jueves, 31 de mayo de 2018

NCI Drug Dictionary - National Cancer Institute | t/T/2

NCI Drug Dictionary - National Cancer Institute

National Cancer Institute



428 results found for: T
Thorazine
(Other name for: chlorpromazine)
threonine tyrosine kinase inhibitor CFI-402257
An orally bioavailable, selective inhibitor of the dual specificity protein kinase TTK (monopolar spindle 1 kinase, Mps1), with potential antineoplastic activity. Upon administration, the Mps1 inhibitor CFI-402257 selectively binds to and inhibits the activity of Mps1. This inactivates the spindle assembly checkpoint (SAC) and accelerates mitosis, resulting in chromosomal misalignment and missegregation, and mitotic checkpoint complex destabilization. This induces cell death in Mps1-overexpressing cancer cells. Mps1, a tyrosine and serine/threonine kinase expressed in proliferating normal tissues, is essential for proper SAC functioning and chromosome alignment. Overexpressed in various human tumors, Mps1 plays a key role in uncontrolled tumor cell growth. Check for active clinical trials using this agent. (NCI Thesaurus)
thrombomodulin alfa
A recombinant, soluble form of the human protein thrombomodulin, with potential anticoagulant activity. Upon administration, thrombomodulin binds to thrombin, which stimulates the activation of protein C. Activated protein C (APC) degrades factor Va and Factor VIIa in the presence of the cofactor protein S, inhibits thrombin formation, and prevents both thrombin-mediated coagulation and further clot formation. Check for active clinical trials using this agent. (NCI Thesaurus)
Thymectacin
(Other name for: brivudine phosphoramidate)
thymidine
A pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix. Check for active clinical trials using this agent. (NCI Thesaurus)
thymidylate synthase inhibitor DFP-11207
An orally available thymidylate synthase (TS) inhibitor with potential antineoplastic activity. Upon oral administration, DFP-11207 binds to and inhibits TS. This reduces thymine nucleotide synthesis, inhibits DNA synthesis and cell division, causes DNA damage and leads to tumor cell apoptosis. TS catalyzes the conversion of deoxyuridine monophosphate (dUMP) to deoxythymidine monophosphate (dTMP). Check for active clinical trials using this agent. (NCI Thesaurus)
Thymitaq
(Other name for: nolatrexed dihydrochloride)
Thymoglobulin
(Other name for: anti-thymocyte globulin)
thymopentin
A synthetic pentapeptide which is the active site of the naturally occurring hormone thymopoietin with immunomodulating properties. Thymopentin enhances the production of thymic T cells and may help restore immunocompetence in immunosuppressed subjects. This agent also augments the effects of ionizing radiation by arresting cancer cells in the G2/M phase of the cell cycle. Check for active clinical trials using this agent. (NCI Thesaurus)
Thyrogen
(Other name for: recombinant thyrotropin alfa)
thyroxine
A hormone synthesized and secreted by the thyroid gland containing four iodine atoms and is converted to triiodothyronine (T3) in the body, influencing metabolism and organ function. Check for active clinical trials using this agent. (NCI Thesaurus)
Thytropar
(Other name for: recombinant thyroid-stimulating hormone)
tiazofurin
A synthetic nucleoside analogue with antineoplastic activity. Tiazofurin (TR) is anabolized intracellularly to an analogue of NAD, tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH); IMPDH is the rate-limiting enzyme for de novo purine synthesis. Inhibition of IMPDH results in reduced levels of guanylates, resulting in the inhibition tumor cell growth in vitro and in vivo. Check for active clinical trials using this agent. (NCI Thesaurus)
tibolone
A synthetic anabolic steroid with estrogenic, androgenic and progestagenic activities. The 3alpha- and 3beta-hydroxy metabolites of tibilone activate estrogenic receptors (ERs) in bone and vaginal tissue leading to a decrease in bone turnover, and decreased vaginal dryness, respectively; derived from the 3beta-hydroxy metabolite, its delta4-isomer activates androgenic receptors (ARs) in the brain and liver and progestogenic receptors (PRs) in endometrial tissue, affecting sexual function, lipid metabolism, and endometrial function, respectively. In breast and endometrial tissue, tibolone metabolites inhibit sulfatase, preventing the conversion of circulating estrone sulfate and estradiol sulfate to estrone and estradiol, respectively; estrogen-mediated effects in the breast and uterus are thus reduced. Check for active clinical trials using this agent. (NCI Thesaurus)
TICE BCG solution
(Other name for: BCG solution)
tigapotide
A synthetic 15-mer peptide corresponding to amino acids 31-45 of the 94-amino acid isoform of human prostate secretory protein (PSP-94) with potential anti-metastasis and anti-angiogenesis activities. Tigapotide may inhibit the secretion of the metastasis-related protein matrix metalloproteinase-9 (MMP-9) and its potential binding to its cell surface receptor CD44; may interfere with the vascular endothelial growth factor (VEGF) signaling pathway, resulting in an anti-angiogenesis effect; and may reduce the levels of parathyroid hormone-related protein (PTHrP), decreasing plasma calcium levels. PSP-94, one of three predominant proteins found in seminal fluid, may be down-regulated in prostate cancer, representing a potential survival mechanism for prostate cancer cells. MMP-9 is implicated in the invasion and metastasis of cancer. PTHrP may be expressed by various tumor cell types, resulting in the hypercalcemia of malignancy. Check for active clinical trials using this agent. (NCI Thesaurus)
tigatuzumab
A humanized agonistic monoclonal antibody directed against human tumor necrosis factor-related apoptosis-inducing ligand receptor 2 (TRAIL-R2) with potential antitumor activity. Mimicking the natural receptor ligand TRAIL, tigatuzumab binds to TRAIL-R2, activating signal transduction pathways that may result in tumor cell apoptosis and a reduction in tumor growth. A member of the tumor necrosis factor (TNF) receptor family, TRAIL-R2, also known as DR5 (death receptor 5), is expressed on the surfaces of many types of malignant cells. Check for active clinical trials using this agent. (NCI Thesaurus)
tigecycline
A broad-spectrum glycylcycline antibiotic derived from tetracycline. Tigecycline binds to the 30S ribosomal subunit, thereby interfering with the binding of aminoacyl-tRNA to the mRNA-ribosome complex. This prevents the incorporation of amino acid residues into the elongating peptide chain, inhibiting protein synthesis and eventually bacterial cell growth.
TIGIT-targeting agent MK-7684
An antagonistic agent targeting the co-inhibitory molecule and immune checkpoint inhibitor T-cell immunoglobulin (Ig) and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT; T-cell immunoreceptor with Ig and ITIM domains; T-cell immunoglobulin and ITIM domain), with potential immune checkpoint inhibitory and antineoplastic activities. Upon administration, MK-7684 targets and binds to TIGIT expressed on various immune cells, particularly on tumor-infiltrating T lymphocytes (TILs) and natural killer (NK) cells, thereby preventing the interaction of TIGIT with its ligands CD112 (nectin-2; poliovirus receptor related-2; PVRL2) and CD155 (poliovirus receptor; PVR; nectin-like protein 5; NECL-5), which are expressed on T cells, NK cells and certain cancer cells. This enhances the interaction of CD112 and CD155 with the costimulatory receptor CD226 (DNAX Accessory molecule-1; DNAM-1), which is expressed on immune cells, such as NK cells and CD8+ T cells, and activates CD226-mediated signaling. This activates the immune system to exert a T-cell-mediated immune response against cancer cells. TIGIT, a member of the Ig super family and an immune inhibitory receptor, is overexpressed on tumor antigen-specific CD8+ T cells and CD8+ TILs and plays a key role in the suppression of T-cell proliferation and activation; it is involved in tumor cell immune evasion, and the inhibition of antiviral immune responses. Check for active clinical trials using this agent. (NCI Thesaurus)
TIL 1383I T cell receptor-transduced autologous T cells
Autologous peripheral blood lymphocytes-derived T cells transduced with a retroviral encoding TIL 1383I, a T cell receptor (TCR) specific for melanoma antigen tyrosinase, with potential immunostimulating and antineoplastic activity. After transduction, expansion in culture, and reintroduction into the patient, TIL 1383I TCR-transduced autologous T cells bind to tumor cells expressing tyrosinase, which may induce cytokine expression, activation and proliferation of T-cells, and a specific cytotoxic T-lymphocyte (CTL) response against tyrosinase-expressing tumor cells. TIL 1383I TCR originated from a melanoma patient’s CD4+ tumor-infiltrating lymphocytes and is reactive against a class I MHC (HLA-A2)-restricted epitope (368-376) of tyrosinase. Check for active clinical trials using this agent. (NCI Thesaurus)
timolol maleate gel forming solution
A gel forming solution containing the maleate salt of timolol, a propanolamine derivative and a non-selective beta-adrenergic antagonist, with intraocular pressure-reducing activity. Although the precise mechanism of action of timolol's ocular hypotensive action is not clearly established at this time, studies suggest that it may be the result of decreased aqueous humor production (possibly by reduction of blood flow to the ciliary processes and cAMP synthesis) as well as a slight increase in outflow facility. Timolol gel-forming solution can potentially be used topically as well, in the prevention of the neoangiogenesis that may occur following pulsed dye laser treatment of port wine stains. Check for active clinical trials using this agent. (NCI Thesaurus)
timonacic
A cyclic sulfur amino acid derivative with potential antineoplastic and antioxidant activities. Acting on cellular membranes of malignant cells through an unknown mechanism, timonacic may induce malignant cells to revert back to an untransformed state. This agent may also restore contact inhibition, a phenomenon characterized by the paracrine inhibition of mitosis following the formation of a critical cell mass, presumably the result of cell-to-cell signal transfer. Timonacic may also produce antioxidant effects secondary to its release of cysteine and restoration of glutathione concentrations. Check for active clinical trials using this agent. (NCI Thesaurus)
Timoptic-XE
(Other name for: timolol maleate gel forming solution)
Tindamax
(Other name for: tinidazole)
tinidazole
A 5-nitroimidazole derivative with antiprotozoal property. Although the mechanism of action has not been fully elucidated, it has been suggested that tinidazole is metabolized and yields nitrite anions and metronidazole. Metronidazole's nitro group in turn is reduced via the parasite ferredoxin, thereby generating a series of free nitro radicals including nitro anions. Toxicity is achieved via depletion of sulfhydryl groups and DNA strand breaks with multiple hits having an additive effect and ultimately leading to cell death. Check for active clinical trials using this agent. (NCI Thesaurus)
tinzaparin sodium
The sodium salt of a low molecular weight heparin (LMWH) obtained by controlled enzymatic depolymerization of heparin from porcine intestinal mucosa with antithrombotic properties. Tinzaparin is a potent inhibitor of several activated coagulation factors, especially Factors Xa and IIa (thrombin); its primary activity is mediated through the plasma protease inhibitor antithrombin. In addition, this agent may inhibit angiogenesis through: 1) competitive binding of the heparin-binding sites on endothelial cells for the proangiogenic cytokines vascular endothelial growth factor (VEGF) and beta-fibroblast growth factor (beta-FGF) and 2) increasing the release of tissue factor pathway inhibitor (TFPI), a negative regulator of angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
tiomolibdate diammonium
An ammonium salt with potential antiangiogenic and antitumor activities. ammonium Tiomolibdate diammonium has been found to deplete systemic copper reserves through an unknown mechanism. This agent has been shown to inhibit the activities of cuproenzymes, including superoxide dismutase 1 (SOD1) and cytochrome c oxidase (COX), which may contribute to its antiangiogenic and antitumor effects. Check for active clinical trials using this agent. (NCI Thesaurus)
tiotropium bromide monohydrate
