoclonal antibody directed against the human A33 antigen, with potential immunomodulatory and antineoplastic activity. Anti-A33 monoclonal antibody KRN330 recognizes and binds to the human A33 antigen, which may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against A33-positive colorectal cancers. A33 antigen, a 43 kDa transmembrane glycoprotein of the immunoglobulin superfamily, is highly and homogenously expressed in 95% of colorectal cancer cancers with only restricted expression in normal colonic mucosa and small bowel epithelia. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-A5B1 integrin monoclonal antibody PF-04605412

A monoclonal antibody directed against the human alpha5beta1 integrin with potential antiangiogenic and antineoplastic activities. Anti-alpha5beta1 integrin monoclonal antibody PF-04605412 selectively binds to alpha5beta1 integrin, preventing the binding of integrin ligands. This may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alpha5beta1-expressing tumor cells. Alpha5beta1 integrin, a cell adhesion and signaling receptor, is often overexpressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-ACTR/4-1BB/CD3zeta-viral vector-transduced autologous T lymphocytes ACTR087

Autologous T lymphocytes that are genetically modified and transfected with a viral vector expressing the ACTR gene, a proprietary gene encoding for an antibody-coupled T cell receptor (ATCR), with potential antineoplastic activity. The ACTR contains the extracellular Fc receptor CD16 domain, normally found on certain immune cells, such as natural killer (NK) cells, coupled to the co-immunostimulatory signaling domain 4-1BB, normally expressed on T cells, and linked to the intracellular CD3 zeta domain (CD3z), which is needed for TCR signaling. Upon reintroduction into the patient and co-administration of a cancer-specific antibody, the co-administered antibody targets and binds to the tumor-associated antigen (TAA) expressed on the tumor cell. In turn, this induces the activation of the ACTR087 cells and destruction of the tumor cells by a) releasing cytotoxins that directly kill cancer cells; b) releasing cytokines that trigger an immune response and recruit other immune-mediated killer cells to kill the tumor cells; b) targeting and killing adjacent tumor cells that are not bound to the antibody; c) inducing T-cell proliferation and thereby further enhancing the T-cell mediated tumor cell attack. CD3 zeta is one of several membrane-bound polypeptides found in the TCR/CD3 complex; it enhances the survival and persistence of T lymphocytes. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of the TAA. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-AG7 antibody drug conjugate AbGn-107

An antibody drug conjugate (ADC) composed of a monoclonal antibody that targets the tumor-associated antigen (TAA) AG7 and is linked, through a hydrophilic, self-immolative linker, to a proprietary cytotoxic payload, with potential antineoplastic activity. Upon administration of AbGn-107 the antibody moiety targets and binds to the AG7 antigen expressed on a variety of cancer cells. Upon binding and internalization, the linker is cleaved and the payload is released, binds to tubulin, inhibits tubulin polymerization and kills the AG7-expressing tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-AGS-16 monoclonal antibody AGS-16M18

A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-16 with potential antineoplastic activity. Anti-AGS-16 monoclonal antibody AGS-16M18 selectively binds to AGS-16, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) in tumor cells expressing AGS-16. While normally expressed at low levels in the proximal tubules of the kidney, AGS-16 has been found to be overexpressed in more than 95% of kidney and 40% of liver neoplasms. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-AGS-5 antibody-drug conjugate ASG-5ME

An antibody drug conjugate (ADC) containing the fully human IgG2k monoclonal antibody targeting an epitope of SLC44A4 (AGS-5) linked, via a valine-citrulline (vc) maleimidocaproyl (mc) linker, to the antimicrotubulin drug monomethyl auristatin E (MMAE), with potential antineoplastic activity. The monoclonal antibody moiety of ASG-5ME selectively binds to AGS-5. After internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis. SLC44A4, potentially a sodium-dependent transmembrane transport protein, is overexpressed on more than 80 percent of samples derived from patients with pancreatic, prostate and gastric cancers. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-AGS-8 monoclonal antibody AGS-8M4

A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-8 with potential antineoplastic activity. Anti-AGS-8 monoclonal antibody AGS-8M4 selectively binds to AGS-8, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing AGS-8. While normally expressed at low levels in the heart in response to ischemia, AGS-8 has been found to be expressed in more than 70% of ovarian neoplasms. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-ALK-1 monoclonal antibody PF-03446962

