(Other name for: theophylline)
A human IgG4 monoclonal antibody against B-cell activating factor (BAFF), with potential immunomodulating and antineoplastic activities. Tabalumab binds to and inhibits the activity of both soluble and cell surface-bound BAFF. This may reduce the activity, proliferation and survival of B-cells. A dysregulated expression of BAFF, a member of the tumor necrosis factor (TNF) family of proteins, is often seen in certain autoimmune diseases and certain cancers, and may promote B lymphocyte activation, proliferation and survival.
(Other name for: thioguanine)
Tabloid brand thioguanine
(Other name for: thioguanine)
An orally bioavailable substituted benzamide derivative with potential antineoplastic activity. Tacedinaline inhibits histone deacetylation, which may result in histone hyperacetylation, followed by the induction of differentiation, the inhibition of cell proliferation, and apoptosis in susceptible tumor cell populations.
(Other name for: cimetidine)
An orally bioavailable, small-molecule, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential immunomodulating, anti-inflammatory, and antineoplastic activities. Talmapimod specifically binds to and inhibits the phosphorylation of p38 MAPK, which may result in the induction of tumor cell apoptosis, the inhibition of tumor cell proliferation, and the inhibition of tumor angiogenesis. This agent may also enhance proteasome inhibitor-induced apoptosis. p38 MAPK is a serine/threonine protein kinase involved in a MAPK signaling cascade that controls cellular responses to various environmental stresses, cytokines, and endotoxins.
An oncolytic, recombinant herpes simplex type-1 virus (HSV) encoding thuman cytokine granulocyte-macrophage colony stimulating factor (GM-CSF) with potential immunostimulating and antineoplastic activities. Upon administration, talminogene laherparepvec selectively infects and replicates in tumor cells, thereby inducing tumor cell lysis. In addition, expressed GM-CSF may stimulate a cytotoxic T cell response against tumor cells, resulting in immune-mediated tumor cell death in addition to HSV-mediated oncolytic tumor cell death.
The ammonium salt of an antimetabolite analogue of aminopterin with potential antineoplastic activity. As a folate antagonist, talotrexin binds to and inhibits the function of dihydrofolate reductase, resulting in the inhibition of folate metabolism, DNA synthesis, and cell division. Hydrosoluble, talotrexin is actively transported into cells by the reduced folate carrier (RFC) and, therefore, is unlikely to be associated with P-glycoprotein-mediated multidrug resistance.
The hydrate of tatirelin, a thyrotropin releasing hormone (TRH) analogue with potential neuroprotective, analgesic and central nervous system-stimulating (CNS)/analeptic activities. Taltirelin mimics the physiological actions of TRH on the CNS while exerting a minimal effect on the release of thyrotrophin (TSH) from the anterior lobe of the pituitary. Like TRH, the mechanism of action of this agent in the CNS has not been fully elucidated mechanism, but may involve various cerebral monoamine pathways. Compared to TRH, taltirelin has a much longer half-life and duration of effects.
(Other name for: talotrexin ammonium)
An orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity. As a specific retinoic acid receptor (RAR) alpha/beta agonist, tamibarotene is approximately ten times more potent than ATRA in inducing cell differentiation and apoptosis in HL-60 (human promyelocytic leukemia) cell lines in vitro. Due to a lower affinity for cellular retinoic acid binding protein (CRABP), tamibarotene may show sustained plasma levels compared to ATRA.
In addition, this agent may exhibit a lower toxicity profile than ATRA, in part, due to the lack of affinity for the RAR-gamma receptor, the major retinoic acid receptor in the dermal epithelium.
A humanized monoclonal antibody directed against nerve growth factor (NGF), a modulator of nociceptor function, with potential analgesic activity. Tanezumab binds to NGF and prevents NGF binding to its high affinity, membrane-bound, catalytic receptor tropomyosin-related kinase A (TrkA), which is present on sympathetic and sensory neurons; reduced stimulation of TrkA by NGF inhibits the pain-transmission activities of these neurons. NGF, a neurotrophin, is critical to the growth and maintenance of sympathetic and sensory neurons. In addition, NGF may induce mast cells to release inflammatory proteins and may induce the upregulation of substance P and other pain-related peptides in sympathetic and sensory neurons. Upon neurotrophin binding, TrkA phosphorylates itself and members of the MAPK pathway, mediating the multiple neuronal effects of NGF.