The monohydrate bromide salt form of tiotropium, a quaternary ammonium derivative of atropine and a long-acting muscarinic receptor antagonist, with bronchodilating activity. Upon inhalation, tiotropium binds to and blocks mainly muscarinic M3 receptors located on smooth muscle cells, thereby preventing smooth muscle contraction Check for active clinical trials using this agent. (NCI Thesaurus)
tipifarnib
A nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
tirabrutinib
An orally available formulation containing an inhibitor of Bruton agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, tirabrutinib covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
tirapazamine
A benzotriazine di-N-oxide with potential antineoplastic activity. Tirapazamine is selectively activated by multiple reductases to form free radicals in hypoxic cells, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. This agent also sensitizes hypoxic cells to ionizing radiation and inhibits the repair of radiation-induced DNA strand breaks via inhibition of topoisomerase II. Check for active clinical trials using this agent. (NCI Thesaurus)
Tirazone
(Other name for: tirapazamine)
tisagenlecleucel
Autologous T lymphocytes transduced with a modified lentiviral vector expressing a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment) and the zeta chain of the TCR/CD3 complex (CD3-zeta), coupled to the signaling domain of 4-1BB (CD137), with potential immunomodulating and antineoplastic activities. Upon transfusion, tisagenlecleucel direct the T lymphocytes to CD19-expressing tumor cells, thereby inducing a selective toxicity in CD19-expressing tumor cells. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD19 and the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3-zeta (or CD247) is a transmembrane signaling adaptor polypeptide that regulates the assembly of complete TCR complexes and their expression on the cell surface. Check for active clinical trials using this agent. (NCI Thesaurus)
TISSEEL VH
(Other name for: fibrin sealant)
titanium dioxide/zinc oxide sunscreen cream SPF 60
A sunscreen formulated with titanium dioxide and zinc oxide with broad UV spectrum-blocking properties. Upon topical application, titanium dioxide and zinc oxide reflect and block both UVA and UVB ultraviolet light rays, protecting the skin against UVA and UVB radiation that causes sunburn, premature aging of the skin and skin cancer.SPF30 and SPF60 contain 5% titanium dioxide and zinc oxide, and 7.5% titanium dioxide and zinc, oxide respectively. Check for active clinical trials using this agent. (NCI Thesaurus)
tivantinib
An orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity. Tivantinib binds to the c-Met protein and disrupts c-Met signal transduction pathways, which may induce cell death in tumor cells overexpressing c-Met protein or expressing consitutively activated c-Met protein. c-Met protein, the product of the proto-oncogene c-Met, is a receptor tyrosine kinase also known as hepatocyte growth factor receptor (HGFR); this protein is overexpressed or mutated in many tumor cell types and plays key roles in tumor cell proliferation, survival, invasion, and metastasis, and tumor angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
Tivicay
(Other name for: dolutegravir)
tivozanib
An orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGFR tyrosine kinases, frequently overexpressed by a variety of tumor cell types, play a key role in angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
tizanidine hydrochloride
The hydrochloride salt form of tizanidine, an imidazoline derivative structurally similar to clonidine and an adrenergic agonist with muscle relaxant property. Tizanidine stimulates alpha-2 adrenergic receptors in the central nervous system, thereby inhibiting presynaptic release of norepinephrine and increasing the inhibitory effect on alpha motor neurons and motor reflexes. Tizanidine exerts some activity at the postsynaptic excitatory amino acid receptors and imidazoline receptors which may contribute to the overall reduction in facilitation of spinal motor neurons. Overall, tizanidine hydrochloride causes muscle relaxation, reduces spasticity and antinociceptive effects. Check for active clinical trialsusing this agent. (NCI Thesaurus)
TLR 2/6/9 agonist PUL-042
A solution consisting of a combination of two toll-like receptor (TLR) ligands: Pam2CSK4 acetate (Pam2), a synthetic diacylated lipopeptide (LP) that is an agonist of TLR2 and TLR6 (TLR2/6) and the TLR9 agonist oligodeoxynucleotide (ODN) M362, which contains unmethylated CpG-based dinucleotides, with potential immunostimulating activity. Upon administration via inhalation of the PUL-042 solution, the components in PUL-042 bind to and activate TLRs on lung epithelial cells. This induces the epithelial cells to produce peptides and reactive oxygen species (ROS) against pathogens, including bacteria, fungi and viruses, that are present in the lungs. M362, through binding of the CpG motifs to TLR9 and subsequent TLR9-mediated signaling, initiates the innate immune system and activates macrophages, natural killer (NK) cells, B cells, and plasmacytoid dendritic cells (pDCs), stimulates interferon-alpha (IFN-a) production and induces a T-helper 1 cells (Th1)-mediated immune response. Pam2CSK4, through TLR2/6, activates the production of T-helper 2 cells (Th2), leading to the production of Th2-specific cytokines. Altogether, this protects against and kills the pathogens present in the lungs and prevents pulmonary infection. TLRs play fundamental roles in both pathogen recognition and the activation of innate immunity. Check for active clinical trials using this agent. (NCI Thesaurus)
TLR4 agonist G100
A synthetic lipid A derivative and selective toll-like receptor 4 (TLR4) agonist composed of glucopyranosyl lipid-A (GLA) in a stable, oil-in-water emulsion (GLA-SE), with potential immunostimulating and antineoplastic activities. Upon intratumoral administration into the immunosuppressed tumor microenvironment (TME), TLR4 agonist G100 binds to and activates TLR4 on various immune cells, thereby stimulating dendritic cells (DCs), monocytes and macrophages. This activation results in the production of pro-inflammatory cytokines and chemokines. This induces a T helper cell-1 (Th1) immune response and activates a cytotoxic T-lymphocyte (CTL) response against tumor-associated antigens (TAAs) that were released in the TME by tumor cells lysed during cytotoxic treatments, such as radiotherapy. TLR4, a member of the TLR family, plays a key role in the activation of innate immunity. Check for active clinical trials using this agent. (NCI Thesaurus)
TLR4 agonist GSK1795091
A toll-like receptor 4 (TLR4) agonist, with potential immunoadjuvant activity. Upon administration, GSK1795091 binds to and activates TLR4, thereby stimulating dendritic cells (DCs), monocytes and macrophages. This activation results in the production of pro-inflammatory cytokines, including interferon gamma (IFN-g), tumor necrosis factor-alpha (TNF-a) and the interleukins (IL), IL-1 beta, -6 and -12. This may induce a T helper cell-1 (Th1) immune response and, upon co-administration of a vaccine containing tumor-associated antigens (TAAs), activates a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing those TAAs. TLR4, a member of the TLR family, plays a key role in the activation of innate immunity. Check for active clinical trials using this agent. (NCI Thesaurus)
TLR7 agonist ANA773 tosylate
The tosylate salt form of ANA773, a Toll-like Receptor 7 (TLR7) agonist prodrug with potential immunostimulating activity. Upon oral administration, ANA773 is metabolized into its active form that binds to and activates TLR7, thereby stimulating dendritic cells (DCs) and enhancing natural killer cell (NK) cytotoxicity. This activation results in the production of proinflammatory cytokines, including interferon alpha, and enhanced antibody-dependent cellular cytotoxicity (ADCC). TLR7 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)
TLR7/8 agonist MEDI9197
A toll-like receptor type 7 and 8 (TLR7/8) agonist with potential immunostimulating and antitumor activities. Upon intratumoral administration, TLR7/8 agonist MEDI9197 binds to and activates TLR7 and 8, thereby stimulating antigen-presenting cells (APCs), including dendritic cells (DCs). Activation of DCs results in the production of proinflammatory cytokines, and the activation of cytotoxic T-lymphocyte (CTL) and B-lymphocyte immune responses. This may cause tumor cell lysis. TLR7 and 8, members of the TLR family, play fundamental roles in the activation of the immune system. Check for active clinical trialsusing this agent. (NCI Thesaurus)
TLR8 agonist VTX-2337
A small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities. TLR8 agonist VTX-2337 binds to TLR8, present in cutaneous dendritic cells, monocytes/macrophages, and mast cells, which may result in the activation of the central transcription factor nuclear factor-B, the secretion of proinflammatory cytokines and other mediators, and a Th1-weighted antitumoral cellular immune response. Primarily localized to endosomal membranes intracellularly, TLR8, like other TLRs, recognizes pathogen-associated molecular patterns (PAMPs) and plays a key role in the innate immune system. Check for active clinical trials using this agent. (NCI Thesaurus)
TLR9 agonist DUK-CPG-001
A synthetic CpG-rich oligonucleotide with potential immunopotentiating activity. TLR9 agonist DUK-CPG-001 binds to and activates intracellular toll-like receptor 9 (TLR9) in monocytes/macrophages, plasmacytoid dendritic cells (DCs), natural killer (NK) cells and B cells. This initiates immune signaling pathways, activates DCs, NK cells and B cells, and induces both the production of T-helper 1 cells (Th1) and a Th1-mediated immune response. TLR9 is a member of the TLR family, which plays a key role in both pathogen recognition and the activation of innate immunity. Check for active clinical trials using this agent. (NCI Thesaurus)
TLR9 agonist EMD 1201081
A synthetic oligonucleotide containing phosphorothioate oligodeoxynucleotide with potential immunopotentiating activity. TLR9 agonist EMD 1201081 binds to and activates the intracellular Toll-like receptor (TLR) 9 in monocytes/macrophages, plasmacytoid dendritic cells (DCs) and B cells, initiating immune signaling pathways, activating B cells and inducing T-helper cell cytokine production. 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)
TLR9 agonist IMO-2055
A synthetic oligonucleotide containing unmethylated CpG dinucleotides with potential immunopotentiating activity. Mimicking unmethylated CpG sequences in bacterial DNA, TLR9 agonist IMO-2055 binds to and activates intracellular Toll-like receptors (TLR) 9 in monocytes/macrophages, plasmacytoid dendritic cells (DCs) and B cells, initiating immune signaling pathways and activating B cells and DCs and inducing T-helper cell cytokine production. 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 trialsusing this agent. (NCI Thesaurus)
TLR9 agonist MGN1703
A synthetic oligonucleotide based on a proprietary double stem-loop immunomodulator design with potential immunostimulating activity. TLR9 agonist MGN1703 binds to and activates intracellular Toll-like receptor 9 (TLR9) in monocytes/macrophages, plasmacytoidal and myeloid dendritic cells (DCs), and natural killer (NK) cells, initiating immune signaling pathways and inducing T-helper 1 cell (Th1) production leading to the production of memory T cells and a Th1-mediated immune response. By activating the immune system, MGN1703 may attack tumor associated antigen (TAAs). 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)
TLR9 agonist SD-101
A proprietary oligonucleotide with immunostimulatory activity. Immunostimulatory phosphorothiolate oligodeoxyribonucleotide SD-101 targets Toll-Like Receptor 9 (TLR9) found on a specialized subset of dendritic cells. The interaction of TLR9 with SD-101, in conjunction with an allergen or antigen, induces activation of memory T helper cells 1 (Th1) against a specific pathogen or allergen, thereby leading to long-lasting therapeutic effects. Furthermore, this agent does not cause a generalized activation of the immune system. Check for active clinical trials using this agent. (NCI Thesaurus)
TLR-directed cationic lipid-DNA complex JVRS-100
