Dictionary of drugs: O
Dictionary of pharmaceutical drugs/medications sorted alphabetically
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- C | C1 | C2
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- 0 - 9
Drug dictionary O
A guanine analogue with antineoplastic activity. O(6)-benzylguanine binds the DNA repair enzyme O(6)-alkylguanine DNA alkyltransferase (AGT), transferring the benzyl moiety to the active-site cysteine and resulting in inhibition of AGT-mediated DNA repair. Co-administration of this agent potentiates the effects of other chemotherapeutic agents that damage DNA.
A biscuit containing oats.
The mesylate salt of obatoclax, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon.
A glycoengineered, humanized IgG1 monoclonal antibody with potential antineoplastic activity. Obinutuzumab, a third generation type II anti-CD20 antibody, selectivity binds to the extracellular domain of the human CD20 antigen on malignant human B cells. The Fc region carbohydrates of the antibody, enriched in bisected non-fucosylated glycosylation variants, contribute to its higher binding affinity for human FcgammaRIII receptors compared to non-glycoengineered antibodies, resulting in enhanced antibody-dependent cellular cytotoxicity (ADCC) and caspase-independent apoptosis. In addition, modification of elbow hinge sequences within the antibody variable framework regions may account for the strong apoptosis-inducing activity of R7159 upon binding to CD20 on target cells.
The sodium salt of a phosphorothioate antisense oligonucleotide targeted to the initiation codon region of mRNA for the anti-apoptotic gene Bcl-2. Oblimersen inhibits Bcl-2 mRNA translation, which may result in decreased expression of the Bcl-2 protein and tumor cell apoptosis. This agent may enhance the efficacy of standard cytotoxic chemotherapy. The anti-apoptotic bcl-2 protein is an integral outer mitochondrial membrane protein (OMMP) that is overexpressed in some cancer cell types and is linked to tumor drug resistance.
An Fc-engineered monoclonal antibody directed against human CD20 with potential antineoplastic activity. Ocaratuzumab specifically binds to CD20 antigen (B1), preventing mitogen-induced B-cell proliferation; inhibiting B-cell differentiation; and promoting antibody-dependent cell-mediated cytotoxicity (ADCC) and apoptosis of B cells expressing CD20. The Fc portion of this monoclonal antibody has been engineered to possess a higher binding affinity for variant Fc receptors on T helper cells, resulting in an augmentation of the anti-tumor immune response. Because of Fc engineering, this agent may be significantly more potent than rituximab in inducing B cell-directed ADCC. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development.
A Fc-modified, humanized monoclonal antibody directed against the B-cell CD20 cell surface antigen, with immunosuppressive activity. Ocrelizumab binds to CD20 on the surfaces of B-cells, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) of B-cells overexpressing CD20. The CD20 antigen, a non-glycosylated cell surface phosphoprotein that acts as a calcium ion channel, is found on over 90% of B-cells, B-cell lymphomas, and other lymphoid tumor cells of B-cell origin; it plays an important role in B-cell functioning.
Brand name for indium In 111 pentetreotide
The acetate salt of a synthetic long-acting cyclic octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin. Octreotide is a more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Similar to somatostatin, this agent also suppresses the luteinizing hormone response to gonadotropin-releasing hormone, decreases splanchnic blood flow, and inhibits the release of serotonin, gastrin, vasoactive intestinal peptide (VIP), secretin, motilin, pancreatic polypeptide, and thyroid stimulating hormone.
A synthetic long-acting octapeptide analogue of endogenous somatostatin. Octreotide pamoate binds to somatostatin receptors expressed by some neuroendocrine and non-neuroendocrine tumor cells, thereby initiating somatostatin receptor-mediated apoptosis. Other possible antineoplastic activities of this agent include suppression of tumor angiogenesis and tumor growth-promoting insulin-like growth factor 1 (IGF-1).