A biphenyl matrix metalloproteinase (MMP) inhibitor (MMPI) with potential antineoplastic activity. Tanomastat inhibits MMP-2, MMP-3, and MMP-9, inhibiting extracellular matrix degradation and potentially inhibiting angiogenesis, tumor growth and invasion, and metastasis. MMPs consist of at least 18 zinc-containing endo-proteinases that are capable of degrading collagen and proteoglycan.
tapentadol hydrochloride ER
An orally active, extended-release preparation of the hydrochloride salt of tapentadol with analgesic activity. Tapentadol is a synthetic, centrally acting analgesic with a dual mechanism of action involving mu-opioid receptor agonism and norepinephrine reuptake inhibition. This agent may be effective in the management of pain, cancer-related and other.
(Other name for: cytarabine)
An orally active synthetic enantiomer of flurbiprofen. Tarenflurbil activates c-Jun N terminal kinase, increases AP-1 binding to DNA, and downregulates cyclin D1 expression, resulting in arrest of tumor cells in the G1 phase of the cell cycle and apoptosis. This agent also affects the expression of nuclear factor kappa B, a rapid response transcription factor that stimulates the immune response to tumor cells. Tarenflurbil does not inhibit the enzyme cyclo-oxygenase.
(Other name for: teicoplanin)
TARP 27-35 peptide vaccine
A peptide-based cancer vaccine, containing amino acid residues 27 through 35 of T cell receptor gamma alternate reading frame protein (TARP), with potential immunostimulatory and antineoplastic activities. Upon administration, TARP 27-35 peptide vaccine may stimulate a host cytotoxic T-cell (CTL) response against TARP-expressing tumor cells, resulting in tumor cell cytotoxicity. The nuclear protein TARP is commonly expressed on prostate and breast cancer cells and is highly immunogenic.
TARP 29-37-9V peptide vaccine
A peptide-based cancer vaccine, consisting of amino acid residues 29 through 37 of T cell receptor gamma alternate reading frame protein (TARP) with a leucine-to-valine substitution at position 9, with potential immunostimulatory and antineoplastic activities. Upon administration, TARP 29-37-9V peptide vaccine may induce a cytotoxic T-lymphocyte (CTL) response against TARP-expressing tumor cells, which may result in decreased tumor cell proliferation. The leucine-to-valine substitution at position 9 of this peptide improves its immunogenicity. The nuclear protein TARP is commonly expressed on prostate and breast cancer cells and is highly immunogenic.
(Other name for: bavituximab)
A synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues. In addition, TAS-108 activates the co-repressor Silencing Mediator for Retinoid and Thyroid hormone receptor (SMRT), a protein that inhibits the activities of the estrogen receptors, which may contribute to the antitumor activity of TAS-108.
The sodium salt form of tasisulam, an acyl-sulfonamide compound with potential antiproliferative activity. Tasisulam activates, through an as of yet not fully elucidated mechanism, the intrinsic mitochondrial-mediated cell death pathway as manifested by decreased adenosine triphosphate (ATP), cytochrome C release, activation of caspases, loss of mitochondrial membrane potential, production of reactive oxygen species (ROS) and eventually apoptosis.
A quinoline-3-carboxamide linomide analogue with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.
(Other name for: dimesna)
taxol analogue SID 530
An intravenous formulation containing docetaxel, a semi-synthetic, second-generation taxane derived from a compound found in the European yew tree, Taxus baccata, with potential antineoplastic activity. Taxol analogue SID 530 binds to and stabilizes tubulin, inhibiting microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death.
(Other name for: DHA-paclitaxel)
(Other name for: ceftazidime sodium)
Tc 99m sestamibi
Sestamibi is a large synthetic molecule of the isonitrile family, which can be labeled with Tc99m. It passes through cells membranes passively, collecting in cells with large numbers of mitochondria. It is often used for imaging of the thyroid and parathyroid.
(Other name for: technetium Tc 99m methylene diphosphonate)
technetium Tc 99m DTPA
A radiopharmaceutical core of chelating agent DTPA (diethylenetriaminepentaacetic acid) complexed with the gamma-emitting radionuclide technetium Tc 99m with radioimaging application. Tc-99m-DTPA has been utilized as a radiotracer, when conjugated to tissue specific molecules, in a wide variety of nuclear imaging studies, including brain, lung, and renal function studies.
technetium Tc 99m ethylenedicysteine-deoxyglucose
A radiopharmaceutical consisting of ethylenedicysteine-deoxyglucose (EC-DG) labeled with the metastable radioisotope technetium Tc-99 (99mTc). Upon administration, technetium Tc 99m ethylenedicysteine-deoxyglucose accumulates in cells with increased metabolic activity such as proliferating tumor cells; tumor tissue may then be imaged using gamma scintigraphy.