A cationic lipid DNA complex (CLDC) consisting of DOTIM/cholesterol liposomes and plasmid DNA, containing immunostimulatory CpG and non-CpG motifs, with potential immunostimulating and antineoplastic activities. Upon systemic administration, TLR-directed cationic lipid-DNA complex JVRS-100 enters dendritic cells (DCs) and macrophages; immunostimulatory DNA binds to and activates Toll-like receptors (TLRs), which may result in the generation of anti-tumor natural killer (NK) cell and T-cell responses by the innate immune system. In addition, as a vaccine adjuvant, this agent may induce a strong cytotoxic T-lymphocyte (CTL) response to co-administered antigen. Check for active clinical trials using this agent. (NCI Thesaurus)
TNFerade
(Other name for: golnerminogene pradenovec)
TNP-470
A synthetic analog of fumagillin, an antibiotic isolated from the fungus Aspergillus fumigatus fresenius with antineoplastic activity. TNP-470 binds to and irreversibly inactivates methionine animopeptidase-2 (MetAP2), resulting in endothelial cell cycle arrest late in the G1 phase and inhibition of tumor angiogenesis. This agent may also induce the p53 pathway, thereby stimulating the production of cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
tobramycin sulfate
The sulfate salt of tobramycin, an aminoglycoside antibiotic derived from the bacterium Streptomyces tenebrarius with bactericidal activity. Following active transport into the cell, tobramycin binds irreversibly to a specific aminoglycoside receptor on the bacterial 30S ribosomal subunit and fixes the 30 S-50 S ribosomal complex at the start codon (AUG), interfering with the initiation of protein synthesis. In addition, this agent induces misreading of the mRNA template, which results in 1) detachment of the ribosomal complex and inhibition of protein elongation or 2) incorporation of the incorrect amino acids into the growing polypeptide chain and the production of abnormal or nonfunctional proteins. Altogether, cell permeability is altered and cell death ensues. Check for active clinical trials using this agent. (NCI Thesaurus)
Tobrex
(Other name for: tobramycin sulfate)
Toca FC
(Other name for: extended-release flucytosine)
tocilizumab
A recombinant, humanized IgG1 monoclonal antibody directed against the interleukin-6 receptor (IL-6R) with immunosuppressant activity. Tocilizumab targets and binds to both the soluble form of IL-6R (sIL-6R) and the membrane-bound form (mIL-6R), thereby blocking the binding of IL-6 to its receptor. This prevents IL-6-mediated signaling. Il-6, a pro-inflammatory cytokine that plays an important role in the regulation of the immune response, is overproduced in autoimmune disorders and certain types of cancers. Check for active clinical trials using this agent. (NCI Thesaurus)
tocladesine
An antimetabolite and a chlorine derivative of the intracellular secondary messenger, cyclic adenosine 3,5-monophosphate (cAMP), with potential antineoplastic activity. Tocladesine appears to be converted to 8-chloro-adenosine by phosphodiesterases and subsequently phosphorylated to 8-chloro-ATP, which functions as a purine analogue and competes with ATP in transcription. In addition, generation of 8-chloro-ATP depletes the endogenous ATP pool that is essential for many biological reactions in intracellular energy transfer. As a result, this agent causes RNA synthesis inhibition, blocks cellular proliferation, and induces apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
tocophersolan
A water-soluble amphipathic formulation of d-alpha-tocopherol succinate coupled, through a succinate linker, to polyethylene glycol (PEG) 1000. Due to its amphipathic property in which it forms its own micelles, tocophersolan is easily taken up into enterocytes, even in the absence of bile salts; fat soluble d-alpha-tocopherol is then released after hydrolysis. This formulation enhances the absorption of d-alpha-tocopherol compared to the administration of free d-alpha-tocopherol. In addition, tocophersolan may enhance the absorption of water-insoluble agents and other fat-soluble vitamins. Check for active clinical trials using this agent. (NCI Thesaurus)
Tocosol Paclitaxel
(Other name for: paclitaxel vitamin E-based emulsion formulation)
tocotrienol
Any of the four forms, alpha, beta, gamma and delta, of a member of the vitamin E family, with potential hypocholesterolemic, antithrombotic, antioxidant, immunomodulating and antineoplastic activities. Tocotrienol inhibits the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, thereby lowering cholesterol levels. In addition, tocotrienol acts through multiple signal transduction pathways to induce cell cycle arrest and caspase-mediated apoptosis, and to decrease tumor cell proliferation. In addition, this agent may inhibit angiogenesis through the blockage of vascular endothelial growth factor receptor (VEGFR) and the subsequent inhibition of tumor cell-induced vessel formation. Also, this agent prevents free radical formation and inhibits lipid peroxidation, thereby preventing DNA cell damage. Tocotrienol farnesyl isoprenoid side chains contain 3 double bonds, which are absent in tocopherols, likely contribute to its anti-cancer activities. Check for active clinical trials using this agent. (NCI Thesaurus)
tocotrienol-rich fraction
An orally available nutritional supplement containing high amounts of the vitamin E family member tocotrienol with antioxidant, hypolipidemic and potential immunomodulating and antiproliferative activity. Upon oral administration, tocotrienol-rich fraction (TRF) accumulates in tumor cells and induces cell cycle arrest, programmed cell death, and inhibits tumor cell proliferation. In addition, this agent suppresses 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase activity and inhibits angiogenesis. Rice bran oil, palm oil and annatto seed oil are common sources of TRF. Check for active clinical trials using this agent. (NCI Thesaurus)
tofacitinib
An orally available inhibitor of Janus kinases (JAK), with immunomodulatory and anti-inflammatory activities. Upon administration, tofacitinib binds to JAK and prevents the activation of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This may decrease the production of pro-inflammatory cytokines, such as interleukin (IL)-6, -7, -15, -21, interferon-alpha and -beta, and may prevent both an inflammatory response and the inflammation-induced damage caused by certain immunological diseases. JAK kinases are intracellular enzymes involved in signaling pathways affecting hematopoiesis, immunity and inflammation. Check for active clinical trials using this agent. (NCI Thesaurus)
Tolak
(Other name for: topical fluorouracil)
tolazamide
An intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. Tolazamide is converted into five major metabolites that are excreted into the urine. Tolazamide is more potent than tolbutamide and similar in potency to chlorpropamide on a milligram basis. This agent may cause cholestatic jaundice. Check for active clinical trialsusing this agent. (NCI Thesaurus)
tolbutamide
A first-generation sulfonylurea with hypoglycemic activity. Tolbutamide binds to and blocks adenosine triphosphate (ATP)-sensitive potassium channels on the beta cell membrane of the pancreatic islet tissues. This leads to potassium efflux, which results in depolarization, calcium influx, calcium-calmodulin binding, kinase activation, and release of insulin-containing granules by exocytosis. In addition, tolbutamide may increase the number and affinity of cell surface insulin receptors, thereby enhancing the peripheral response to insulin. Tolbutamide is a CYP2C9 substrate. Check for active clinical trials using this agent. (NCI Thesaurus)
tolcapone
A benzophenone derivative and a catechol-O-methyltransferase (COMT) inhibitor. Tolcapone selectively and reversibly inhibits COMT, an enzyme that catalyzes the metabolism of biologically active catechols and their hydroxylated metabolites by transferring the methyl group of S-adenosyl-L-methionine to the phenolic group of catechol-containing substrates. When given in conjunction with a peripheral dopa decarboxylase inhibitor and levodopa, tolcapone may prevent the metabolism of levodopa to 3-methoxy-4-hydroxy- L-phenylalanine (3-OMD) in the brain and peripheral tissues leading to increased bioavailability and enhancement of delivery to the central nervous system (CNS) of levodopa. Check for active clinical trials using this agent. (NCI Thesaurus)
tolfenamic acid
An orally available, benzoic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, analgesic and potential anti-neoplastic activities. Tolfenamic acid inhibits the activity of the enzymes cyclooxygenase (COX) I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The decrease in prostaglandin synthesis results in the therapeutic effects of this agent. Tolfenamic acid also inhibits thromboxane A2 synthesis, by thromboxane synthase, which decreases platelet aggregation. In addition, this agent exerts anti-tumor effects through COX-dependent and independent pathways. Specifically, this agent induces the production of reactive oxygen species, causes DNA damage, increases nuclear factor-kappa B (NF-kB) activation and the expression of activating transcription factor 3 (ATF3) and NSAID-activated gene-1 (NAG1), and inhibits the expression of specificity proteins (Sp), which reduces the expression of Sp-dependent anti-apoptotic and growth-promoting proteins. Altogether, this enhances tumor cell apoptosis, and reduces tumor cell growth and angiogenesis. Check for active clinical trials using this agent. (NCI Thesaurus)
Tolinase
(Other name for: tolazamide)
Toll-like receptor 9 agonist IMO-2125
A proprietary synthetic oligonucleotide-based agonist of toll-like receptor 9 (TLR9), with potential immunostimulating activity. Upon administration, TLR9 agonist IMO-2125 binds to and activates TLR9 expressed by plasmacytoid dendritic cells (pDCs) and B cells. This initiates immune signaling pathways, activates B cells and pDCs, and induces a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells. 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)
tomato-soy juice
A juice containing tomato extract and soy protein with potential chemopreventive and antiproliferative activities. Tomato-soy juice contains phytochemicals, including flavonoids, such as the soy isoflavone genistein, and carotenoids, including lycopene. These phytochemicals may exhibit antioxidative activity, antitumor activity by modulating certain tumor-associated signal transduction pathways, and apoptosis-inducing activity. Check for active clinical trials using this agent. (NCI Thesaurus)
Tomudex
(Other name for: raltitrexed)
Topamax
(Other name for: topiramate)
topical betulinic acid
A topical formulation of a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) with antiinflammatory, anti-HIV and antineoplastic activities. Betulinic acid induces apoptosis through induction of changes in mitochondrial membrane potential, production of reactive oxygen species, and opening of mitochondrial permeability transition pores, resulting in the release of mitochondrial factors involved in apoptosis, activation of caspases, and DNA fragmentation. Although originally thought to exhibit specific cytotoxicity against melanoma cells, this agent has been found to be cytotoxic against non-melanoma tumor cell types including neuroectodermal and brain tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
topical calcitriol
A topical formulation containing the hormonally active form of vitamin D3, with potential protective activity against chemotherapy-induced alopecia (CIA). Upon topical application to the scalp, calcitriol may prevent keratinocyte apoptosis in anagen hair follicles. Therefore, this agent may protect against the damaging effects of certain chemotherapeutics to the hair follicles. Check for active clinical trials using this agent. (NCI Thesaurus)
topical celecoxib
A topical cream formulation containing celecoxib, a nonsteroidal anti-inflammatory drug (NSAID), with anti-inflammatory and potential keratolytic, chemopreventive and antineoplastic activities. Upon topical application to the affected area, celecoxib selectively binds to and inhibits cyclooxygenase-2 activity (COX-2), which may result in localized keratinocyte apoptosis. The breakdown of keratinocytes prevents their proliferation locally and may reduce tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
topical cocaine hydrochloride
A topical formulation of the hydrochloride salt of the tropane alkaloid cocaine, with local anesthetic activity. Upon topical application of the cocaine hydrochloride solution to nasal mucous membranes, cocaine reversibly binds to and blocks the voltage-gated sodium channels in the neuronal cell membranes. By stabilizing neuronal membranes, cocaine inhibits the initiation and conduction of nerve impulses and produces a reversible loss of sensation.
