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Dictionary of drugs: 0-9

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Dictionary of pharmaceutical drugs/medications sorted alphabetically

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Drug terms 0-9

A lipophilic copper(II)bis(thiosemicarbazone) labeled with the positron-emitting isotope (61)Cu with hypoxia-selective and radioisotopic activities. With a high membrane permeability and redox potential, (61)Cu-ATSM easily enters and selectively resides in hypoxic cells. The extent of (61)Cu-ATSM retention in tissue is inversely related to the state of tissue oxygenation allowing the quantitation of tissue hypoxia with positron emission tomography (PET).

A radioconjugate consisting of the positron emitting radioisotope fluorine F 18 conjugated to the substance P antagonist receptor quantifier (SPA-RQ) used in radioimaging. [18F]-labeled substance P antagonist receptor quantifier is an antagonist of the neurokinin 1 (substance P) receptor (NK1R) and can function as a positron emission tomography (PET) imaging agent for detecting NK1R-expressing cells and tissues. NK1Rs are frequently expressed on the plasma membranes of tumor cells from glioblastoma and breast and pancreatic carcinomas.

A deoxycytidine analog and high-affinity substrate for deoxycytidine kinase (DCK), labeled with fluorine F 18, with potential diagnostic activity upon positron emission tomography (PET) imaging. [18F]L-FAC is preferentially taken up by and accumulated in cells with high deoxycytidine kinase (DCK) levels, such as in tumor cells with dysregulated nucleoside metabolism. Upon uptake through the nucleoside transporter, [18F]L-FAC is phosphorylated by DCK and, subsequently, the 18F moiety can be visualized upon PET imaging. As many nucleoside analog prodrugs are chemotherapeutic agents that require DCK for activation, [18F]L-FAC can potentially be used as a marker to predict chemotherapeutic efficacy of these prodrugs. In addition, as DCK is upregulated in certain immune cells, such as activated T-cells, [18F]L-FAC can also be used to measure immune activation in response to immunomodulating agents. DCK, a rate-limiting enzyme in the nucleoside salvage pathway for DNA synthesis, is overexpressed in certain solid tumors, lymphoid and myeloid malignancies and certain immune cells, such as proliferating T-lymphocytes.

A radioconjugate composed of 2′-deoxy-2′-18F-fluoro-5-methyl-beta-L-arabinofuranosylcytosine ([18F]L-FMAC), a L-deoxycytidine analog and high-affinity substrate for deoxycytidine kinase (DCK), labeled with fluorine F 18, with potential diagnostic activity during positron emission tomography (PET) imaging. Upon administration, [18F]L-FMAC is preferentially taken up by and accumulated in cells with high DCK levels, including tumor cells with dysregulated nucleoside metabolism. After phosphorylation by DCK, the 18F moiety can be visualized by PET imaging. As many nucleoside analog prodrugs are chemotherapeutic agents that require DCK for their phosphorylation and activation, [18F]L-FMAC can potentially be used as a marker to measure DCK activity and to predict the chemotherapeutic efficacy of DCK-dependent prodrugs. DCK, a rate-limiting enzyme in the deoxyribonucleoside salvage pathway for DNA synthesis, is overexpressed in certain solid tumors, lymphoid and myeloid malignancies and certain immune cells, such as proliferating T-lymphocytes. The L-enantiomer is less susceptible to deamination by cytidine deaminase (CDA) than the D-enantiomer and increases the stability of this radioconjugate.

A small molecular-weight, malonic acid-based probe [(2-(5-fluoro-pentyl)-2-methyl-malonic acid or ML-10] labeled with the radioactive isotope fluorine F 18 with potential apoptosis radioimaging use. Upon administration, [F18]-ML-10 binds selectively to apoptotic cells due to apoptotic cell membrane features that differ from those of normal, healthy and necrotic cell membranes. Upon entering the apoptotic cell, this agent accumulates within the cytoplasm where it can be imaged using positron emission tomography (PET). Detection of apoptotic cells using this imaging technology may be useful in monitoring tumor responses to cytotoxic therapies. ML-10 appears to mimic the alkyl-malonic acid motif present in gamma -carboxyglutamic (Gla), an amino acid that plays a crucial role in the binding of clotting factors to negatively-charged phospholipids exposed on the surfaces of apoptotic cells.