technetium Tc 99m galactosyl human serum albumin
A colloid formulation of human galactosyl serum albumin (GSA) conjugated to the chelating agent diethylene-triaminepentaacetic acid (DTPA) and complexed to the gamma-emitting isotope technetium-99m (99mTc-GSA) with potential diagnostic imaging activity. Upon intravenous administration, the galactosyl moiety of 99mTc-GSA binds to asialoglycoprotein receptors (ASGPR) located on hepatic cells. Upon SPECT (Single Photon Emission Computed Tomography) imaging, liver function can be assessed. The expression of ASGPR, which are solely found on the plasma membrane of mammalian hepatocytes, is associated with hepatic function.
technetium Tc 99m glycopeptide
A technetium Tc 99m radiopharmaceutical of a glutamate-rich peptide (GP) conjugated, via carbodiimide linker, to the heparin-like polysaccharide chitosan (CH) in a 1:1 ratio, with potential tumor targeting property. Upon administration, 99m Tc-glycopeptide targets and is taken up by glutamate-specific transporters on tumor cells. Upon internalization, the Tc99m moiety can be visualized upon scanning. GP may potentially be used as a drug carrier for antineoplastic drug delivery to tumor cells.
Technetium Tc 99m human serum albumin colloid
A colloid formulation of human serum albumin (HSA) labeled with Technetium-99m (Tc-99m) with diagnostic imaging properties. This HSA radioconjugate contains the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. A potential advantage of the Tc-99m-HSA suspension is its smaller colloid particle size as compared to formulations containing either sulfur or tin, thereby allowing for enhanced imaging of the lymphatic draining pattern during lymphoscintigraphic or sentinel lymph node mapping procedures.
technetium Tc 99m hydroxydiphosphonate
A radioconjugate containing hydroxydiphosphonate (HDP) labeled with the metastable radioisotope technetium Tc (99mTc), with radioimaging activity. Upon intravenous administration, skeletal uptake of technetium Tc-99m HDP occurs as a function of skeletal blood flow and osteogenic activity. HDP has a specific affinity for hydroxyapatite crystals in bone where abnormal accumulation of increased osteoid mineralization has occurred. Labeling of HDP with 99mTc allows gamma scintigraphic imaging of areas of abnormal osteogenesis associated with malignant bone lesions.
technetium Tc 99m mebrofenin
A radioconjugate composed of the iminodiacetic acid derivative mebrofenin bound to an isotope of the synthetic element technetium (Tc). Upon administration and rapid clearance form the circulation, technetium Tc 99m mebrofenin is secreted into the hepatobiliary system, emitting gamma rays that are detectable with planar scintigraphy or single photon emission computer tomography (SPECT). Mebrofenin has no pharmacological effect at the recommended dosage for diagnostic imagining.
technetium Tc 99m methylene diphosphonate
A radiopharmaceutical containing methylene diphosphonate (medronate; MDP) complexed with the gamma-emitting radionuclide technetium Tc 99m with radioisotopic activity and hydroxyapatite affinity. Upon intravenous administration, skeletal uptake of technetium Tc 99m methylene diphosphonate occurs as a function of skeletal blood flow and osteogenic activity. The MDP moiety of this agent has affinity for hydroxyapatite crystals in bone with abnormal accumulation at sites with increased osteoid mineralization; labeling of MDP with Tc 99m allows scinitgraphic imaging of areas of abnormal osteogenesis associated with malignant bone lesions.
technetium Tc 99m-labeled albumin microspheres
An injectable radiopharmaceutical formulation containing human serum albumin (HSA) microspheres labeled with technetium-99m (Tc-99m) with diagnostic imaging activity. Technetium Tc 99m-labeled albumin microspheres contain the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. Upon injection into the hepatic artery, the radionuclide portion allows for SPECT (single photon emission computed tomography) imaging of distribution patterns of the albumin microspheres. This may possibly predict the distribution of other agents with similar particle sizes within the liver and may give a prediction of the tumor response upon administration of such agents.
technetium Tc 99m-labeled macroaggregated albumin
An injectable radiopharmaceutical formulation containing human serum albumin (HSA) labeled with technetium-99m (Tc99m) in macroaggregates (MAA) with diagnostic imaging activity. Technetium Tc 99m-labeled macroaggregated albumin contains the gamma-emitting Tc99m, a metastable nuclide of molybdenum-99. Upon injection into the hepatic artery and upon SPECT (single photon emission computed tomography) imaging, distribution patterns and possible prediction of expected distribution of agents with similar particle sizes within the liver can be assessed and may give a prediction about the tumor response upon administration of such agents.