topical fluorouracil
A topical formulation containing the antimetabolite 5-fluorouracil (5-FU), with antineoplastic activity. Upon topical administration, 5-FU is converted into the active metabolite 5-fluoroxyuridine monophosphate (F-UMP), which competes with uracil during RNA synthesis and inhibits RNA processing. Conversion of 5-FU into another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase; this results in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in DNA synthesis, and thus inhibits DNA synthesis. Altogether, this prevents the proliferation of tumor cells locally. Check for active clinical trials using this agent. (NCI Thesaurus)
topical gemcitabine hydrochloride
A topical preparation of gemcitabine hydrochloride with antineoplastic activity. Gemcitabine, an analogue of the antimetabolite nucleoside deoxycytidine, is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
topical keratin
A topical formulation containing the naturally-derived biomaterial keratin that has wound repair-promoting, hemostatic, moisturizing and potential radioprotective activities. Upon topical application to an injured site, keratin adheres to the injured tissue, and forms an extracellular matrix that mimics the structure and function of the native tissue. This exogenous extracellular matrix is able to absorb fluid, accelerate thrombus formation through beta1 integrin-mediated platelet adhesion and forms a physical seal on the wound. This facilitates tissue regeneration by promoting cellular proliferation and migration, reducing pro-inflammatory cytokine and chemokine expression and altering the expression of extracellular matrix components and adhesion molecules. Altogether, this promotes wound healing and provides protection from damage due to thermal or radiation exposure. Keratin is an essential component in nails, hair and skin. Check for active clinical trials using this agent. (NCI Thesaurus)
topical menthol
A topical cream containing menthol that both causes a localized cooling sensation and has analgesic activities. Upon topical application, menthol acts on the cold-sensitive transient receptor potential cation channel subfamily M member 8 (TMPR8), which provides a cooling sensation. This treatment also provides an analgesic effect through the activation of the inhibitory group II/III metabotropic glutamate receptors (mGluRs). This may decrease neuropathic pain from chemotherapy. In addition, the topical application of menthol causes vasodilation. Check for active clinical trials using this agent. (NCI Thesaurus)
topical myristyl nicotinate cream
A topical cream containing the ester prodrug myristyl nicotinate (MN), a lipophilic nicotinic acid derivative with potential chemopreventive activity. Upon topical application, myristyl nicotinate penetrates into the epidermis where the agent is cleaved and is converted into nicotinic acid (niacin); nicotinic acid then diffuses into cells where it is converted to nicotinamide adenine dinucleotide (NAD). NAD may stimulate poly(ADP-ribose) polymerase-1 (PARP-1); enhance skin cell turnover and epidermal differentiation; and strengthen skin barrier function. NAD is a coenzyme that plays a crucial role in many redox reactions; PARP-1 is an enzyme that plays an important role in DNA repair. Check for active clinical trials using this agent. (NCI Thesaurus)
topical naloxone hydrochloride
A topical lotion formulation of the dehydrated, hydrochloride salt form of naloxone, an opiate antagonist, with potential anti-pruritic activity. Upon topical application of the naloxone lotion, naloxone binds to and blocks epidermal mu-opiate receptors. This may suppress or diminish pruritus. Check for active clinical trials using this agent. (NCI Thesaurus)
topical phenylephrine solution
A topical solution containing phenylephrine, a sympathomimetic amine with vasoconstricting activity. Upon topical application to the oral mucosa, phenylephrine may activate alpha-adrenergic receptors in the mucosa thereby causing vasoconstriction. As a result, this agent may reduce swelling of the mucosal membranes and decrease radiotherapy-induced mucositis. Check for active clinical trials using this agent. (NCI Thesaurus)
topical piperidine nitroxide MTS-01
A topical gel containing a cell permeable hydrophilic piperidine nitroxide with potential radioprotective and antioxidant activity. As a stable, free radical compound, MTS-01 may be able to protect cells against the damaging effects of reactive oxygen species (ROS), upon exposure to ionizing radiation and oxidative stress. The topically applied MTS-01 may protect normal tissue from radiation-induced toxicity, such as radiation dermatitis, during radiation therapy. Check for active clinical trials using this agent. (NCI Thesaurus)
topical sirolimus
A topical formulation containing the macrolide sirolimus (rapamycin), which is produced by the organism Streptomyces hygroscopicus, with potential anti-proliferative activity. Upon application of topical sirolimus, this agent migrates into the skin and is internalized by the affected cells. In turn, sirolimus binds to the immunophilin FK binding protein-12 (FKBP-12) and forms a sirolimus:FKBP-12 complex. This complex binds to and inhibits the activity of the serine/threonine kinase mammalian target of rapamycin (mTOR). It also decreases the production of vascular endothelial growth factor (VEGF) and results in the suppression of cellular proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
topical VBP-926 solution
A topical solution with potential anti-inflammatory activity. Upon topical application to the affected area, VBP-926 may help reduce paronychia. Iatrogenic paronychia is associated with chemotherapy treatment. Check for active clinical trials using this agent. (NCI Thesaurus)
topical vitamin E
A topical preparation of the fat-soluble vitamin E with potential antioxidant and cytoprotective activities. As a potent antioxidant and radical scavenger, vitamin E ameliorates free-radical damage to cell membranes, thereby protecting cells from reactive oxygen species and maintaining the integrity of cellular macromolecules. In addition, vitamin E noncompetitively inhibits cyclooxygenase (COX) activity in many tissues, which may decrease inflammation. Vitamin E is a generic name for a group of compounds known as tocopherols and tocotrienols (tocols). Check for active clinical trials using this agent. (NCI Thesaurus)
topical wound spray HP802-247
A cell-based combination product consisting of a fibrinogen solution and a cell preparation containing allogeneic non-proliferating, living human skin-derived keratinocytes and fibroblasts, suspended in thrombin, with potential topical wound healing enhancing and topical anti-ulcer activity. Upon sequential spray of the two components of HP802-247 topically, a thin fibrin matrix is formed on the wound surface and the cellular components are capable of secreting wound healing cytokines and growth factors, such as vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), granulocyte-macrophage colony-stimulating growth factor (GM-CSF) and keratinocyte growth factor. Cell concentration and keratinocyte-to-fibroblast ratio in HP802-247 are essential for optimal growth factor production and thus the efficacy of this agent. Check for active clinical trials using this agent. (NCI Thesaurus)
topiramate
A sulfamate-substituted monosaccharide with anticonvulsant activity. Although the mechanism of action has not been fully elucidated, topiramate appears to antagonize kainate/AMPA subtype glutamate receptors, which results in stabilization of hyper-excited neural membranes, inhibition of repetitive neuronal firing, and a decrease in propagation of synaptic impulses, thus impeding seizure activity. In addition, this agent enhances chloride channels activated by the inhibitory neurotransmitter GABA. Kainate/AMPA subtype glutamate receptors are ligand-activated cation channels that mediate the fast component of excitatory postsynaptic currents in neurons of the central nervous system. Check for active clinical trials using this agent. (NCI Thesaurus)
topoisomerase I inhibitor Genz-644282
A non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. Check for active clinical trialsusing this agent. (NCI Thesaurus)
topoisomerase I inhibitor LMP400
An indenoisoquinoline and non-camptothecin inhibitor of topoisomerase I (Top I) with potential antineoplastic activity. Topoisomerase I inhibitor LMP400 binds to the topoisomerase I-DNA covalent cleavage complexes, and inhibits repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. Compared to camptothecins, indenoisoquinolines are chemically stable, produce stable Top I-DNA cleavage complexes, induce unique DNA cleavage sites and appear more resistant to multidrug efflux pumps. Check for active clinical trials using this agent. (NCI Thesaurus)
topoisomerase I inhibitor LMP776
An indenoisoquinoline and non-camptothecin inhibitor of topoisomerase I (Top I) with potential antineoplastic activity. Topoisomerase I inhibitor LMP776 binds to the topoisomerase I-DNA covalent cleavage complexes, and inhibits repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. Compared to camptothecins, indenoisoquinolines are chemically stable, produce stable Top I-DNA cleavage complexes, induce unique DNA cleavage sites and appear more resistant to multidrug efflux pumps. Check for active clinical trials using this agent. (NCI Thesaurus)