A fully human, IgG2 monoclonal antibody directed against activin-like receptor kinase 1 (ALK-1) with potential antineoplastic activity. Anti-ALK-1 monoclonal antibody PF-03446962 binds to and neutralizes ALK-1. This may disrupt tumor endothelial cell function and inhibit tumor angiogenesis, eventually leading to an inhibition of tumor cell proliferation. ALK-1, a member of the transforming growth factor beta (TGF-b) type I receptor family, is overexpressed on endothelial cells in a variety of tumor cell types and increases endothelial cell proliferation and migration. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-amyloid monoclonal antibody NEOD001

A monoclonal antibody against amyloid with potential use in the treatment of amyloid light chain (AL) and AA amyloidosis. Upon intravenous administration, anti-amyloid monoclonal antibody NEOD001 specifically binds to amyloid fibrils. This prevents the formation of amyloid deposits in certain organs and facilitates their clearance. It also reduces the level of amyloid deposits in organs and prevents organ dysfunction. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-androgen siRNA SXL01

A small-interfering RNA (siRNA) directed against androgen receptor (AR), with potential antineoplastic activity. Upon administration of anti-AR siRNA SXL01, the siRNAs bind to AR mRNAs, which may result in the inhibition of translation of the AR protein. By preventing AR expression, AR-mediated signaling is decreased, which leads to growth inhibition for AR-expressing tumor cells. AR, overexpressed in a variety of cancers, is involved in cellular proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-ANG2 monoclonal antibody MEDI-3617

A fully human IgG1 monoclonal antibody against angiopoietin 2 (ANG2), with potential antiangiogenic activity. Anti-ANG2 monoclonal antibody MEDI-3617 binds to Ang2 and interferes with the interaction between Ang2 and its receptor TEK tyrosine kinase (Tie2), thereby resulting in the disruption of vascular remodeling. This may inhibit angiogenesis and may eventually lead to an inhibition of tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

antiangiogenic drug combination TL-118

A proprietary, oral suspension containing a combination of agents comprised of a nonsteroidal anti-inflammatory agent, an alkylating agent, a histamine H2 antagonist and a sulfonamide with potential anti-angiogenic and antineoplastic activities. Antiangiogenic drug combination TL-118 is administrated as a specific dosing regimen and may result in a synergistic effect and reduce angiogenesis and inhibit tumor cell proliferation. Check for active clinical trials using this agent.

anti-AXL monoclonal antibody-MMAE conjugate

An antibody-drug conjugate (ADC), consisting of a human monoclonal antibody directed against AXL receptor tyrosine kinase (AXL; UFO) and conjugated, through a protease-cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of HuMax-AXL-ADC binds to AXL, which is expressed on the surfaces of a variety of cancer cell types. Upon endocytosis and enzymatic cleavage, MMAE is released into the tumor cell cytosol, where it binds to tubulin and inhibits tubulin polymerization; this may result in G2/M phase arrest and apoptosis. AXL, a member of the TAM (TYRO3, AXL and MER) family of receptor tyrosine kinases and overexpressed by many tumor cell types, plays a key role in tumor cell proliferation, survival, invasion and metastasis; its expression is associated with drug resistance and poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-B4 blocked ricin immunotoxin

An immunotoxin comprised of an anti-B4 (anti-CD19) murine monoclonal antibody linked to the modified plant-derived toxin blocked ricin. The antibody moiety of anti-B4 blocked ricin immunotoxin binds to B lymphocytes that express B4; after internalization of the immunotoxin by the B4-expressing B cell, the ricin moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in the B lymphocyte 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. "Blocked" ricin is ricin which has been chemically modified such that the lectin binding sites of the B chain (galactose-binding sites) have been blocked by covalent attachment of affinity ligands, leaving the ribosome-inactivating activity of the ricin A chain intact. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-B7-H3 antibody DS-5573a

An antibody directed against the immunoregulatory protein B7-homologue 3 (B7-H3, CD276), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, anti-B7-H3 antibody DS-5573a binds to the cell surface antigen B7-H3, thereby blocking B7-H3-mediated signaling. This abrogates the inhibitory effect on T-cell activation and may activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against B7-H3-expressing tumor cells. B7-H3, a type I transmembrane protein and a member of the B7 co-stimulatory protein superfamily, is overexpressed on certain tumor cell types and on various immune cells. It is a negative regulator of the T-cell activation and and its overexpression plays a key role in tumor cell invasion and metastasis. Check for active clinical trials using this agent. (NCI Thesaurus)