A 2-nitroimidazole labeled with the positron-emitting radioisotope fluorine F 18. HX4, the 2-nitroimidazole moiety of [F-18]HX4, is selectively bioreduced and bound in hypoxic tumor cells, permitting the imaging of hypoxic tumor cells with positron emission tomography (PET).

A radiopharmaceutical consisting of a sulfonamide covalently attached to the positron-emitting isotope fluorine F 18 with CA-IX-binding and radioisotopic activities. Upon administration, the sulfonamide moiety of [F18]VM4-037 binds to the cell-surface tumor-associated antigen (TAA) carbonic anhydrase IX isoenzyme (CA-IX); CA-IX-expressing tumor cells can then be visualized using positron emission tomography (PET). CA-IX has been found to be elevated in a variety of hypoxic tumors; elevated CA-IX has been positively correlated with tumor growth, tumor invasion and poor prognosis.

A selective, orally bioavailable inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11b-HSD1; 11bHSD1; HSD11B1), with potential protective activity. Upon administration, AZD4017 selectively binds to and inhibits the activity of 11b-HSD1. This prevents the conversion of cortisone to the active hormone cortisol that activates glucocorticoid receptors. By blocking cortisol production in metabolic tissues, AZD4017 may inhibit the adverse metabolic effects, such as glucose intolerance, hyperinsulinemia, systolic hypertension, increased adiposity, myoatrophy and dermal atrophy, caused by exogenous administration of glucocorticoids in these tissues. 11bHSD1 is highly expressed in metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a crucial role in regenerating active glucocorticoid from circulating glucocorticoids and regulates the production of cortisol to activate the glucocorticoid receptors. AZD4017 does not inhibit the anti-inflammatory activity of the administered glucocorticoids.

A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata radiolabeled with carbon 11 (11C) with antineoplastic and radiotracer properties. During the S phase of the cell cycle, topotecan inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Quantitation of 11C topotecan accumulated in tumor tissues by positron emission tomography (PET) may help predict responses to topotecan therapy.

An iodine 123-radiolabled small molecule that exhibits high affinity for prostate-specific membrane antigen (PSMA) with potential use in molecular imaging. 123-I-MIP-1095, a radiolabeled glutamate-urea-lysine analogue, selectively binds PSMA, which allows imaging of PSMA-expressing prostate cancer cells with gamma scintigraph. PSMA is a transmembrane glycoprotein highly expressed by malignant prostate epithelial cells and vascular endothelial cells of various solid tumors.

The orally bioavailable C-4 methyl carbonate analogue of paclitaxel, labeled with radioactive carbon 14, with radioisotope and potential antineoplastic activities. 14C BMS-275183 binds to tubulin and inhibits microtubule disassembly, which may result in cell cycle arrest at the G2/M phase and inhibition of cell division, and subsequently cell death. This agent may be useful for treating multi-drug resistant (MDR) tumors because it does not appear to be a substrate for P-glycoprotein.

A stable derivative of prostaglandin E2 (PGE2) with potential hematopoietic activity. Administration of 16,16 dimethyl-prostaglandin E2 (dmPGE2) appears to lead to increased formation of hematopoietic stem and progenitor cells. Even though the exact mechanism of action has yet to be fully elucidated, this agent may stimulate hematopoiesis by activating the Wnt signaling pathway, which increases cellular levels of beta-catenin, a subunit of the cadherin protein complex.

A fluorine-18-labeled acycloguanosine derivative substrate for herpes simplex virus type-1 thymidine kinase (HSV1-tk). 18F-FHBG is used as a reporter probe to image the expression of the herpes simplex virus type-1 thymidine kinase (HSV1-tk) gene in gene transfer therapy. HSV1-tk and and HSV1-tk-metabolized 18F-FHBG co-localize, allowing positron emission tomography (PET) localization of HSV1-tk gene-transfected tissue and the assessment of gene transfer efficiency.