topoisomerase I/II inhibitor NEV-801
A multi-targeted agent with potential antineoplastic activity. Upon administration, NEV-801 appears to selectively inhibit topoisomerase (Topo) I and II, and activates hypoxia-inducible factor 1 (HIF-1) transcription and the expression of vascular endothelial growth factor (VEGF) mRNA. NEV-801 is also able to overcome multidrug resistance (MDR) 1-mediated resistance. Check for active clinical trials using this agent. (NCI Thesaurus)
Topoisomerase-1 Inhibitor LMP744
An indenoisoquinoline derivative and topoisomerase 1 (Top1) inhibitor, with potential antineoplastic activity. Upon administration, LMP744 binds to and stabilizes cleaved DNA-Top1 complexes, which prevents DNA re-ligation, induces stable, irreversible DNA strand breaks, prevents DNA repair, and leads to cell cycle arrest and apoptosis. As tumor cells proliferate at a much higher rate than normal cells, LMP744 specifically targets cancer cells. Top1, a DNA modifying enzyme essential for transcription, replication, and repair of double-strand DNA breaks, is overexpressed in tumor cells. Check for active clinical trialsusing this agent. (NCI Thesaurus)
topotecan hydrochloride
The hydrochloride salt of a semisynthetic derivative of camptothecin with antineoplastic activity. During the S phase of the cell cycle, topotecan selectively stabilizes topoisomerase I-DNA covalent complexes, inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when complexes are encountered by the DNA replication machinery. Camptothecin is a cytotoxic quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Check for active clinical trials using this agent. (NCI Thesaurus)
topsalysin
A targeted prodrug consisting of a recombinant modified form of the Aeromonas protoxin proaerolysin (PA), bearing a prostate-specific protease cleavage site, with potential antineoplastic activity. When injected directly into the prostate, topsalysin is hydrolyzed to the active toxin aerolysin by the serine protease prostate specific antigen (PSA), a protein overexpressed by prostate cancers and prostate cells in hyperplastic prostatic tissue. Aaerolysin molecules then oligomerize to form ring-like heptamers that are incorporated into the lipid bilayers of cell membranes, forming large membrane channels and resulting in the leakage of cellular contents and lysis of PSA-expressing prostate cells. Check for active clinical trials using this agent. (NCI Thesaurus)
Toradol
(Other name for: ketorolac tromethamine)
Toraymyxin
(Other name for: polymyxin-B immobilized fiber PMX-20R)
TORC1/2 kinase inhibitor DS-3078a
An orally bioavailable inhibitor of raptor-mTOR protein complex (TORC1) and rictor-mTOR protein complex (TORC2) with potential antineoplastic activity. TORC1/2 inhibitor DS-3078a binds to and inhibits both TORC1 and TORC2 , which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. TORC1 and 2 are upregulated in some tumors and play an important role in the PI3K/Akt/mTOR signaling pathway, which is frequently dysregulated in human cancers. Check for active clinical trials using this agent. (NCI Thesaurus)
toremifene citrate
The citrate salt of a nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which is manifested depending on the tissue or species. Check for active clinical trials using this agent. (NCI Thesaurus)
Torisel
(Other name for: temsirolimus)
TORKi
(Other name for: mTOR kinase inhibitor CC-223)
tosedostat
A proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death. Noxa is a member of the BH3 (Bcl-2 homology 3)-only subgroup of the proapoptotic Bcl-2 (B-cell CLL/lymphoma 2) protein family. Check for active clinical trials using this agent. (NCI Thesaurus)
tositumomab
A murine IgG2 monoclonal antibody directed against the CD20 antigen, found on the surface of B-cells. Tositumomab binds to the CD20 surface membrane antigen, resulting in apoptosis, and may stimulate antitumoral cell-mediated and/or antibody-dependent cytotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)
tositumomab and iodine I 131 tositumomab
A murine IgG2a lambda monoclonal antibody, both unradiolabeled and radiolabeled with iodine I 131, directed against the human B cell-specific surface antigen CD20. Tositumomab binds to CD20, resulting in complement-dependent cytotoxicity (CDC), antibody-dependent cellular cytotoxicity (ADCC), and apoptosis in B cells expressing CD20; in addition to the antibody-mediated cytotoxicity, iodine I 131 tositumomab delivers cytotoxic ionizing radiation specifically to CD20-expressing B cells. In a two-step therapeutic regimen, a predose of unradiolabeled tositumomab is administered first followed by the administration of a dosimetric dose of iodine I 131 tositumomab; 7-14 days later, a therapeutic dose of iodine I 131 tositumomab is administered. The predose of unradiolabeled tositumomab binds to nontumor B cells, increasing the terminal half-life of radiolabeled antibody while protecting nontumor B cells from radiolabeled antibody-mediated radiocytotoxicity. Check for active clinical trials using this agent. (NCI Thesaurus)
total tumor RNA-loaded dendritic cell vaccine
A cancer vaccine containing autologous dendritic cells (DCs) that are loaded with total tumor RNA (TTRNA) from a specific tumor, with potential immunostimulatory and antineoplastic activities. Upon administration, TTRNA-loaded DC vaccine may elicit a highly specific cytotoxic T-cell (CTL) response against the tumor-associated antigens (TAAs) encoded by the TTRNA. Check for active clinical trials using this agent. (NCI Thesaurus)
Totect
(Other name for: dexrazoxane hydrochloride)
Toviaz
(Other name for: fesoterodine fumarate)
tozasertib lactate
The lactate salt of tozasertib, a synthetic, small-molecule Aurora kinase inhibitor with potential antitumor activity. Tozasertib binds to and inhibits Aurora kinases (AKs), thereby inducing apoptosis in tumor cells in which AKs are overexpressed. AKs, a family of serine-threonine kinases, are essential for mitotic progression, spindle formation, centrosome maturation, chromosomal segregation, and cytokinesis. Check for active clinical trials using this agent. (NCI Thesaurus)
TPF regimen
A regimen consisting of docetaxel, cisplatin and fluorouracil used for the treatment of squamous cell head and neck cancer and gastric cancer. (NCI Thesaurus)
T-Phyl
(Other name for: theophylline)
TPI 287
A synthetic, third generation taxane with potential antineoplastic activity. TPI 287 binds to tubulin and stabilizes microtubules, resulting in inhibition of microtubule assembly/disassembly dynamics, cell cycle arrest at the G2/M phase, and apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
TPO receptor agonist ONO-7746
An orally available small molecule and platelet thrombopoietin (TPO) receptor (TPOR; MPL) agonist with potential megakaryopoiesis stimulating activity. Upon administration, TPOR agonist ONO-7746 binds to and stimulates TPOR, which may lead to the proliferation and differentiation of megakaryocytes. In turn, this may increase the production of blood platelets and may prevent chemotherapy induced thrombocytopenia (CIT). TPOR is a cytokine receptor and member of the hematopoietin receptor superfamily.
trabectedin
A tetrahydroisoquinoline alkaloid isolated from the marine tunicate Ecteinascidia turbinate with potential antineoplastic activity. Binding to the minor groove of DNA, trabectedin inteferes with the transcription-coupled nucleotide excision repair machinery to induce lethal DNA strand breaks.and blocks the cell cycle in the G2 phase. Check for active clinical trials using this agent. (NCI Thesaurus)
trabedersen
A transforming growth factor (TGF)-beta2 specific phosphorothioate antisense oligodeoxynucleotide with the sequence 5'-CGGCATGTCTATTTTGTA-3', with potential antineoplastic activity. Trebedersen binds to TGF-beta2 mRNA causing inhibition of protein translation, thereby decreasing TGF-beta2 protein levels; decreasing intratumoral TGF-beta2 levels may result in the inhibition of tumor cell growth and migration, and tumor angiogenesis. TGF-beta2, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
TraceIT
(Other name for: iodinated polyethylene glycol-based hydrogel tissue marker)
TraceIT Hydrogel
(Other name for: iodinated polyethylene glycol-based hydrogel tissue marker)
TraceIT Tissue Marker
(Other name for: iodinated polyethylene glycol-based hydrogel tissue marker)
TRAIL receptor agonist ABBV-621
A fusion protein composed of a tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) receptor agonist consisting of six receptor binding domains (RBDs) of TRAIL fused to the Fc-domain of a human immunoglobulin G1 (IgG1) antibody, with potential pro-apoptotic and antineoplastic activities. Upon administration of TRAIL receptor agonist ABBV-621, this fusion protein binds to TRAIL-receptors, pro-apoptotic death receptors (DRs) TRAIL-R1 (death receptor 4; DR4) and TRAIL-R2 (death receptor 5; DR5), expressed on tumor cells, thereby inducing tumor cell apoptosis. ABBV-621 is designed to maximize receptor clustering for optimal efficacy. TRAIL, a member of the TNF superfamily of cytokines, plays a key role in the induction of apoptosis through TRAIL-mediated death receptor pathways.