An inhibitor of cathepsin K with potential anti-osteoporotic activity. Odanacatib selectively binds to and inhibits the activity of cathepsin K, which may result in a reduction in bone resorption, improvement of bone mineral density, and a reversal in osteoporotic changes. Cathepsin K, a tissue-specific cysteine protease that catalyzes degradation of bone matrix proteins such as collagen I/II, elastin, and osteonectin plays an important role in osteoclast function and bone resorption.
Brand name for sonidegib OEPA regimen]] A regimen consisting of vincristine, etoposide, prednisone and doxorubicin for the treatment of male patients with childhood Hodgkin lymphoma.
Brand name for diethylstilbestrol
Brand name for diethylstilbestrol
Brand name for diethylstilbestrol
A fully human, high-affinity IgG1 monoclonal antibody directed against the B cell CD20 cell surface antigen with potential antineoplastic activity. Ofatumumab binds specifically to CD20 on the surfaces of B cells, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) of B cells overexpressing CD20. The CD20 antigen, found on over 90% of B cells, B cell lymphomas, and other B cells of lymphoid tumors of B cell origin, is a non-glycosylated cell surface phosphoprotein that acts as a calcium ion channel; it is exclusively expressed on B cells during most stages of B cell development.
A chemotherapy regimen that includes leucovorin, 5-fluorouracil and oxaliplatin, which may be used in the treatment of pancreatic cancer. ofloxacin]] A fluoroquinolone antibacterial antibiotic. Ofloxacin binds to and inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, enzymes involved in DNA replication and repair, resulting in cell death in sensitive bacterial species.
Brand name for trastuzumab oglufanide disodium]] The disodium salt of a synthetic form of a naturally-occurring dipeptide consisting of L-glutamic acid and L-tryptophan with potential antiangiogenic and potential immunomodulating activities. Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitic C virus and intracellular bacterial infections.
A synthetic derivative of thienobenzodiazepine with antipsychotic, antinausea, and antiemetic activities. As a selective monoaminergic antagonist, olanzapine binds with high affinity binding to the following receptors: serotoninergic, dopaminergic, muscarinic M1-5, histamine H1, and alpha-1-adrenergic receptors; it binds weakly to gamma-aminobutyric acid type A, benzodiazepine, and beta-adrenergic receptors. The antinausea and antiemetic effects of this agent appear to be due to the blockade of 5-HT2 and 5-HT3 receptors for serotonin. Although its exact mechanism of action in schizophrenia is unknown, it has been proposed that olanzapine's antipsychotic activity is mediated through antagonism to dopamine D2 receptors with rapid ligand-receptor dissociation kinetics that help to minimize extrapyramidal symptoms (EPS). Olanzapine may also stimulate appetite.
A small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.
A 45-mer L-stereoisomer RNA oligonucleotide linked to a 40 kDa polyethyleneglycol that targets the small chemokine stromal cell-derived factor 1 (SDF-1 or CXCL12) with potential antineoplastic and hematopoietic stem cell-mobilization activities. Olaptesed pegol specifically binds to SDF-1 thereby preventing the binding of SDF-1 to its receptors CXCR4 and CXCR7, and blocking the subsequent receptor activation. This may prevent angiogenesis, tumor cell proliferation, invasion and metastasis and could sensitize tumor cells to chemotherapy. In addition, inhibition of SDF-1/CXCR4 interaction may induce mobilization of hematopoietic cells from the bone marrow into blood. The unique mirror-image configuration of this agent renders it resistant to hydrolysis and does not hybridize with native nucleic acids. Furthermore, this agent does not induce the innate immune response and has shown a favorable immunogenicity profile.
A fully human IgG1 monoclonal antibody directed against the platelet-derived growth factor receptor alpha (PDGFR alpha) with potential antineoplastic activity. Olaratumab selectively binds to PDGFR alpha, blocking the binding of its ligand, PDGF; signal transduction downstream of PDGFR through the MAPK and PI3K pathways is inhibited, which may result in inhibition of angiogenesis and tumor cell proliferation. Overexpressed by various cancer cell types, PDGFR is a transmembrane protein tyrosine kinase receptor, consisting of isoforms A and B, that is important in regulating cellular growth and differentiation and angiogenesis.