technetium Tc 99m-NC100692
A synthetic Arg-Gly-Asp (RGD)-containing cyclic peptide radiolabeled with technetium Tc 99m with integrin-binding and radioisotopic activities. Upon administration, technetium Tc 99m-NC100692 binds to alpha5beta3 integrin and to a lesser extent alpha5beta5; subsequently, alpha5beta3-expressing tumor cells can be visualized using scintigraphy and the degree of tumor angiogenesis can be determined. Integrins, membrane-spanning protein receptors, may be upregulated on proliferating endothelial cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells and poor prognosis.
A sulfated polysaccharide isolated from various Arthrobacter bacterial species. Possessing potential antiangiogenic and antineoplastic properties, tecogalan binds to basic fibroblast growth factor (bFGF), thereby preventing bFGF from binding to its receptors. Disruption of this receptor binding results in the inhibition of bFGF-stimulated endothelial cell growth, proliferation, and migration.
(Other name for: tetrodotoxin)
An orally bioavailable fluoropyrimidine antagonist composed of tegafur combined with two modulators of 5-flurouracil (5-FU) activity, 5-chloro-2,4-dihydroxypyridine (CDHP) and potassium oxonate, in a molar ratio of 1:0.4:1. Tegafur is a prodrug of 5-fluorouracil, an antimetabolite that inhibits thymidylate synthase, DNA synthesis and cell division, and competes with uridine triphosphate, thus inhibiting RNA and protein synthesis. CDHP is a reversible inhibitor of dihydropyrimidine dehydrogenase (DPD), the liver enzyme responsible for rapid catabolism of 5-FU into inactive metabolites. Potassium oxonate preferentially localizes in the gut and inhibits the enzyme orotate phosphoribosyl-transferase (OPRT), thereby decreasing activation of 5-FU in the gut and activated 5-FU-related gastrointestinal toxicity.
A water-soluble prodrug of a cyanoguanidine compound with potential antineoplastic activity. In vivo, teglarinad chloride is rapidly converted into active drug through hydrolytic cleavage of a carbonate ester bond. Although the exact mechanism of action has yet to be fully elucidated, the active drug appears to antagonize nuclear factor-kappa B (NF-kB) transcription, resulting in the induction of tumor cell apoptosis.
(Other name for: carbamazepine)
The orally bioavailable mesylate salt of the 17-allylaminogeldanamycin (17-AAG) small-molecule inhibitor of several receptor protein tyrosine kinases with potential antiangiogenic and antineoplastic activities. Telatinib binds to and inhibits the vascular endothelial growth factor receptors (VEGFRs) type 2 and 3, platelet-derived growth factor receptor beta (PDGFRb) and c-Kit, which may result in the inhibition of angiogenesis and cellular proliferation in tumors in which these receptors are upregulated.
These telatinib-inhibited receptor protein tyrosine kinases are overexpressed or mutated in many tumor cell types and may play key roles in tumor angiogenesis and tumor cell proliferation. 17-AAG is a synthetic analogue of the benzoquinone ansamycin antibiotic geldanamycin and has also been found to inhibit the molecular chaperone Hsp90.
The hydrochloride salt form of telavancin, a lipoglycopeptide and a semisynthetic derivative of vancomycin with antibacterial activity against gram-positive bacteria. Like vancomycin, telavancin binds tightly to the D-alanyl-D-alanine residue of cell wall precursors, thereby interfering with bacterial cell wall synthesis. In addition, the lipophilic moiety of telavancin may interact with the lipid bilayer in the bacterial cell membrane, thereby compromising the integrity of cell membrane and causing cell membrane depolarization. This novel mechanism of action may contribute to telavancin's rapid bactericidal activity and its improved activity over vancomycin against some antibiotic resistance gram-positive bacteria.
A synthetic thymidine nucleoside analogue with antiviral activity highly specific for the treatment of hepatitis B virus (HBV). Intracellularly, telbivudine is phosphorylated to its active metabolite, telbivudine triphosphate. The dideoxy telbivudine triphosphate competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). This results in the blockade of HBV DNA replication and viral propagation.