trametinib
An orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. Check for active clinical trials using this agent. (NCI Thesaurus)
tranexamic acid
A synthetic derivative of the amino acid lysine with antifibrinolytic activity. With strong affinity for the five lysine-binding sites of plasminogen, transexamic acid competitively inhibits the activation of plasminogen to plasmin, resulting in inhibition of fibrinolysis; at higher concentrations, this agent noncompetitively inhibits plasmin. This agent has a longer half-life, is approximately ten times more potent, and is less toxic than aminocaproic acid, which possesses similar mechanisms of action. Check for active clinical trials using this agent. (NCI Thesaurus)
trans sodium crocetinate
The sodium salt of the trans-isomer of the carotenoid crocetin with potential antihypoxic and radiosensitizing activities. Trans sodium crocetinate (TSC) increases the diffusion rate of oxygen in aqueous solutions such as from plasma to body tissue. The agent has been shown to increase available oxygen during hypoxic and ischemic conditions that may occur in hemorrhage, vascular and neurological disorders, and in the tumor microenvionment. Check for active clinical trials using this agent. (NCI Thesaurus)
transdermal 17beta-estradiol gel BHR-200
A proprietary, transdermal, hydroalcoholic gel formulation containing 17beta-estradiol, with potential antineoplastic activity. Upon topical administration, 17beta-estradiol exerts its antineoplastic effect(s) through as of yet not fully elucidated mechanism(s) of action(s). This formulation may induce feedback inhibition via the hypothalamic–pituitary–gonadal axis feedback loop, block the secretion of luteinizing hormone (LH) and prevent the release of testosterone from Leydig cells in the testes, thus suppressing testosterone secretion. In addition, 17beta-estradiol inhibits enzymes involved in steroidogenesis, thereby further inhibiting androgen production. Since testosterone is required to sustain prostate tumor growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. In addition, 17beta-estradiol prevents bone loss, and suppresses andropause symptoms, such as hot flashes, which appear during androgen-deprivation therapy (ADT) where the standard of care is the use of gonadotropin releasing hormone (GnRH) analogs. Compared to oral estrogens, the topical gel formulation lowers the risk of cardiovascular side effects. Check for active clinical trials using this agent. (NCI Thesaurus)
transdermal 4-hydroxytestosterone
A transdermal formulation containing 4-hydroxytestosterone (4-OHT), a steroidal aromatase inhibitor (AI) and androgen receptor (AR) antagonist, with potential antineoplastic activity. 4-OHT is largely converted into 4-hydroxyandrostenedione (4-OHA) and irreversibly binds to and inhibits aromatase, thereby blocking the conversion of androstenedione to estrone, and testosterone to estradiol. This may inhibit tumor cell proliferation in estrogen-dependent tumor cells. In addition, 4-OHT binds to the AR and may inhibit AR-mediated tumor cell growth. Aromatase, a cytochrome P-450 enzyme, is overexpressed in a variety of cancer cells; it plays a key role in estrogen biosynthesis. Compared to oral 4-OHT, the transdermal formulation allows for continuous release of 4-OHT into the bloodstream and prevents first pass metabolism by the liver. Check for active clinical trials using this agent. (NCI Thesaurus)
transdermal estrogen
A transdermal formulation containing the synthetic form of estradiol, the most potent, endogenously produced estrogen. Upon topical administration, estradiol diffuses through the cell membrane and binds to and activates specific intracellular estrogen receptors located on estrogen-responsive tissues, including the reproductive tract, breast, pituitary, hypothalamus, liver, and bone. The activated ligand-receptor complex binds to estrogen response elements on DNA and promotes the transcription of genes involved in the functioning of the female reproductive system and secondary sex characteristics. In addition, estradiol inhibits the pituitary secretion of the gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism. Check for active clinical trials using this agent. (NCI Thesaurus)
transferrin receptor-targeted anti-RRM2 siRNA CALAA-01
A proprietary transferrin receptor-targeted nanoparticle preparation of a non-chemically modified small-interfering RNA (siRNA) directed against the M2 subunit of ribonucleotide reductase (RRM2) with potential antineoplastic activity. Upon administration, transferrin receptor-targeted anti-RRM2 siRNA CALAA-01 binds to transferrin receptors (TfRs), releasing anti-RRM2 siRNA after endocytosis; anti-RRM2 siRNA silences the expression of RRM2 via the RNAi pathway, impeding the assembly of the holoenzyme ribonucleotide reductase (RR) which catalyzes the production of deoxyribonucleotides. As a result, inhibition of cellular proliferation may occur in cells expressing TfR, a cell surface protein overexpressed on various cancer cell types. Check for active clinical trials using this agent. (NCI Thesaurus)
transferrin receptor-targeted liposomal p53 cDNA
A cationic liposomal, tumor-targeting p53 (TP53) gene delivery system with potential anti-tumor activity. Transferrin receptor-targeted liposomal p53 cDNA contains plasmid DNA encoding the tumor suppressor protein p53 packaged in membrane-like liposome capsules that are complexed with anti-transferrin receptor single-chain antibody (TfRscFv). Upon systemic administration, the anti-TfRscFv selectively binds to tumor cells expressing transferrin receptors. The p53 plasmid is delivered into the nucleus and as a result, p53 protein is produced in tumor cells that have altered p53 function. This results in the restoration of normal cell growth control mechanisms as well as normal response mechanisms to DNA damage. Check for active clinical trials using this agent. (NCI Thesaurus)
transferrin-CRM107
A synthetic targeted protein toxin which consists of human transferrin (Tf) conjugated to a diphtheria toxin that contains a point mutation (CRM107). After binding to the transferrin receptor expressed on the tumor cell surface, transferrin-CRM107 is internalized, where the diphtheria toxin moiety exerts its cytotoxic effect intracellularly by inhibiting protein synthesis through ADP-ribosylation of elongation factor. Check for active clinical trialsusing this agent. (NCI Thesaurus)
transgenic lymphocyte immunization vaccine
A vaccine consisting of a preparation of allogeneic lymphocytes that encode a gene for telomerase. In transgenic lymphocyte immunization, the transgenic cells are infused into the patient, where they serve as antigen- presenting cells (APCs) with the dual function of antigen synthesis and presentation. Vaccination produces an immune response targeting cancer cells expressing telomerase. Check for active clinical trials using this agent. (NCI Thesaurus)
TransMID
(Other name for: transferrin-CRM107)
transthyretin antisense oligonucleotide ISIS-TTR Rx
An antisense oligonucleotide (ASO) targeting transthyretin (TTR), which has potential use in the treatment of TTR amyloidosis (ATTR). Upon subcutaneous administration, TTR ASO ISIS-TTR Rx targets and binds to messenger RNA (mRNA) for both variant and wild-type forms of TTR inside liver cells, thereby inhibiting translation of both mutant and wild-type TTR. Inhibition of TTR protein synthesis lowers TTR blood levels and decreases the amount of and/or prevents TTR amyloid deposits, which accumulate in and cause damage to various body organs and tissues. ATTR is caused by mutations in the TTR gene, which lead to TTR protein misfolding; misfolded wild-type and mutant forms of TTR protein accumulate in tissues as amyloid deposits in most ATTR patients.
tranylcypromine sulfate
The sulfate salt form of tranylcypromine, an orally bioavailable, nonselective, irreversible, non-hydrazine inhibitor of both monoamine oxidase (MAO) and lysine-specific demethylase 1 (LSD1/BHC110), with antidepressant and anxiolytic activities, and potential antineoplastic activities. Upon oral administration, tranylcypromine exerts its antidepressant and anxiolytic effects through the inhibition of MAO, an enzyme that catalyzes the breakdown of the monoamine neurotransmitters serotonin, norepinephrine, epinephrine and dopamine. This increases the concentrations and activity of these neurotransmitters. Tranylcypromine exerts its antineoplastic effect through the inhibition of LSD1. Inhibition of LSD1 prevents the transcription of LSD1 target genes. LSD1, a flavin-dependent monoamine oxidoreductase and a histone demethylase, is upregulated in a variety of cancers and plays a key role in tumor cell proliferation, migration, and invasion. Check for active clinical trials using this agent. (NCI Thesaurus)
TrasGEX
(Other name for: glycooptimized trastuzumab-GEX)
trastuzumab
A recombinant humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2). After binding to HER2 on the tumor cell surface, trastuzumab induces an antibody-dependent cell-mediated cytotoxicity against tumor cells that overexpress HER2. HER2 is overexpressed by many adenocarcinomas, particularly breast adenocarcinomas. Check for active clinical trials using this agent. (NCI Thesaurus)
trastuzumab conjugate BI-CON-02
A conjugated form of trastuzumab, a humanized monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2; ERBB2), with potential immunomodulating and antineoplastic activities. Upon administration, the trastuzumab conjugate BI-CON-02 targets and binds to HER2 on the tumor cell surface, thereby inducing both cytotoxic T-lymphocyte (CTL) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.
trastuzumab duocarmazine
An antibody-drug conjugate (ADC) composed of the recombinant humanized anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab linked, via a cleavable linker, to the duocarmycin prodrug, seco-duocarmycin-hydroxybenzamide-azaindole (seco-DUBA), with potential antineoplastic activity. Upon administration of trastuzumab duocarmazine, the trastuzumab moiety binds to HER2 on the tumor cell surface, which triggers the endocytosis of this agent. The linker is then cleaved inside the tumor cell by proteases at the dipeptide valine-citrulline (vc), and releases the active moiety, duocarmycin. Duocarmycin binds to the minor groove of DNA, alkylates adenine at the N3 position, and induces cell death. In addition, trastuzumab induces antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2 is overexpressed by many carcinomas and is associated with a poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
trastuzumab/tesirine antibody-drug conjugate ADCT-502
An antibody-drug conjugate (ADC) consisting of an engineered version of the humanized monoclonal anti-human epidermal growth factor receptor 2 (HER2) immunoglobulin G1 (IgG1) trastuzumab that is site-specifically conjugated, via a cleavable linker, to the cytotoxic, DNA cross-linking pyrrolobenzodiazepine (PBD) dimer-based drug tesirine, which targets DNA minor grooves, with potential antineoplastic activity. Upon administration, the trastuzumab moiety of trastuzumab/tesirine ADC ADCT-502 targets the cell surface antigen HER2, which is expressed on various cancer cells. Upon antibody/antigen binding, internalization of the ADC and cleavage of the linker, the cytotoxic PBD moiety is released. The imine groups of tesirine bind to the N2 positions of guanines on opposite strands of DNA. This induces interstrand cross-links in the minor groove of DNA, inhibits DNA replication, leads to G2/M cell cycle arrest, induces cell death and inhibits the proliferation of HER2-overexpressing tumor cells. The tumor-associated antigen (TAA) HER2 is expressed by various solid tumors and is associated with a poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
Trasylol
(Other name for: aprotinin bovine)
Traumasept
(Other name for: povidone-iodine solution)
Traumeel S
Diluted extracts isolated from plants and minerals, including belladonna, arnica, St. Johns wort, and Echinacea. As a homeopathic mouth rinse preparation, Traumeel S exhibits antiinflammatory activity; the mechanism of action has not been fully elucidated. This agent may reduce the severity and duration of treatment-related stomatitis. Check for active clinical trials using this agent. (NCI Thesaurus)
Travasol
(Other name for: amino acid injection)
Treanda
(Other name for: bendamustine hydrochloride)
trebananib