A lipid soluble cardiac glycoside with potential antineoplastic activity. Upon administration, oleandrin specifically binds to and inhibits the alpha3 subunit of the Na/K-ATPase pump in human cancer cells. This may inhibit the phosphorylation of Akt, upregulate MAPK, inhibit NF-kb activation and inhibit FGF-2 export and may downregulate mTOR thereby inhibiting p70S6K and S6 protein expression. All of this may lead to an induction of apoptosis. As cancer cells with relatively higher expression of the alpha3 subunit and with limited expression of the alpha1 subunit are more sensitive to oleandrin, one may predict the tumor response to treatment with lipid-soluble cardiac glycosides such as oleandrin based on the tumors Na/K-ATPase pump protein subunit expression. Overexpression of the alpha3 subunit in tumor cells correlates with tumor proliferation.
A monoclonal antibody against the ectoenzyme CD73 (cluster of differentiation 73), also known as 5'-nucleotidase (5'-NT; ecto-5'-nucleotidase) with potential antineoplastic activity. Upon administration, oleclumab targets and binds to CD73, leading to clustering of and internalization of CD73. This prevents CD73-mediated conversion of adenosine monophosphate (AMP) to adenosine and decreases the amount of free adenosine. This prevents adenosine-mediated lymphocyte suppression and increases the activity of CD8-positive effector cells. This also activates macrophages, and reduces both myeloid-derived suppressor cells (MDSCs) and regulatory T-lymphocytes. By abrogating the inhibitory effect on the immune system and enhancing the cytotoxic T-cell-mediated immune response against cancer cells, tumor cell growth decreases. In addition, clustering and internalization of CD73 decreases the migration of cancer cells and prevents metastasis. CD73, a plasma membrane protein upregulated on a number of cancer cell types, catalyzes the conversion of extracellular nucleotides, such as AMP, to membrane-permeable nucleosides, such as adenosine; it plays a key role in adenosine-mediated immunosuppression within the tumor microenvironment.
A mixture of non-digestible carbohydrates, containing the fermentable plant fructans oligosaccharide and inulin, with potential prebiotic activity. Resisting hydrolysis by intestinal digestive enzymes, inulin and oligofructose serve as growth media and energy substrates for bifidobacteria in the colon; beneficial colonic commensal bacteria such as bifidobacteria may inhibit the colonization of the intestine by pathogenic bacteria and have been inplicated to inhibit colon carcinogenesis. Oligofructose-enriched inulin may be administered in combination with probiotic bifidobacteria. In addition, this agent may promote the absorption of calcium and magnesium from the gastrointestinal tract.
A preparation containing plant-derived polyphenolic bioflavonoids composed of multimers (dimers, trimers, or higher order polymers) of the flavan-3-ol-based monomers catechin and epicatechin that are extracted from sources rich in these chemicals (such as grape seeds, grape skin and pine bark), with potential anti-oxidant, anti-inflammatory, anti-microbial, anti-cancer and protective activities. Upon oral administration of oligomeric procyanidin complex (OPC), the polyphenols exert anti-oxidant activity by scavenging free radicals, which prevents both the formation of reactive oxygen species (ROS), particularly nitrous oxide (NO), and DNA damage. OPC also inhibits chemical-induced lipid peroxidation. In addition, OPC reduces the production of advanced glycation end-products (AGEs), decreases AGE accumulation in tissues, and inhibits the progression of AGE/receptor for AGE (RAGE)-mediated inflammatory transduction pathways, which inhibits the activation of pro-inflammatory transcriptional regulators, and prevents the secretion of pro-inflammatory cytokines/chemokines. This ultimately prevents inflammatory-driven damage to end organs and may reduce inflammation-induced cancer formation and progression. In addition, OPC inhibits the activity of a variety of enzymes, including xanthine oxidase, collagenase, elastase, hyaluronidase and beta-glucuronidase.