A radioconjugate and an acetate analog labeled with fluorine F 18 ((18)F-FAC), a positron-emitting isotope, with potential prostate tumor tracer property using positron emission tomography (PET). Although the mechanism of action is unclear, fluorine F 18 acetate preferentially accumulates in tumor tissue, serving as a tracer for imaging tumors with PET. Fluorine 18 has a longer radioactive half-life (110 min) vs. the half-life of carbon-11 acetate (20.4 min). Furthermore, (18)F-FAC showed a rapid clearance from liver and extensive excretion to bile and urine in comparison with carbon-11 acetate, therefore this tracer may be a useful alternative to C-11 acetate for the detection of prostate tumors by PET.

A radiofluorinated 2-nitroimidazole derivate with hypoxia-specific tracer activity. Misonidazole is reduced under hypoxic conditions and in reduced form covalently binds to macromolecules in hypoxic cells. 18F (fluorine-18) radiofluorination of misonidazole to form 18F-fluoromisonidazole allows radioisotopic imaging of reduced misonidazole bound to macromolecules in hypoxic cells.

A radiotracer containing a pegylated dimeric Arg-Gly-Asp (RGD) peptide (NH2-mini-PEG-E[c(RGDyK)]2 or PRGD2) radiolabeled with fluorine 18F-fluorobenzoate (18F-FB), with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET). Upon administration, the RGD moiety of 18F-labeled mini-PEG spacered RGD dimer (18F-FPRGD2) binds to alphaVbeta3 integrin. Upon PET, alphaVbeta3-expressing tumor cells can be visualized and the degree of tumor angiogenesis can be determined. This agent exhibits increased integrin receptor binding affinity, tumor cell uptake and increased radiolabeling yield as compared to the non-pegylated form (18F-FRGD2). Integrins, transmembrane glycoproteins, may be upregulated on proliferating tumor vessel endothelial cells and various cancer cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells, metastasis and an overall poor prognosis.

A heparin derivative in which the 2-O and 3-O sulfate groups of heparin are removed and that lacks anticoagulant activity, with potential anti-inflammatory, immodulatory and antineoplastic activities. Upon administration, 2-O, 3-O desulfated heparin (ODSH) binds to both chemokine stromal cell-derived factor 1 (SDF-1 or CXCL12) and CXC chemokine receptor 4 (CXCR4). This prevents the interaction of CXCL12 with CXCR4, blocks CXCR4 activation, and may result in decreased proliferation and migration in CXCR4-overexpressing tumor cells. In addition, inhibition of CXCL12/CXCR4 interaction may induce mobilization of hematopoietic cells from the bone marrow into the blood.  In addition, ODSH prevents the interaction of the receptor for advanced glycation end-products (RAGE) with its ligands, including advanced glycation end-products (AGEs), Mac-1(CD11b/CD18), the nuclear pro-inflammatory protein high mobility group box protein-1 (HMGB-1), carboxymethyl lysine-bovine serum albumin (CML-BSA) and members of the S100 calgranulin family. In addition, this agent inhibits the enzymes heparanase, cathepsin G, and human leukocyte elastase, which are involved in inflammation and metastasis. ODSH also binds to platelet factor 4 (PF4 or CXCL4) and may prevent PF4's inhibitory effect on platelet production.  Altogether, this may inhibit tumor cell invasiveness and metastasis. ODSH also binds to platelet factor 4 (PF4 or CXCL4) and may prevent PF4's inhibitory effect on platelet production. This may increase platelet production. Unlike heparin, this agent does not induce heparin-induced thrombocytopenia (HIT). RAGE, a receptor belonging to the immunoglobulin superfamily, plays a key role in inflammation and is overexpressed in a variety of cancers. CXCR4 is a chemokine receptor belonging to the G protein-coupled receptor (GPCR) family that plays an important role in chemotaxis, chemoresistance and angiogenesis, and is upregulated in several tumor cell types. The interaction between CXCL12/CXCR4 induces retention of hematopoietic cells in the bone marrow.