An angiopoietin (Ang) 1 and 2 neutralizing peptibody, with potential antiangiogenic activity. Trebananib targets and binds to Ang1 and Ang2, thereby preventing the interaction of the angiopoietins with their target tie2 receptors. 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)
Trelstar Depot
(Other name for: triptorelin pamoate)
tremelimumab
A human immunoglobulin (Ig) G2 monoclonal antibody directed against the human T-cell receptor protein cytotoxic T-lymphocyte-associated protein 4 (CTLA4), with potential immune checkpoint inhibitory and antineoplastic activities. Tremelimumab binds to CTLA4 on activated T-lymphocytes and blocks the binding of the antigen-presenting cell ligands B7-1 (CD80) and B7-2 (CD86) to CTLA4, resulting in inhibition of CTLA4-mediated downregulation of T-cell activation. This promotes the interaction of B7-1 and B7-2 with another T-cell surface receptor protein CD28, and results in a B7-CD28-mediated T-cell activation that is unopposed by CTLA4-mediated inhibition. This leads to a cytotoxic T-lymphocyte (CTL)-mediated immune response against cancer cells. CTLA4, an inhibitory receptor and member of the immunoglobulin superfamily, plays a key role in the downregulation of the immune system. Check for active clinical trials using this agent. (NCI Thesaurus)
Tremfya
(Other name for: guselkumab)
Trental
(Other name for: pentoxifylline)
treosulfan
The prodrug of a bifunctional sulfonate alkylating agent with myeloablative, immunosuppresive, and antineoplastic activities. Under physiological conditions, treosulfan converts nonenzymatically to L-diepoxybutane via a monoepoxide intermediate. The monoepoxide intermediate and L-diepoxybutane alkylate DNA at guanine residues and produce DNA interstrand crosslinks, resulting in DNA fragmentation and apoptosis. In escalated doses, this agent also exhbits myeloablative and immunosuppressive activities. Check for active clinical trials using this agent. (NCI Thesaurus)
tretinoin
A naturally-occurring acid of retinol. Tretinoin binds to and activates retinoic acid receptors (RARs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, and inhibition of tumorigenesis. This agent also inhibits telomerase, resulting in telomere shortening and eventual apoptosis of some tumor cell types. The oral form of tretinoin has teratogenic and embryotoxic properties. Check for active clinical trials using this agent. (NCI Thesaurus)
Trexall
(Other name for: methotrexate)
TriAb
(Other name for: monoclonal antibody 11D10 anti-idiotype vaccine)
triamcinolone
A synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B. Check for active clinical trials using this agent. (NCI Thesaurus)
triamcinolone acetonide
The acetonide salt of triamcinolone, a synthetic glucocorticosteroid with immunosuppressive and anti-inflammatory activities. Triamcinolone binds to specific cytosolic glucocorticoid receptors, which subsequently interact with the glucocorticoid receptor response element on DNA, gene expression is altered so that the synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. Consequently, chronic inflammatory and autoimmune reactions are reduced. Check for active clinical trials using this agent. (NCI Thesaurus)
triapine
A synthetic heterocyclic carboxaldehyde thiosemicarbazone with potential antineoplastic activity. Triapine inhibits the enzyme ribonucleotide reductase, resulting in the inhibition of the conversion of ribonucleoside diphosphates to deoxyribonucleotides necessary for DNA synthesis. This agent has been shown to inhibit tumor growth in vitro. Check for active clinical trials using this agent. (NCI Thesaurus)
triazinate
A synthetic dihydrotriazine derivative with antineoplastic properties. As an antifolate agent related to methotrexate (MTX), triazinate inhibits the enzyme dihydrofolate reductase (DHFR), resulting in decreased tetrahydrofolate production and interference with thymidylate synthesis. Unlike MTX, this agent is not converted to polyglutamate forms. Triazinate also inhibits the transport of folates and may be selectively toxic to MTX-resistant tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
triazine derivative TriN2755
A synthetic triazene derivative with antineoplastic activity. Upon metabolic activation via N-demethylation, TriN2755 is converted into highly reactive carbocations that can alkylate DNA and other macromolecules, thereby resulting in DNA cross links, inhibiting DNA replication and repair, and subsequently inducing apoptosis. This agent has high hydrophilicity and photostability and shows a favorable toxicity profile over the other triazenes. Check for active clinical trials using this agent. (NCI Thesaurus)
tributyrin
A triglyceride prodrug of butyric acid with potential antineoplastic activity. Butyrate, the active metabolite of tributyrin, inhibits histone deacetylase, resulting in increased differentiation, decreased proliferation, cell cycle arrest, and apoptosis in some tumor cell lines. Check for active clinical trials using this agent. (NCI Thesaurus)
triciribine phosphate
The phosphate salt of the synthetic, cell-permeable tricyclic nucleoside triciribine with potential antineoplastic activity. Triciribine inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. Akts are anti-apoptotic serine/theronine-specific protein kinases that phosphorylate and inactivate components of the apoptotic machinery, including Bcl-xL/Bcl-2-associated death promoter (BAD) and caspase 9. Check for active clinical trials using this agent. (NCI Thesaurus)
triclosan/copolymer/fluoride toothpaste
A fluoride-based toothpaste containing the anti-inflammatory and broad-spectrum antibacterial agent triclosan and polyvinylmethyl ether maleic acid copolymer (PVM/MA), with potential antibacterial, anti-inflammatory, and protective activities. Upon application of the triclosan/copolymer/fluoride toothpaste to the teeth, the toothpaste helps remove plaque accumulation. The fluoride protects the teeth against cavities while the triclosan prevents inflammation and may protect against gingivitis and mucositis. The copolymer in the toothpaste enhances the uptake of triclosan by enamel and buccal epithelial cells, thereby prolonging its protective effect and enhancing its activity. Check for active clinical trials using this agent. (NCI Thesaurus)
Tricor
(Other name for: fenofibrate)
trientine hydrochloride
The hydrochloride salt form of a metal chelating agent with potential anti-angiogenic activity. Trientine chelates excess copper (Cu) ions in the body; the excess copper is subsequently removed from the body through the kidneys. As Cu is an essential cofactor for cuproenzymes, such as superoxide dismutase 1 (SOD1), depletion of copper may inhibit the activation of signal transduction pathways required for cellular proliferation and angiogenesis. In addition, trientine may inhibit copper-induced secretion of interleukin-8 (IL-8). Check for active clinical trials using this agent. (NCI Thesaurus)
trifluoperazine hydrochloride
The hydrochloride salt of trifluoperazine, a phenothiazine derivative and a dopamine, alpha-adrenergic, and anticholinergic antagonist with antipsychotic, anxiolytic, and antiemetic activities. Trifluoperazine blocks central dopamine receptors, which may prevent or mitigate delusions and hallucinations caused by an excess of dopamine; dopamine blockade in the chemoreceptor trigger zone (CTZ) may result in an antiemetic effect. This agent binds to central adrenergic receptors, which may result in anxiolytic effects.Trifluoperazine also functions as a calmodulin inhibitor, elevating cytosolic calcium. Check for active clinical trials using this agent. (NCI Thesaurus)
trifluridine
A fluorinated thymidine analog with potential antineoplastic activity. Trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. This agent also exhibits antiviral activity. Check for active clinical trials using this agent. (NCI Thesaurus)
trifluridine and tipiracil hydrochloride
An orally bioavailable combination agent composed of the cytotoxic pyrimidine analog trifluridine (5-trifluoro-2’-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor (TPI) tipiracil hydrochloride, in a molar ratio of 1.0:0.5 (TFT:TPI), with potential antineoplastic activity. After oral administration of trifluridine and tipiracil hydrochloride, TFT is phosphorylated to the active monophosphate form TF-TMP, which binds covalently to the active site of thymidylate synthase, thereby reducing the nucleotide pool levels required for DNA replication. Furthermore, the triphosphate form TF-TTP can be incorporated into DNA, which induces DNA fragmentation and leads to the inhibition of tumor growth. TPI exhibits a dual effect: 1) an anti-angiogenic effect mediated through the inhibition of thymidine phosphorylase, which plays an important role in nucleotide metabolism and a variety of development processes, including angiogenesis, 2) increased bioavailability of the normally short-lived antimetabolite TFT by preventing its degradation into the inactive form trifluorothymine (TF-Thy). The synergistic effect of the components in TAS-10 may demonstrate antitumor activity in 5-FU-resistant cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)
trigriluzole
A formulation comprised of a prodrug form of the benzothiazole derivative riluzole, with potential anti-depressant, anxiolytic and antineoplastic activities. Following oral administration, trigriluzole is converted into the active form riluzole. While the mechanism of action of riluzole is unknown, its pharmacological activities, some of which may be related to its effect, include the following: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) interference with intracellular events that follow transmitter binding at excitatory amino acid receptors. These activities may result in myorelaxation and sedation due to the blockade of glutamatergic neurotransmission. Additionally, these activities may result in the inhibition of enzymes that are necessary for cell growth, which may decrease tumor cell growth and metastasis. Check for active clinical trials using this agent. (NCI Thesaurus)
Trileptal
(Other name for: oxcarbazepine)
Trilisate
(Other name for: choline magnesium trisalicylate)
trilostane
A synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex, resulting in the decreased synthesis of mineralocorticoids and glucocorticoids and the decreased conversion of pregnenolone to progesterone. Check for active clinical trialsusing this agent. (NCI Thesaurus)
trimeric GITRL-Fc OMP-336B11
A Fc-engineered human fusion protein composed of two trimers of tumor necrosis factor (ligand) superfamily, member 18 (TNFSF18; GlTRL) linked to an immunoglobulin Fc domain (GITRL-Fc), with potential immunostimulatory and antineoplastic activities. Upon administration, trimeric GITRL-Fc OMP-336B11 targets, binds to and activates its co-stimulatory surface receptor (glucocorticoid-induced tumor necrosis factor receptor (GITR; TNFRSF18) expressed on T lymphocytes and certain tumor cell types. This activates T lymphocytes, causes T-lymphocyte proliferation and suppresses the activity of regulatory T cells (Treg). This promotes cytotoxic T-lymphocyte (CTL)-mediated killing of tumor cells. GITRL, a member of the tumor necrosis factor (TNF) family of ligands, functions to activate the co-stimulatory receptor GITR to enhance T-cell-modulated immune responses. Check for active clinical trials using this agent. (NCI Thesaurus)
trimethoprim-sulfamethoxazole
A synthetic combination of two antibacterial agents, trimethoprim and sulfamethoxazole. This synergistic combination, also known as co-trimoxazole, inhibits two sequential steps in the bacterial metabolism of folic acid. Trimethoprim is a pyrimidine inhibitor of dihydrofolate reductase; sulfamethoxazole is a sulfamide inhibitor of bacterial dihydrofolate synthetase. Check for active clinical trials using this agent. (NCI Thesaurus)
trimethylcolchicinic acid
A colchicine analog with potential antineoplastic activity. Trimethylcolchicinic acid binds to tubulin, inhibiting its polymerization into microtubules and preventing cell division. Check for active clinical trials using this agent. (NCI Thesaurus)
trimetrexate glucuronate
A lipid soluble methotrexate derivative with potential antineoplastic activity. Trimetrexate glucuronate inhibits the enzyme dihydrofolate reductase, thereby preventing the synthesis of purine nucleotides and thymidylate, with subsequent inhibition of DNA and RNA synthesis. Trimetrexate glucuronate also exhibits antiviral activity. Check for active clinical trials using this agent. (NCI Thesaurus)