A synthetic antisense oligonucleotide against Bcl-2 messenger RNA with potential antitumor activity. Oligonucleotide SPC2996 binds to and inactivates Bcl-2 mRNA, thereby inhibiting the expression of Bcl-2 protein, promoting tumor cell apoptosis, and potentially enhancing the efficacy of standard cytotoxic chemotherapy. Linked to tumor drug resistance, the antiapoptotic protein Bcl-2 is upregulated in several types of cancers.
Produced by pressing olives, olive oil has a high content of monounsaturated fats, thought beneficial for health. Major components of the phenolic fraction of olive oil, lignans and pinoresinols are potent antioxidants present in extra virgin (first pressed) oils. Containing vitamins E and F, other antioxidant compounds, foods containing high amounts of lignan precursors may be protective against breast, colon, and prostate cancer, as well as heart diseases. Used mainly in cooking today, olive oil has been used for medicines and in cosmetics.
A capsule containing an extract of olive oil, rich in polyphenols and curcumin, the polyphenol derived from the plant Curcuma longa, also known as turmeric, with potential anti-neoplastic, -angiogenic, -inflammatory, -oxidant and chemopreventive activities. The olive oil extract/curcumin-based capsule is rich in phytonutrients, especially polyphenols. Upon oral administration, the polyphenols, and other active ingredients in this supplement may exert anti-inflammatory activity by decreasing the production of inflammation mediators, such as TNF-alpha, interleukin (IL) 1-beta, IL-6, IL-10, interferon gamma, thromboxane B2, and leukotriene B4. They also inhibit a variety of pro-inflammatory enzymes, such as cyclooxygenase 1 (COX-1) and COX-2, block the formation of reactive-oxygen species and neutralize free radicals. In addition, curcumin and some other polyphenols disrupt cell signal transduction pathways involved in carcinogenesis. Specifically, curcumin inhibits cell invasion by inhibiting matrix metalloproteinase-9 (MMP-9) expression by suppressing NF-kB and AP-1 activation.
An injectable, isotonic, nutritional lipid emulsion composed of approximately 80% refined olive oil and 20% refined soybean oil, used for parenteral nutrition. The olive oil/soya oil/egg lecithin emulsion provides about 15% of saturated fatty acids (SFA), 65% of mono-unsaturated fatty acids (MUFA) and 20% of essential poly-unsaturated fatty acids (EPUFA). Upon parenteral administration, the emulsion supplies calories, for energy, and essential fatty acids that can be incorporated into cell membranes. The fatty acids may decrease the production of certain pro-inflammatory cytokines, including interleukin 1 (IL-1), IL-6 and tumor necrosis factor (TNF). In addition to olive oil and soya oil, this lipid emulsion contains egg lecithin and provides phosphorus and choline, which are needed to maintain cell membrane integrity.
An orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild type form.
Brand name for simeprevir
A semisynthetic formulation of the cytotoxic plant alkaloid homoharringtonine isolated from the evergreen tree Cephalotaxus with potential antineoplastic activity. Omacetaxine mepesuccinate binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. This agent also induces differentiation and apoptosis in some cancer cell types.
A humanized monoclonal antibody directed against the C-epsilon 3 domain of immunoglobulin E. Olizumab binds to this IgE domain, thereby preventing IgE from binding to its high-affinity mast-cell receptor.
An orally bioavailable combination agent containing ombitasvir, an inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, paritaprevir, a synthetic acylsulfonamide inhibitor of the HCV protease complex comprised of non-structural protein 3 and 4A (NS3/NS4A), and the cytochrome P450 (CYP) 3A4 inhibitor ritonavir, with potential activity against HCV. Upon oral administration of ombitasvir/paritaprevir/ritonavir, ombitasvir, enters the cell and binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. After intracellular uptake, paritaprevir reversibly binds to the active center and binding site of the HCV NS3/NS4A protease and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts both the processing of viral proteins and the formation of the viral replication complex, which inhibits viral replication in HCV genotype 1-infected host cells. Although ritonavir is not active against HCV, it strongly inhibits the activity of CYP3A4, thereby blocking the degradation of paritaprevir, which is a CYP3A4 substrate. This leads to an increased concentration and half-life of paritaprevir as compared to the administration of paritaprevir without ritonavir. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. NS3, a serine protease essential for the proteolytic cleavage of multiple sites within the HCV polyprotein, plays a key role during HCV ribonucleic acid (RNA) replication. NS4A is an activating factor for NS3. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family, and infection is associated with the development of hepatocellular carcinoma (HCC).