A deoxyuridine prodrug with potential antineoplastic activity. Upon cellular uptake, 2’-F-ara-deoxyuridine (FAU) is phosphorylated by thymidine kinase to FAU monophosphate and subsequently methylated in the 5'-position by thymidylate synthase (TS) to its activated form, 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FMAUMP is incorporated into DNA leading to an inhibition of DNA synthesis and so cell growth. The catalytic activity of TS is critical to activation of FAU and subsequent incorporation into DNA. FAU may be beneficial in the case of tumors with high TS activity that are resistant to TS inhibitors.

An orally bioavailable fluorinated analog of fucose that is a protein fucosylation inhibitor, with potential antineoplastic and immunomodulating activities. Upon administration of SGN-2FF, 2-fluorofucose (2-FF) mimics fucose and is converted to guanosine diphosphate (GDP)-2FF, which prevents the formation of the fucosylation substrate GDP-fucose, and the incorporation of fucose into glycoproteins by fucosyltransferase. As fucosylation of glycoproteins plays a key role in many biological processes, such as protein function, receptor binding, cell signaling and cellular adhesion, and is essential for tumor progression, blocking fucosylation decreases tumor cell growth. In addition, blocking fucosylation of monoclonal antibodies generates fucose-deficient antibodies that exert enhanced antibody-dependent cell-mediated cytotoxicity (ADCC).

A radiopharmaceutical agent comprised of a pegylated dimeric arginine-glycine-aspartic acid (RGD)-based peptide labeled with 2-fluoropropionyl, with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET). The RGD moiety of 2-fluoropropionyl-labeled pegylated dimeric RGD peptide targets and binds to alphaVbeta3 integrin. Upon PET imaging, alphaVbeta3 integrin-expressing tumor cells can be visualized and expression levels can be quantified. Compared to other fluorine F 18 labeled RGD-containing peptides, this agent shows increased affinity to alphaVbeta3 integrin, enhanced tumor uptake as well as improved pharmacokinetics. alphaVbeta3 integrin, overexpressed on certain tumor cells and tumor endothelial cells, plays a key role in angiogenesis, tumor proliferation and survival.

A preparation of autologous human T-lymphocytes isolated from renal cell cancer (RCC) patient and transduced with 2G-1 TCR, a retroviral vector encoding the alpha and beta chains of a T-cell receptor that recognizes TNF-related apoptosis inducing ligand (TRAIL) bound to death receptor 4 (DR4), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and introduction into the RCC patient, 2G-1 TCR retroviral vector-transduced lymphocytes may stimulate a cytotoxic T lymphocyte (CTL) response against RCC cells with TRAIL bound to DR4 on their surfaces. TRAIL, a member of the TNF superfamily, is a homotrimeric type II membrane protein that rapidly induces oligomerization of receptor intracellular death domains and apoptosis in a variety of tumor cells when bound to its receptors; DR4 (TRAIL receptor 1), a member of the TNF receptor family, is overexpressed by a variety of malignant cell types.

A depot formulation containing a bioresorbable, controlled-release, calcium sulphate-based paste of the nonsteroidal antiandrogen 2-hydroxyflutamide (2-HOF) with potential antineoplastic activity. Upon injection into the tumor site in the prostate, 2-hydroxyflutamide depot slowly releases 2-HOF, which competitively binds to androgen receptors (ARs), blocking the binding of dihydrotestosterone (DHT). This may inhibit androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest and decreased cellular proliferation. In addition, 2-HOF inhibits nuclear uptake of androgen in androgen-responsive tissues.

An orally bioavailable, synthetic analog of the fatty acid oleic acid, with potential antitumor activity. Upon administration, 2-hydroxyoleic acid (2OHOA) activates sphingomyelin synthase (SMS), thereby increasing the concentration of sphingomyelin (SM) and diacylglycerol (DAG) in the tumor cell membrane and decreasing membrane levels of phosphatidylethanolamine (PE) and phosphatidylcholine (PC). This restores the normal, healthy levels and ratios of membrane lipids. By restoring normal membrane lipid structure and composition, this agent inhibits membrane-protein associated signaling and the aberrant activity of signaling pathways in certain tumor cells, including the Ras/MAPK and PI3K/AKt pathways. This inhibits tumor cell proliferation, induces tumor cell differentiation, and eventually can cause cell death.

An orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

A ring-substituted amphetamine derivative, structurally related to the hallucinogen mescaline, with entactogenic, neurotoxic, and motor-stimulatory activities. 3,4-methylenedioxymethamphetamine (MDMA) produces an acute, rapid enhancement in both the release of serotonin from and the inhibition of serotonin reuptake by serotonergic nerve endings in the brain. Once within the cell, MDMA depletes stores of tryptophan hydroxylase (TPH) via acute oxidative inactivation; in turn, depleted stores of TPH leave cell terminals open to damage from oxidative stress, possibly a source of MDMA neurotoxicity. This agent also induces norepinephrine, dopamine, and acetylcholine release and can act directly on a number of receptors, including alpha 2-adrenergic and 5-hydroxytryptamine (5-HT) 2A receptors. MDMA may suppress the dyskinesia associated with long-term use of L-dopamine (L-DOPA) without affecting the efficacy of L-DOPA treatment.

A hapten-carrier immunoconjugate composed of the hapten trans-3′-aminomethyl nicotine conjugated to a recombinant P. aeruginosa exoprotein A, rendered nontoxic through amino acid depletion, with potential immunostimulating activity. Upon vaccination with 3'-aminomethyl nicotine-P. aeruginosa r-exoprotein A conjugate vaccine, the immune system may produce anti-nicotine antibodies. Antibody-bound nicotine cannot pass the blood brain barrier (BBB) to activate brain nicotine receptors. Nicotine, a small organic molecule that is not immunogenic, must be haptenized and conjugated to a carrier protein, such as nontoxic recombinant P. aeruginosa exoprotein A, to induce an antibody response. Aluminium hydroxide may be used as an adjuvant for this vaccine.

A synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule.

A synthetic analogue of nucleoside uridine lacking a ring nitrogen in the 3-position. 3-deazauridine inhibits cytidine synthase, thereby reducing intracellular levels of cytidine and deoxycytidine and disrupting DNA and RNA synthesis. This agent may trigger apoptosis and enhance differentiation of neoplastic cells.

A population of proprietary, off-the-shelf, three-dimensional (3D)-expanded, allogeneic placenta-derived stromal cells that can potentially be used to increase hematopoietic recovery from hematological disorders or after a hematopoietic stem cell transplant (HSCT). Upon intramuscular (IM) injection of placental expanded (PLX)-R18, these cells secrete a range of specific hematopoietic, regenerative proteins depending on their in vivo environment. The secreted proteins are involved in maintenance, renewal, proliferation, differentiation, and mobilization of hematopoietic progenitor cells (HPCs), and include, but are not limited to, granulocyte colony-stimulating factor (GCSF), monocyte chemoattractant protein-1 (MCP-1/CCL2), MCP-3 (CCL7), interleukin-6 (IL-6), and IL-8. This increases the number of colony-forming hematopoietic progenitors in the bone marrow, regenerates the bone marrow hematopoietic cells, and elevates and restores blood cell production.

A radioconjugate composed of the radionuclide fluorine F 18 conjugated to L-glutamic acid, with potential imaging activity upon positron emission tomography (PET). Upon intravenous administration, the glutamic acid moiety of 4-[18F]fluoroglutamic acid specifically binds to tumor cells and is preferentially taken up by tumor cells due to the higher metabolic activity and enhanced glutaminolytic pathway in these cells compared to normal, healthy cells. Upon internalization and PET, tumor cells can be imaged and assessed. Tumor cells use the amino acid glutamine for nutritional purposes necessary for energy production and growth; as tumor cells proliferate more rapidly than normal healthy cells, glutamine uptake is higher in certain cancer cells.