(Other name for: ezatiostat hydrochloride)
telomerase peptide vaccine GV1001
A synthetic peptide vaccine containing a 16-amino-acid human telomerase reverse transcriptase peptide(hTERT: 611-626) with potential antineoplastic activity. Vaccination with telomerase peptide vaccine GV1001, which binds multiple HLA class II molecules and harbors putative HLA class I epitopes, may activate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against telomerase-expressing tumor cells. Telomerase, a reverse transcriptase normally repressed in healthy cells, is overexpressed in most tumor cell types and plays a key role in cellular proliferation.
telomerase: 540-548 peptide vaccine
A recombinant peptide consisting of the amino acid residues 540 to 548 of the human telomerase reverse transcriptase (hTERT). Telomerase expression has been directly linked to tumor development; its catalytic subunit is expressed in the majority of human cancer cells, but infrequently in normal cells. Vaccination with telomerase:540-548 peptide may stimulate cytotoxic T cells to recognize and kill telomerase-expressing cells.
The hydrochloride salt of an anthrapyrazole antineoplastic antibiotic. Teloxantrone intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair, as well as RNA and protein synthesis.
(Other name for: topical piperidine nitroxide MTS-01)
(Other name for: halofuginone hydrobromide)
A lipophilic preparation of 7-ethyl-10-hydroxycamptothecin (SN-38) with potential antineoplastic activity. Tenifatecan is an oil-in-water emulsion of tocopherol covalently linked, via a succinate linker, to SN-38, an active metabolite of the camptothecin derivative irinotecan. After the succinate linker is hydrolyzed in vivo, the active moiety SN-38 is released and selectively stabilizes topoisomerase I-DNA covalent complexes, thereby inhibiting religation of topoisomerase I-mediated single-stranded DNA breaks and inducing lethal double-stranded DNA breaks; DNA replication is inhibited and apoptosis is triggered. This agent may provide greater delivery and exposure of SN-38 to the tumor than can be achieved with irinotecan.
A synthetic antiviral acyclic nucleotide analogue of adenosine 5-monophosphate. Tenofovir is incorporated into human immunodeficiency viral DNA instead of the natural substrate deoxyadenosine 5-triphosphate, thereby inhibiting HIV-1 reverse transcriptase (RT), an RNA-dependent DNA polymerase, and resulting in DNA chain termination and impairment of viral replication and propagation. This agent prevents HIV from reproducing in uninfected cells only. Tenofovir exhibits activity against the hepatitis B virus (HBV).
A synthetic tetra-methylated derivative of nordihydroguaiaretic acid (NDGA) and transcriptional inhibitor with potential antiviral, antiangiogenic, and antineoplastic activities. Terameprocol competes with the transcription factor Sp1 for specific Sp1 DNA binding domains within gene promoter regions during DNA synthesis. In virally-infected cells, blocking of the Sp1 binding site suppresses Sp1-regulated viral promoter activity and gene expression, thereby inhibiting viral transcription and replication. In tumor cells, blockage of Sp1 binding sites by this agent interferes with the transcription of the Sp1-dependant genes cyclin-dependant kinase (Cdc2), survivin, and vascular endothelial growth factor (VEGF), which are overexpressed in a variety of cancers. By suppressing Sp1-regulated transcription of these genes, terameprocol may reduce tumor angiogenesis and tumor cell proliferation and induce tumor cell apoptosis.
A derivative of the phthalanilide compounds. Terephthalamidine belongs to a family of compounds which appear to reversibly bind to the minor groove of the DNA double helix but not intercalate DNA. This agent also has been suggested to form ionic complexes with many biological components in vitro, including nucleic acids, proteins and lipids.
A triazene triepoxide with antineoplastic activity. Teroxine alkylates and cross-links DNA, thereby inhibiting DNA replication.
A semi-synthetic, orally bioavailable taxane derivative with potential antineoplastic and antiangiogenic properties. Tesetaxel binds to and stabilizes tubulin, promoting microtubule assembly and thereby preventing microtubule depolymerization. This may lead to cell cycle arrest and an inhibition of cell proliferation. This agent may also inhibit pro-angiogenic factors such as vascular endothelial growth factor (VEGF). As it represents poor substrate for P-glycoprotein-related drug resistance mechanisms, this agent may be useful for treating multi-drug resistant tumors.
(Other name for: testolactone)
(Other name for: thiotepa)
(Other name for: therapeutic testosterone)
A progesterone derivative with antineoplastic activity. Testolactone inhibits steroid aromatase, thereby preventing the formation of estrogen from adrenal androstenedione and reducing endogenous estrogen levels.