A synthetic water-soluble analogue of combretastatin A4, derived from the South African willow bush (Combretum caffrum), with potential vascular-disrupting and antineoplastic activities. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrata, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis.
Any fatty acid that contains an unsaturated bond originating from the 3rd carbon from the methyl end. Omega-3 fatty acids do not occur naturally with chain lengths shorter than 16 carbon units.
An ethyl ester form of omega-3 fatty acid derived from fish oil, with activity in decreasing serum triglyceride levels. Although its mechanism of action isn't known, omega-3-acid ethyl esters may work by decreasing the amount of triglycerides and other fats made in the liver.
A benzimidazole with selective and irreversible proton pump inhibition activity. Omeprazole forms a stable disulfide bond with the sulfhydryl group of the hydrogen-potassium (H+ - K+) ATPase found on the secretory surface of parietal cells, thereby inhibiting the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen and suppressing gastric acid secretion. This agent exhibits no anticholinergic activities and does not antagonize histamine H2 receptors.
A pentahydrochloride salt of omiganan, a synthetic cationic antimicrobial peptide with wide-spectrum activity against both gram-positive and gram-negative bacteria and fungi. Omiganan pentahydrochloride, an analog of indolicidin, acts by disrupting bacterial cytoplasmic membranes and has been tested in a topical gel for the prevention of catheter-related bloodstream infections.
Brand name for iohexol
Brand name for gadodiamide
A humanized monovalent monoclonal antibody directed against the hepatocyte growth factor receptor (c-Met) with potential antineoplastic activity. Onartuzumab binds to the extracellular domain of c-Met, preventing the binding of its ligand, hepatocyte growth factor (HGF); the activation of the c-Met signaling pathway is thus inhibited, which may result in cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase, is overexpressed on the cell surfaces of a variety of cancer cell types and may play a key role in their proliferation, invasion and survival.
Brand name for pegaspargase
Brand name for PGLA/PEG copolymer-based paclitaxel
Brand name for octreotide pamoate
An adenovirus serotype 5 strain, selectively replication competent in cells defective in the Rb/p16 tumor suppressor pathway, with potential oncolytic activity. Oncolytic adenovirus Ad5-Delta 24RGD contains an integrin binding RGD-4C motif, allowing Coxsackie adenovirus receptor-independent infection of tumor cells, which are often deficient for Coxsackie and adenovirus receptors (CARs). Selectively replication competent in cells that are defective in retinoblastoma gene (Rb) or cyclin-dependent kinase inhibitor-2A (p16), active replication of oncolytic adenovirus Ad5-Delta 24RGD in tumor cells may induce oncolysis or cell lysis. As integral components of the late G1 restriction point, the Rb gene product and p16 are negative regulators of the cell cycle; ovarian cancer cells and non-small cell lung cancer cells may be defective in the Rb/p16 pathway.
A genetically modified oncolytic viral strain of human adenovirus (Ad) with potential immunostimulating and antineoplastic activities. Upon intratumoral administration, the oncolytic adenovirus CAdVEC selectively infects and replicates in tumor cells, leading to tumor cell lysis. Additionally, CAdVEC has been genetically modified to express currently undisclosed immunomodulatory molecules that may enhance the anti-tumor effects of endogenous T lymphocytes as well as adoptively transferred chimeric antigen receptor (CAR) T cells.