A preparation of genetically modified autologous T-lymphocytes transduced with a retroviral vector expressing a chimeric antigen receptor (CAR) targeting the human tumor-associated antigen (TAA) MUC16ecto and encoding the human pro-inflammatory cytokine interleukin-12 (IL-12), fused to the signaling domain of the zeta chain of the TCR/CD3 complex (28z), and a truncated form of the human epidermal growth factor receptor (EGFRt), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, 4H11-28z/fIL-12/EGFRt-expressing autologous T-lymphocytes are directed to and induce selective toxicity in MUC16-expressing tumor cells. In addition, the T-cells secrete IL-12 which induces secretion of interferon-gamma, promotes the activation of natural killer cells (NKs), and induces cytotoxic T-cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. Devoid of both ligand binding domains and tyrosine kinase activity, the expressed EGFRt both facilitates in vivo detection of the administered, transduced T-cells and can promote elimination of those cells through a cetuximab-induced antibody-dependent cellular cytotoxicity (ADCC) response. MUC16, a transmembrane protein and glycosylated mucin, is overexpressed on the cell surface of the majority of ovarian cancer cells but not on healthy cells. MUC16ecto is the extracellular portion of MUC-16 and is the part that is retained by cells after cleavage of CA-125.

An iodinated doxorubicin analogue with antiamyloid activity. 4'-Iodo-4'-deoxydoxorubicin (IDOX) binds with high affinity to five types of natural amyloid fibrils including immunoglobulin light chains, amyloid A, transthyretin (methionine-30 variant), ß-protein (Alzheimer), and ß2-microglobulin. This agent may inhibit fibril growth, increasing the solubility of amyloid tissue deposits and facilitating their clearance. IDOX has also been shown to insulin amyloid fibrillogenesis in vitro.

A synthetic derivative of estradiol. 4-nitroestrone 3-methyl ether inhibits estrogen sulfotransferase (EST), a progesterone-induced secretory endometrial enzyme which affects estrogen receptor levels. This agent has been shown to be an effective growth inhibitor of some chemically induced animal mammary tumors.

An emulsion of 4 melanoma peptides with potential immunomodulating and antineoplastic activities. Upon vaccination, 4-peptide melanoma vaccine may stimulate an immune response against 4 different melanoma associated antigens. This may lead to a reduction in tumor cell proliferation of cancer cells expressing these antigens.

Genetically modified autologous T lymphocytes transduced with a lentiviral vector encoding a fourth generation specific chimeric antigen receptor (4SCAR) specific for the disialoganglioside GD2 and which includes the CD3zeta chain and the signaling domains of the co-stimulatory molecules CD28, CD137, and CD27 fused with the suicide gene inducible caspase 9 (iCasp9), with potential immunomodulating and antineoplastic activities. Upon intravenous administration of 4SCAR-GD2 T cells, these cells target the GD2 antigen on tumor cells to induce selective toxicity against GD2-expressing tumor cells. The tumor-associated antigen (TAA) GD2 is overexpressed on the surface of neuroblastoma cells and by other neuroectoderm-derived neoplasms, while it is minimally expressed on normal cells. iCasp9 consists of a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V) linked to human caspase 9. If the administered T cells lead to unacceptable side effects, the chemical homodimerizer AP1903 can be administered; this binds to the drug binding FKBP12-F36V domain and activates caspase 9, which results in the apoptosis of the administered T cells and enhances safety of this agent. CD28, CD137 and CD27, T-cell surface-associated co-stimulatory molecules, are required for full T cell activation.

An orally bioavailable 4-thio modified 2-deoxycytidine analog, with potential antineoplastic activity. Upon administration of 4-thio-2-deoxycytidine (TdCyd), this cytidine analog is incorporated into DNA during replication and inhibits the activity of DNA methyltransferase 1 (DNMT1), which blocks DNA hypermethylation. This results in DNMT1 depletion, hypomethylation of DNA, and the reactivation of tumor suppressor genes that were silenced by hypermethylation; this results in antitumor activity and an inhibition of tumor cell proliferation.