(Other name for: therapeutic testosterone)
A topical gel preparation of synthetic testosterone. In vivo, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes, resulting in an increase in protein anabolism, a decrease in amino acid catabolism, and retention of nitrogen, potassium, and phosphorus; DHT binds with higher affinity to nuclear androgen receptors than testosterone. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Testosterone and DHT promote the development and maintenance of male sex characteristics related to the internal and external genitalia, skeletal muscle, and hair follicles; estradiol promotes epiphyseal maturation and bone mineralization.
An injectable form of the undecanoate ester form of the androgen testosterone, with luteinizing hormone (LH)-secretory inhibiting activity. As testosterone inhibits gonadotropin secretion from the pituitary gland, by administering testosterone the amount of secreted LH is diminished. By inhibiting LH secretion, the growth of Leydig cells, which are normally stimulated by LH to produce testosterone, may be suppressed.
testosterone vaginal cream
A topical cream containing a synthetic form of the endogenous androgenic steroid testosterone. Upon vaginal application, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. DHT binds with higher affinity to androgen receptors than testosterone, activating gene expression more efficiently. In addition, testosterone is irreversibly converted to estradiol by the enzyme complex aromatase, particularly in the liver and adipose tissue. Topical application of testosterone may improve symptoms of vaginal dryness.
(Other name for: therapeutic testosterone)
(Other name for: therapeutic testosterone)
(Other name for: therapeutic testosterone)
tetanus peptide melanoma vaccine
A vaccine consisting of peptides derived from melanoma-associated antigens and a modified T-cell epitope derived from tetanus toxoid. Vaccination with this agent may stimulate a host cytotoxic and helper T-cell response against tumor cells expressing melanoma-associated antigens, resulting in decreased tumor growth.
tetanus toxoid helper peptide
Obtained by genetic engineering from the bacterial Clostridium tetani toxoid, tetanus toxoid helper peptide QYIKANSKFIGITEL (amino acids 830-844) binds to class II MHC molecules as a nonspecific vaccine helper epitope (adjuvant) and induces an increased (and long term) immune response by increasing the helper T-cell response.
tetanus-CMV fusion peptide vaccine
A vaccine containing an inactivated epitope of tetanus toxin fused to a cytomegalovirus (CMV) peptide epitope, with potential anti-viral and immunomodulating activities. Upon administration, tetanus-CMV fusion peptide may stimulate a cytotoxic T-lymphocyte (CTL) response against CMV in the CMV-infected host. Tetanus toxin contains universal T cell helper epitopes.
Any of a group of broad spectrum naphthacene antibiotics isolated from various species of Streptomyces or produced semisynthetically. In bacteria, tetracycline antibiotics block binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis.
The hydrochloride salt of tetracycline, a broad-spectrum naphthacene antibiotic produced semisynthetically from chlortetracycline, an antibiotic isolated from the bacterium Streptomyces aureofaciens. In bacteria, tetracycline blocks binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis and bacterial cell growth. Because naturally fluorescing tetracycline binds to newly formed bone at the bone/osteoid interface, tetracycline-labeling of bone and fluorescence microscopy may be used to perform bone histomorphometry.
tetraphenyl chlorin disulfonate
A meso-tetraphenylchlorin substituted by two adjacent sulfonated groups with potential photosensitizing activity. Upon administration, tetraphenyl chlorin disulfonate incorporates into the cellís endosome and lysosome membranes. Subsequently, cytotoxic agents are administered and accumulate in endosomal and lysosomal compartments; upon local activation by light, tetraphenyl chlorin disulfonate produces reactive oxygen species (ROS), such as singlet oxygen, damaging endo/lysosomal membranes and accumulated cytotoxic agents are released into the tumor cell cytosol. This photochemical internalization (PCI) method can enhance the efficacy and selectivity of cytotoxic agents.
A neurotoxin with potential analgesic activity. Tetrodotoxin binds to the pores of fast voltage-gated fast sodium channels in nerve cell membranes, inhibiting nerve action potentials and blocking nerve transmission. Although found in various species of fish (such as the pufferfish), newts, frogs, flatworms, and crabs, tetrodotoxin, for which there is no known antidote, is actually produced by bacteria such as Vibrio alginolyticus, Pseudoalteromonas tetraodonis, and other vibrio and pseudomonas bacterial species.
A synthetic purine nucleoside analogue with potential antineoplastic activity. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types.