A recombinant oncolytic adenovirus encoding the immunohematopoietic cytokine granulocyte-macrophage colony stimulating factor (GM-CSF) with potential antineoplastic activity. Upon administration, the oncolytic adenovirus selectively infects and replicates in tumor cells, which may result in tumor cells lysis. Synergistically, GM-CSF (sargramostim) expressed by the oncolytic adenovirus may promote a cytotoxic T cell response against tumor cells harboring the oncolytic adenovirus, resulting in an immune-mediated tumor cell death.
Bone marrow-derived autologous mesenchymal stem cells (MSCs) infected with the oncolytic, replication-competent adenovirus ICOVIR5, with potential antineoplastic activity. Upon infusion of the oncolytic adenovirus ICOVIR5-infected autologous MSCs, these cells target the adenovirus to tumors. The oncolytic virus then selectively transfects and replicates in the tumor cells causing a direct cytotoxic effect and lysis of the tumor cells. In addition, the viral infection may stimulate an immune response against the virally-infected tumor cells. This may lead to an inhibition of cancer cell proliferation. ICOVIR-5, a virus derived from wild-type human adenovirus serotype 5 (Had5), has been modified to selectively replicate in tumor cells that have a deregulated retinoblastoma/E2F pathway.
An ICP34.5-, ICP47-deleted, oncolytic herpes simplex type-1 virus (HSV-1) isolated from the mouth of an HSV-1-infected patient of Chinese Han ethnicity, and encoding the immunostimulating factor cytokine granulocyte-macrophage colony stimulating factor (GM-CSF) with potential immunostimulating and antineoplastic activities. Upon administration, the recombinant human GM-CSF HSV-1 selectively infects and replicates in tumor cells, thereby inducing tumor cell lysis. In addition, GM-CSF attracts dendritic cells (DCs) and may stimulate a cytotoxic T cell response against tumor cells, which results in immune-mediated tumor cell death. Deletion of the gene encoding for ICP34.5 provides tumor selectivity and prevents replication in healthy cells. As ICP47 blocks antigen presentation in HSV-infected cells, deletion of this gene may induce a more potent antitumor immune response in the tumor cells. Additionally, deletion of ICP47 causes increased expression of the HSV US11 gene and allows US11 to be expressed as an immediate early and not a late gene. This further enhances the degree of viral replication and oncolysis of tumor cells. Interruption of the ICP6 gene, which encodes the large subunit of the viral ribonucleotide reductase, in the viral vector also enhances selective replication in tumor cells.
A neuroattenuated, replication-competent, recombinant and genetically-engineered herpes simplex virus type 1 (HSV-1), with potential oncolytic and immunostimulating activities. In rQNestin34.5v.2, the UL39 gene encoding for the viral ribonucleotide reductase large subunit infected cell protein 6 (ICP6) and both endogenous copies of the gamma34.5 gene that encodes for the RL1 neurovirulence protein infected cell protein 34.5 (ICP34.5), which is needed for robust viral growth in an infected cell, are deleted, and one copy of the gamma34.5 gene is reinserted under control of a nestin promoter, which is selectively activated in gliomas. Upon intratumoral administration, oncolytic HSV-1 rQNestin34.5v.2 preferentially infects and replicates within the rapidly dividing, glioma cells, thereby directly lysing tumor cells. The released virus particles, in turn, infect and replicate in neighboring tumor cells, thereby further killing tumor cells. rQNestin34.5v.2 also elicits a tumor-specific systemic immune and cytotoxic T-lymphocyte (CTL) response, thereby killing nearby non-infected tumor cells. By inactivating UL39, viral ribonucleotide reductase activity is disrupted, resulting in the inhibition of nucleotide metabolism and viral DNA synthesis in non-dividing, healthy cells but not in dividing cells. Glioma-selective expression of ICP34.5 imparts tumor selectivity by preventing replication in healthy cells.