The fluorine-18 (18F)-radiolabeled pyrimidine analog 5-fluorouracil (5-FU) with positron-emitting activity. Upon administration, 5-[18F]fluorouracil distribution in tumor tissue may be measured with positron emission tomography (PET). The degree of 5-[18F]fluorouracil uptake in tumor tissue may help to predict the response to 5-fluorouracil-based chemotherapy or to determine the response to other therapeutic agents used to treat 5-FU-sensitive tumors.

An equimolar gas mixture of oxygen (O2) and nitrous oxide (N2O) with potential analgesic activity. Upon inhalation, 50% oxygen/50% nitrous oxide premix produces rapidly reversible analgesia. The exact mechanism through which nitrous oxide exerts its analgesic effect has yet to be fully elucidated, but it appears to be associated with the neuronal release of endogenous opioid peptides.

An orally bioavailable, nucleoside analog and DNA methyltransferase I (DNMT1) inhibitor, with potential DNA hypomethylating and antineoplastic activities. Upon administration, 5-aza-4'-thio-2'-deoxycytidine (Aza-TdC) gets incorporated into DNA, where it binds to the active site of DNMT1, a maintenance methyltransferase that contributes to the hypermethylation and silencing of tumor suppressor genes. The formation of covalent DNMT1-DNA complexes inhibits DNMT1, prevents DNA methylation of CpG sites, causes CpG demethylation, and results in the re-expression and re-activation of silenced tumor suppressor genes. This inhibits tumor cell proliferation. DNMT1, overactivated in tumor cells, plays a key role in tumor cell proliferation.

A radioconjugate consisting of a 7 amino acid peptide sequence, KCCFPAQ, that specifically targets human colon cancer and that is labeled, via the linker, GGGSK, with the fluorescent dye, fluorescein isothiocyanate (5-FITC), with potential imaging activity. Following spray application to the colon wall during colonoscopy in areas that look abnormal, the colon heptapeptide moiety of 5-FITC-labeled colon-heptapeptide specifically targets and binds to a cell surface target overexpressed on pre-cancerous or cancerous colon cells. Upon internalization, the FITC moiety allows for fluorescent imaging and the area of interest for biopsies can then be visualized.

A radioconjugate consisting of the 7 amino acid peptide sequence ASYNYDA (GI heptapeptide) and labeled with the fluorescent dye fluorescein isothiocyanate (5-FITC), with potential imaging activity. Upon topical application to the esophageal mucosa using a spray, the heptapeptide moiety of 5-FITC-labeled GI-heptapeptide binds to abnormal cells in the esophagus; the FITC moiety allows for imaging with white light and the area of interest for biopsies can then be visualized.

A fluorinated pyrimidine analogue antimetabolite with potential antineoplastic activity. As a prodrug, 5-fluoro-2-deoxycytidine is converted by intracellular deaminases to the cytotoxic agent 5-fluorouracil (5-FU). 5-FU is subsequently metabolized to active metabolites including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits thymidylate synthase, thereby reducing the production of thymidine monophosphate, which leads to depletion of thymidine triphosphate and the inhibition of DNA synthesis and cell division. FUTP competes with uridine triphosphate (UTP) for incorporation into the RNA strand, which results in the inhibition of RNA and protein synthesis and cell proliferation. Other fluorouracil metabolites also get incorporated into both DNA and RNA, with further inhibition of cellular growth.

A topical formulation containing 0.5 % of antimetabolite 5-fluorouracil (5-FU) and 10% of salicylic acid, with potential antimitotic and keratolytic activity. Upon cutaneous application, 5-FU in the 5-fluorouracil/salicylic acid topical solution impedes pyrimidine metabolism thereby inhibiting cell growth, while the salicylic acid induces anti-inflammatory response and results in keratolytic effect. This may result in the breakdown of keratinocytes and prevent proliferation of keratinocytes locally.