Trimox
(Other name for: amoxicillin)
Triostat
(Other name for: liothyronine sodium)
Tripedia
(Other name for: diphtheria toxoid/tetanus toxoid/acellular pertussis vaccine adsorbed)
triptolide analogue
A water soluble analogue of the diterpenoid triepoxide triptolide isolated from the Chinese herb Tripterygium wilfordii Hook F with potential antineoplastic activity. Upon intravenous administration, the triptolide analogue inhibits heat shock protein 70 (HSP70) and prevents HSP70-mediated inhibition of apoptosis. This leads to both the induction of apoptosis and a reduction of cancer cell growth. HSP70, a molecular chaperone upregulated in various cancer cells, plays a key role in the inhibition of caspase-dependent and -independent apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
triptorelin
A synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men. Check for active clinical trials using this agent. (NCI Thesaurus)
triptorelin pamoate
The pamoate salt of triptorelin, a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion after prolonged administration. After chronic, continuous administration, a sustained decrease in LH, FSH and testicular and ovarian steroidogenesis is observed. The serum testosterone concentration may fall to levels typically seen in surgically castrated men. Check for active clinical trials using this agent. (NCI Thesaurus)
tris-acryl gelatin microspheres
An embolic particle composed of water-soluble, compressible, nonabsorbable tris-acryl gelatin microspheres, with potential use for embolization. Upon administration, the tris-acryl gelatin microspheres (TAGM) serve as an embolic agent before surgery for highly vascularized areas, such as those seen in certain tumors, by penetrating into the vascular system and blocking blood flow. These microspheres may be used to encapsulate various therapeutic agents; drug-loaded microspheres can then be used as drug delivery vehicles during embolization of tumor vasculature. Check for active clinical trials using this agent. (NCI Thesaurus)
Trisenox
(Other name for: arsenic trioxide)
trivalent influenza vaccine
A synthetic vaccine consisting of three inactivated influenza viruses, two different influenza type A strains and one influenza type B strain. Trivalent influenza vaccine is formulated annually, based on influenza strains projected to be prevalent in the upcoming flu season. This agent may be formulated for injection or intranasal administration. Check for active clinical trials using this agent. (NCI Thesaurus)
trivalent live-attenuated influenza vaccine
A weakened live virus vaccine containing three seasonal influenza reassortants with prophylactic activity against influenza subtypes A and B. The trivalent live-attenuated influenza vaccine (LAIV) contains 2 strains of the influenza subtype A, one for H1N1 and one for H3N2, and one strain of subtype B. Upon intranasal administration by sprayer of the trivalent LAIV, the live viruses replicate in the upper respiratory tract and induce an immune response leading to active immunization against influenza subtypes A and B. Check for active clinical trials using this agent. (NCI Thesaurus)
tri-virus/GD2-specific allogeneic cytotoxic T-lymphocytes
Allogeneic tri-viral specific, Epstein-Barr virus (EBV), cytomegalovirus (CMV) and adenovirus (Ad), cytotoxic T-lymphocytes (tV-CTLs) expressing a chimeric antigen receptor (CAR) specific for disialoganglioside GD2 with potential antineoplastic activity. Tri-virus/GD2-specific allogeneic CTLs are produced by transducing tV-CTLs with a GD2-specific CAR retroviral vector. Upon administration, after an allogeneic hematopoietic stem cell transplant, these CTLs may be selective towards EBV, CMV, and Ad-infected cells and GD2-expressing tumor cells. The human glycosphingolipid GD2 is a tumor associated antigen overexpressed on the surface of all tumors of neuroectodermal origin. Check for active clinical trials using this agent. (NCI Thesaurus)
Trivora
(Other name for: ethinyl estradiol/levonorgestrel)
TRK inhibitor LOXO-195
An orally bioavailable, selective tropomyosin-related-kinase (tyrosine receptor kinase; TRK) inhibitor, with potential antineoplastic activity. Upon oral administration, LOXO-195 specifically targets and binds to TRK, including the fusion proteins containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1), 2 (NTRK2), and 3 (NTRK3). This prevents neurotrophin-TRK interaction and TRK activation, which results in both the induction of cellular apoptosis and the inhibition of cell growth in tumors that overexpress TRK and/or express NTRK fusion proteins. LOXO-195 targets specific point mutations that occur after treatment with and result in acquired resistance to another TRK inhibitor; therefore, LOXO-195 is able to overcome acquired resistance to other TRK inhibitors. TRK, a family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded by NTRK family genes. The expression of either mutated forms of or fusion proteins involving NTRK family members results in uncontrolled TRK signaling and plays an important role in tumor cell growth and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
trodusquemine
A naturally-occurring cholestane and non-competitive, allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B), with potential hypoglycemic, anti-diabetic, anti-obesity, and antineoplastic activities. Upon administration, trodusquemine selectively targets and inhibits PTP1B, thereby preventing PTP1B-mediated signaling. This prevents the dephosphorylation of the insulin receptor, which improves insulin signaling and insulin sensitivity, and decreases blood glucose levels. In susceptible cancer cells, inhibition of PTP1B causes a reduction of tumor cell proliferation. In addition, as trodusquemine can cross the blood-brain barrier (BBB), it centrally suppresses appetite and causes weight loss. PTP1B, a tyrosine phosphatase, is elevated in certain cancer cells; it is specifically upregulated in human epidermal growth factor receptor 2 (HER2)-driven cancers where it promotes cell growth, and is correlated with a poor prognosis and increased metastatic potential. In diabetes, PTP1B upregulation plays a major role in insulin resistance.
trofosfamide
An orally bioavailable oxazaphosphorine prodrug with antineoplastic activity. Trofosfamide (TFF) is metabolized predominantly to the cyclophosphamide analogue ifosfamide (IFO), which is then metabolized by liver cytochrome P450s to the active isophosphoramide mustard (IPM). IPM alkylates DNA to form DNA-DNA cross-links, which may result in inhibition of DNA, RNA and protein synthesis, and tumor cell apoptosis. Check for active clinical trials using this agent. (NCI Thesaurus)
troglitazone
An orally-active thiazolidinedione with antidiabetic and hepatotoxic properties and potential antineoplastic activity. Troglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-gamma), a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation. Check for active clinical trials using this agent. (NCI Thesaurus)
tropisetron
An indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, tropisetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy-and radiotherapy-induced nausea and vomiting. Check for active clinical trials using this agent. (NCI Thesaurus)
tropisetron hydrochloride
The hydrochloride salt form of tropisetron, a selective, competitive serotonin 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist, with antinauseant and antiemetic activities. Tropisetron competitively binds to and blocks the action of serotonin at 5HT3 receptors peripherally on vagus nerve terminals located in the gastrointestinal (GI) tract as well as centrally in the chemoreceptor trigger zone (CTZ) of the area postrema of the central nervous system (CNS). This results in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting. Check for active clinical trials using this agent. (NCI Thesaurus)
tropomysin receptor kinase inhibitor AZD7451
A tropomyosin receptor kinase (TRK) inhibitor with potential antineoplastic activity. AZD7451 binds to TRK, thereby preventing the neurotrophin-TRK interaction and subsequent TRK activation. This may eventually result in an inhibition of tumor cell proliferation in TRK-expressing tumor cells. TRK, a receptor tyrosine kinase activated by neurotrophins, is mutated in a variety of cancer cell types and plays an important role in tumor cell growth, invasion and survival.
TroVax
(Other name for: recombinant modified vaccinia Ankara-5T4 vaccine)
troxacitabine
A dioxolane derivative and a novel L-configuration deoxycytidine analogue with potent antineoplastic activity. When incorporated into growing chain during DNA replication, troxacitabine stops DNA polymerization due to its unnatural L-configuration, in contrast to the normal nucleotides with D-configuration. As a result, this agent terminates DNA synthesis upon incorporated into DNA molecules, and consequently interrupts tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)
Troxatyl
(Other name for: troxacitabine)
TRP2 mRNA-electroporated autologous langerhans-type dendritic cell vaccine
A cancer cell vaccine composed of autologous human Langerhans-type dendritic cells (also known as Langerhans cells or LCs) that are electroporated with mRNA encoding full-length murine tyrosinase-related peptide 2 (TRP2), with potential antineoplastic and immunomodulating activities. Upon vaccination, the TRP2 mRNA-electroporated autologous Langerhans-type dendritic cell vaccine may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against TRP2-expressing tumor cells. TRP2, a tautomerase involved in the synthesis of melanin, is only expressed in melanomas, melanocytes, and the retina. The LCs are differentiated from CD34 positive hematopoietic progenitor cells. Check for active clinical trials using this agent. (NCI Thesaurus)
TRPV6 calcium channel inhibitor SOR-C13
An inhibitor of transient receptor potential cation channel vanilloid family member 6 (TRPV6, CaT1 or CATL) with potential antineoplastic activity. TRPV6 calcium channel inhibitor SOR-C13 binds to TRPV6 and prevents the influx of calcium ions into TRPV6-expressing tumor cells. This inhibits the activation of nuclear factor of activated T-cell (NFAT) transcription complex which may result in an inhibition of calcium-dependent cancer cell proliferation and an induction of apoptosis in tumor cells overexpressing TRPV6. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly selective for calcium compared to other cations; it is overexpressed in a variety of tumors and initiates tumor cell growth, proliferation and metastases. Check for active clinical trials using this agent. (NCI Thesaurus)
truncated tissue factor/NGR peptide
A vascular-targeting agent composed of the extracellular domain of the trunctated form of issue factor (tTF) conjugated to the C-terminal peptide GNGRAHA (NGR), with potential procoagulatory and antineoplastic activities. Upon administration, the NGR peptide moiety of tTF-NGR targets and binds to the surface protein aminopeptidase N (CD13) expressed on endothelial cells in tumor vessels. Upon deamidation of the NGR peptide moiety, this agent also binds to integrin alphaVbeta3 (aVb3; CD51/CD61) in the tumor vasculature. In turn, the tTF causes occlusion of the tumor blood vessels, which causes an inhibition of blood supply and flow in the tumor, nutrition and induced tumor cell death and an inhibition of tumor cell proliferation. TF plays a key role in the coagulation cascade. NGR is a asparagine-glycine-arginine containing peptide and ligand of CD13. Both aVb3 and CD13 are surface proteins that are upregulated on endothelial cells of tumor vessels. Check for active clinical trials using this agent. (NCI Thesaurus)
Truphylline
(Other name for: aminophylline)
tryptophanase
Encoded by human TDO2 Gene, 406-aa 48-kDa Tryptophanase is a homotetramer that may bind protoheme IV involved in tryptophan catabolism with broad specificity towards tryptamine and derivatives including tryptophan, 5-hydroxytryptophan, and serotonin. Check for active clinical trials using this agent. (NCI Thesaurus)

1 comentario:

  1. Thymopentin, also known as TP-5, is a synthetic derivative of thymopoietin, a thymic hormone, and has immunoregulatory properties. Thymopentin interacts with T cells, reduces endocrine and behavioral responses to experimental stress. Thymopentin Acetate

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