TGF-beta-resistant LMP-specific cytotoxic T-lymphocytes
A preparation of transforming growth factor-beta (TGF-beta)-resistant cytotoxic T-lymphocytes (CTL) reactive to Epstein-Barr virus (EBV) latent membrane proteins 1 and 2 (LMP 1 and 2) with potential antineoplastic activity. T lymphocytes are transduced with a retroviral vector expressing the dominant-negative mutant type II TGF-beta receptor, which blocks signaling by all three TGF-beta isoforms. These TGF-beta-resistant T-lymphocytes are exposed ex-vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP; subsequent exposure to LMP1- or LMP2-expressing lymphoblastoid cell lines is used to expand the CTL. Administered to patients with EBV-positive tumors, TGF-beta-resistant LMP-specific CTL target LMP-positive cells, which may result in a specific CTL response, followed by cell lysis and inhibition of tumor cell proliferation. Tumor-expressed TGF-beta inhibits T lymphocyte activation and expansion.
A recombinant, chimeric toxin composed of human transforming growth factor alpha (TGF-alpha) fused to a fragment of Pseudomonas exotoxin (PE38) without its cell-binding domain. The TGF-alpha moiety of the agent attaches to tumor cells expressing the epithelial growth factor receptor (EGFR); the exotoxin induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also catalyzes the transfer of ADP ribose from nicotinamide adenine dinucleotide (NAD) to elongation factor-2 in eukaryotic cells, thereby inactivating elongation factor 2 and inhibiting protein synthesis.
A natural aporphine benzylisoquinoline vinca alkaloid with antineoplastic activity. Thalicarpine binds to and inhibits p-glycoprotein, the multidrug resistance efflux pump. Thalicarpine also induces single-strand breaks in DNA and arrests cancer cells at the G2/M and G1 phase of the cell cycle.
thapsigargin prodrug G-202
A soluble, thapsigargin prodrug containing the cytotoxic analog of thapsigargin, 8-O-(12Aminododecanoyl)-8-O debutanoylthapsigargin (12-ADT) linked, via a carboxyl group, to the targeting peptide containing aspartic acid with potential antineoplastic activity. Upon intravenous administration, the non-toxic prodrug targets prostate specific membrane antigen (PSMA), a type II membrane carboxypeptidase, which is overexpressed in prostate cancer cells and in the neovasculature of most solid tumors but not in normal blood vessels. G-202 is subsequently converted, through hydrolysis, into the active cytotoxic analog of thapsigargin 12-ADT-Asp. 12-ADT binds to and blocks the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump, thereby increasing the concentration of cytosolic calcium which leads to an induction of apoptosis. By preventing nutrient supply to tumor cells, G-202 may be able to inhibit tumor growth. Compared to thapsigargin alone, thapsigargin prodrug G-202 is able to achieve higher concentrations of the active agents at the tumor site while avoiding systemic toxicity.
(Other name for: theophylline)
(Other name for: theophylline)
(Other name for: theophylline)
therapeutic allogeneic cytotoxic T lymphocytes
A population of cytotoxic T-lymphocytes (CTLs) that are therapeutically administered to a recipient individual who is genetically distinct from a donor of the same species.
therapeutic allogeneic lymphocytes
A population of lymphocytes therapeutically administered to a recipient individual who is genetically distinct from a donor of the same species.
therapeutic autologous dendritic cells
A population of a type of antigen-presenting cell (APC), the dendritic cell (DC), harvested from a patient and grown in vitro in the presence of tumor-associated antigens (TAAs) derived from the patient's tumor (a technique known as 'pulsing') and then injected back into the patient; autologous DCs so manipulated may stimulate a specific cell-mediated antitumoral cytotoxicity. DCs derived from a patient may also be fused with the patient's tumor cells in vitro to combine sustained tumor antigen expression with the antigen-presenting and immunostimulatory capacities of DCs; when injected back into the patient, these autologous DC-tumor cell hybrids (fusion cells) may stimulate an active antitumoral immune response.
therapeutic autologous lymphocytes
A population of lymphocytes isolated from an individual, altered in vitro, and returned to the same individual for therapeutic purposes.