A multi-epitope vaccine containing the following six class II MHC-restricted peptides: gp100, MelanA/MART-1, two tyrosinase peptides, and the cancer/testis antigens MAGE-A3 and MAGE-A1,2,3,6, with potential antineoplastic activity. Upon administration, melanoma helper peptides induce an antigen-specific, Th1-dominant, CD4+ T-cell response, potentially augmenting cytotoxic T-cell (CTL) responses and maintaining immunologic memory against tumor cells expressing melanoma-specific antigens. The 6MHP vaccine may also induce a CD8+ T-cell response through epitope spreading, potentially priming subsequent immune responses against tumor cells.

A racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities. Although the exact mechanism of action is unknown, 6,8-bis(benzylthio)octanoic acid has been shown to inhibit metabolic and regulatory processes required for cell growth in solid tumors. Both enantiomers in the racemic mixture exhibit antineoplastic activity.

A synthetic triazine analogue of uridine with antimetabolite activity. 6-azauridine inhibits de novo pyrimidine synthesis and DNA synthesis and is converted intracellularly into mono, di-, and triphosphate derivatives, which incorporate into RNA and inhibit protein synthesis.

An inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) and derivative of 3-(3-pyridinyl)-1-[4-pyridinyl]-2-propen-1-one (3PO), with potential antineoplastic activity. Upon administration, PFKFB3 inhibitor PFK-158 binds to and inhibits the activity of PFKFB3, which leads to the inhibition of both the glycolytic pathway in and glucose uptake by cancer cells. This prevents the production of macromolecules and energy that causes the enhanced cellular proliferation in cancer cells as compared to that of normal, healthy cells. Depriving cancer cells of nutrients and energy leads to the inhibition of cancer cell growth. PFKFB3, an enzyme that catalyzes the conversion of fructose-6-phosphate to fructose-2,6-bisphosphate, is highly expressed and active in human cancer cells; it plays a key role in increasing both glycolytic flux in and proliferation of cancer cells.

A selective, orally bioavailable inhibitor of 17beta-hydroxysteroid dehydrogenase type 5 (17bHSD5, aldo-keto reductase 1C3; AKR1C3), with potential antineoplastic activity. Upon administration, ASP9521 selectively binds to and inhibits the activity of 17bHSD5. This prevents the conversion of the adrenal androgens dehydroepiandrosterone and androstenedione into 5-androstenediol and testosterone. By blocking testosterone production, ASP9521 may inhibit the growth of testosterone-dependent cancers such as castration-resistant prostate cancer (CRPC). 17bHSD5, expressed both in normal prostate tissue and in prostate cancer (PC), plays a crucial role in persistent production of androgens despite castration; its expression is associated with increased malignancy of PC.

A semisynthetic analogue of the Streptomyces melanovinaceus-derived tetracyclic antitumor antibiotic quinocarmycin with potential antineoplastic activity. Quinocarmycin belongs to the naphthyridinomycin/saframycin class of antitumor antibiotics. These antibiotics appear to act through DNA alkylation.

A synthetic derivative of staurosporine with antineoplastic activity. 7-hydroxystaurosporine inhibits many phosphokinases, including the serine/threonine kinase AKT, calcium-dependent protein kinase C, and cyclin-dependent kinases. This agent arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis.

A topical gel containing a peptide derived from the human papillomavirus (HPV). Application of 851B gel may stimulate the host immune system to trigger a cytotoxic T-lymphocyte response to cells that express HPV.

A synthetic imidazoquinoline Toll-like receptor 7 (TLR7) agonist with immunostimulating and potential antitumor activities. TLR7 agonist 852A binds to and activates TLR7, thereby stimulating plasmacytoid dendritic cells (pDC) through the TLR7-MyD88-dependent signaling pathway. Activation of pDC results in secretion of interferon alpha, the production of proimflammatory cytokines, the upregulation of co-stimulatory molecules, and enhanced T and B-cell stimulatory responses.

An ointment formulation containing the sulfate salt of 8-hydroxyquinoline in a petrolatum and lanolin base with skin-protecting activity. Upon topical application, 8-hydroxyquinoline sulfate exhibits antiseptic activity while lanolin moisturizes and softens skin.


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