anti-BCMA antibody-drug conjugate GSK2857916

An antibody-drug conjugate (ADC) consisting of an afucosylated, humanized monoclonal antibody, directed against the B-cell maturation antigen (BCMA), conjugated to the auristatin analogue and microtubule inhibitor monomethyl auristatin phenylalanine (MMAF), with potential antineoplastic activity. The anti-BCMA antibody moiety of anti-BCMA ADC GSK2857916 selectively binds to the BCMA on tumor cell surfaces. Upon internalization, the MMAF moiety binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces tumor cell apoptosis. In addition, GSK2857916 induces antibody-dependent cellular cytotoxicity (ADCC). Altogether, this results in the inhibition of cellular proliferation in tumor cells that overexpress BCMA. BCMA, a receptor for a proliferation-inducing ligand and B-cell activating factor, is a member of the tumor necrosis factor (TNF) receptor superfamily and plays a key role in plasma survival; it is found on the surfaces of plasma cells and overexpressed on malignant plasma cells. Afucosylation of the antibody moiety increases ADCC. Check for active clinical trials using this agent. (NCI Thesaurus)

antibiotic SQ109

An orally available, acid-stable diamine antibiotic, with potential antimicrobial activity against a variety of bacteria including Helicobacter pylori (H. pylori) and Mycobacterium tuberculosis (M. tuberculosis). As an ethambutol analogue with asymmetric structure, SQ109 does not act on the same target as ethambutol. However, this agent interferes with cell wall synthesis, thereby causing weakening of the cell wall and ultimately cell lysis. Check for active clinical trials using this agent. (NCI Thesaurus)

antibody-drug conjugate ABBV-085

An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against a tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of ABBV-085 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent.

antibody-drug conjugate ADCT-402

An antibody-drug conjugate (ADC) consisting of an anti-CD19 humanized monoclonal antibody conjugated, via a cleavable linker comprised of valine-alanine and maleimide, to a cytotoxic, cross-linking agent pyrrolobenzodiazepine (PBD) dimer, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the monoclonal antibody portion of anti-CD19-PBD conjugate ADCT-402 targets the cell surface antigen CD19 on various cancer cells. Upon antibody/antigen binding and internalization, the cytotoxic PBD moiety is released. The imine groups of the PBD moiety 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 CD19-overexpressing tumor cells. CD19, a transmembrane receptor and tumor-associated antigen (TAA), is expressed on a number of B-cell-derived cancers. Check for active clinical trials using this agent. (NCI Thesaurus)

antibody-drug conjugate anti-TIM-1-vcMMAE CDX-014

A human immunoglobulin G1 (IgG1) monoclonal antibody-drug conjugate (ADC) targeting the extracellular domain of T-cell immunoglobulin mucin-1 (TIM-1) (clone CR014) and linked, via a valine-citrulline (vc) peptide linker, to the potent cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration of ADC Anti-TIM-1-vcMMAE CDX-014, the monoclonal antibody moiety targets and binds to TIM-1. Upon internalization and proteolytic cleavage, MMAE is released into the cytosol of TIM-1-expressing tumor cells, binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. TIM-1 is upregulated in a variety of cancer cell types while only minimally expressed in healthy tissue. The linkage system in CDX-014 is highly stable in plasma, resulting in cytotoxic specificity for TIM-1-positive cells. Check for active clinical trials using this agent. (NCI Thesaurus)

antibody-drug conjugate BAY79-4620

A monoclonal antibody (MoAb) directed against the MN protein with potential antineoplastic activity. Upon administration of BAY79-4620, this MoAb may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response and an antibody mediated cellular cytotoxicity (ADCC) against MN-expressing tumor cells. MN, a transmembrane glycoprotein, is expressed in some human carcinomas and appears to be involved in cancer cell proliferation and transformation. Check for active clinical trials using this agent. (NCI Thesaurus)

antibody-drug conjugate DFRF4539A

An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against a specific myeloma antigen and conjugated to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DFRF4539A selectively binds to a specific protein expressed on the surface of myeloma cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)

antibody-drug conjugate PF-06647020



An antibody-drug conjugate (ADC) composed of a proprietary monoclonal antibody against an unnamed tumor-associated antigen (TAA) linked to an as of yet undisclosed cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, the monoclonal antibody moiety of PF-06647020 targets and binds to the TAA expressed on tumor cells. Upon binding and internalization, the cytotoxic agent is released and kills the TAA-expressing cancer cells, through an as of yet unknown mechanism of action. Check for active clinical trials using this agent. (NCI Thesaurus)

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