therapeutic breast/ovarian/prostate cancer vaccine DPX-0907
A lipid-based multi-peptide cancer vaccine targeted against multiple cancers with immunopotentiating activity. Therapeutic breast/ovarian/prostate peptide cancer vaccine DPX-0907 is a lyophilized liposomal proprietary preparation comprised of 7 tumor-specific HLA-A2-restricted epitopes (TAAs): topoisomerase II alpha, B-cell receptor-associated protein 31 (CDM protein), TNF-alpha-converting enzyme (TACE/ADAM17), Abelson homolog 2 (Abl2), gamma catenin (Junction plakoglobin), epithelial discoidin domain receptor 1 (EDDR1) and integrin beta 8 subunit. Upon vaccination, the lyophilized antigen/adjuvant/liposome complex is re-suspended in Montanide 1SA51 VG to create a depot effect, thereby presenting the TAAs to the immune system for a prolonged period of time. This may stimulate a potent cytotoxic T-lymphocyte (CTL) immune response against cancer cells that express these 7 TAAs and share epitopes with the vaccine epitope peptides, resulting in tumor cell lysis. The 7 TAAs are overexpressed on the surface of breast/ovarian and prostate cancer cells and play an important role in tumor cell growth and survival.
The synthetic form of the naturally occurring sympathomimetic amine with vasoconstricting, intraocular pressure-reducing, and bronchodilating activities. By stimulating vascular alpha-adrenergic receptors, epinephrine causes vasoconstriction, thereby increasing vascular resistance and blood pressure. When administered in the conjunctiva, this agent binds to alpha-adrenergic receptors in the iris sphincter muscle, resulting in vasoconstriction, a decrease in the production of aqueous humor, and a lowering of intraocular pressure. Through its beta1 receptor-stimulating actions, epinephrine increases the force and rate of myocardial contraction and relaxes bronchial smooth muscle, resulting in bronchodilation.
A synthetic steroid similar or identical to endogenous estetrol, a short-acting estrogen with both agonistic and antagonistic estrogen receptor activity. Administered orally, therapeutic estetrol binds to the estrogen receptor and as a selective estrogen receptor modulator (SERM) exhibits estrogen agonism in certain tissues and estrogen antagonism in others. Displaying weak estrogen activity in the uterus, estetrol acts as an estrogen antagonist in breast tissue. Produced solely by the human fetal liver, endogenous estetrol is the primary estrogen metabolite of estrogen biosynthesis in the human fetal liver.
A steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Typically esterified, estradiol derivatives are formulated for oral or parenteral administration. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. Estradiol exhibits mild anabolic and metabolic properties, and increases blood coagulability.
A sterile, lyophilized powder of hemin, the Fe3+ oxidation product of heme (Fe2+), derived from processed red blood cells. Therapeutic hemin appears to inhibit delta-aminolevulinic acid (ALA) synthetase, a rate-limiting enzyme in the porphyrin/heme biosynthetic pathway, resulting in inhibition of the hepatic and/or marrow synthesis of porphyrin precursors. The mechanism by which therapeutic hematin produces symptomatic improvement in patients with acute episodes of the hepatic porphyrias has not been determined.
A synthetic or semisynthetic analog of natural hydrocortisone hormone produced by the adrenal glands with primary glucocorticoid and minor mineralocorticoid effects. As a glucocorticoid receptor agonist, hydrocortisone promotes protein catabolism, gluconeogenesis, capillary wall stability, renal excretion of calcium, and suppresses immune and inflammatory responses.
therapeutic immune globulin
A preparation of plasma proteins derived from the pooled plasma of adult donors. Largely comprised of IgG antibodies, therapeutic immune globulin provides passive immunization by increasing the recipient's serum levels of circulating antibodies. IgG antibodies have multiple functions, including binding to and neutralizing bacterial toxins; opsonization of pathogens; activation of complement; and suppression of pathogenic cytokines and phagocytes through binding to CD5, interleukin-1a (IL-1a), interleukin 6 (IL-6), tumor necrosis factor-alpha (TNF-alpha), and T-cell receptors. Therapeutic immune globulin may diminish pathogenic mechanisms in some autoimmune diseases by binding to and inhibiting the activity of autoantibodies.
A synthetic or animal-derived form of insulin used in the treatment of diabetes mellitus. Therapeutic insulin is formulated to be short-, intermediate- and long-acting in order to individualize an insulin regimen according to individual differences in glucose and insulin metabolism. Therapeutic insulin may be derived from porcine, bovine or recombinant sources. Endogenous human insulin, a pancreatic hormone composed of two polypeptide chains, is important for the normal metabolism of carbohydrates, proteins and fats and has anabolic effects on many types of tissues.
A therapeutic chemically synthesized form of the pineal indole melatonin with antioxidant properties. The pineal synthesis and secretion of melatonin, a serotonin-derived neurohormone, is dependent on beta-adrenergic receptor function. Melatonin is involved in numerous biological functions including circadian rhythm, sleep, the stress response, aging, and immunity.