A gene therapy agent containing an attenuated, replication-competent, genetically engineered mutant form of the Herpes simplex virus 1 (HSV-1) strain KOS with potential antineoplastic activity. Upon infusion into the hepatic artery, oncolytic HSV-1 rRp450 replicates in hepatocellular carcinoma (HCC) cells and exerts direct cytotoxic effects eventually disrupting cancer cell membranes and liberating progeny virions thereby infecting adjacent tumor cells. In addition, rRp450 expresses the cytochrome P450 transgene that activates oxazaphosphorines, such as cyclophosphamide (CPA). Therefore, CPA can become activated in the presence of rRp450 and exert its antineoplastic effect. rRp450 is deleted for the HSV-1 gene UL39, encoding the viral ribonucleotide reductase large subunit infected cell protein 6 (ICP6), thereby disrupting the activity of viral ribonucleotide reductase and resulting in the inhibition of nucleotide metabolism and viral DNA synthesis in nondividing cells but not in dividing cells. UL39 is replaced by the rat CYP2B1 gene, encoding a cytochrome P450 enzyme that activates oxazaphosphorines. rRp450 also expresses viral thymidine kinase, which activates the cancer prodrug ganciclovir.
A neuroattenuated, replication-restricted, ICP34.5 deleted (RL1 gene)-mutant herpes simplex virus (HSV) type I, constructed from wild-type strain 17, with potential oncolytic activity. Upon intratumoral injection, oncolytic HSV1716 transfects, replicates in, and lyses rapidly dividing cells such as tumor cells. Because the RL1 gene is deleted , HSV1716 is unable to replicate in non-dividing cells.
An attenuated oncolytic Edmonston (Ed) strain of measles virus encoding the human thyroidal sodium iodide symporter (MV-NIS) with potential gene expression and antineoplastic activities. After attachment to and fusion with host tumor cell membranes, MV-NIS may induce tumor cell syncytia and tumor cell lysis. When combined with iodine 123 (I-123), expressed NIS facilitates uptake of I-123 by MV-NIS-infected tumor cells, allowing noninvasive imaging of these cells. MV-NIS may also enhance the oncolytic activity of MV against radiosensitive tumor cells by facilitating the uptake of iodine 131 (I-131) by MV-NIS-infected cells. The cellular receptor for MV is the human CD46 antigen, a type 1 integral membrane glycoprotein found on nearly all human tissues and overexpressed on many cancer cell types.
An oncolytic viral agent containing the oncolytic, live-attenuated strain of the paramyxovirus Newcastle disease virus (NDV), with potential antineoplastic activity. Upon administration, NDV specifically infects and replicates in cancer cells. This may result in a direct cytotoxic effect involving the lysis of tumor cells via apoptotic mechanisms and may eventually lead to an inhibition of cancer cell proliferation.
A modified, replicative oncolytic vaccinia virus (VV), deleted of the genes for tyrosine kinase (TK) and ribonucleotide reductase (RR), and expressing the yeast-originated, bifunctional cytosine deaminase/uracil phosphoribosyltransferase gene (FCU1), with potential immunomodulating and antineoplastic activities. Upon intravenous administration of the oncolytic vaccinia virus TG6002, the virus preferentially targets and infects tumor cells, causing oncolysis. In turn, the lysed tumor cells release various tumor-associated antigens (TAAs), which induce an immune response against the tumor cells. Upon concomitant administration of the non-cytotoxic prodrug flucytosine (5-fluorocytosine; 5-FC), the FCU1 expressed in the infected cancer cells produce the enzymes cytosine deaminase and uracil phosphoribosyltransferase which catalyze the conversion of 5-FC into the cytotoxic forms 5-fluorouracil (5-FU) and 5-fluoro-uridilyl monophosphate (5-FUMP); 5-FU and 5-FUMP exert a cytotoxic effect in the infected tumor cells. Double gene deletion (TK-RR-) restricts the propagation of TG6002 to the tumor cells, thereby reducing toxicity to normal cells.
A genetically modified oncolytic viral strain of the herpes simplex type 1 (HSV-1) virus, with potential oncolytic, immunostimulating and antineoplastic activities. Upon administration, the oncolytic virus RP1 specifically targets, infects and replicates in tumor cells only while not infecting normal, healthy cells. This induces tumor cell lysis. The released virus particles, infect and replicate in neighboring tumor cells, thereby further killing tumor cells. The released tumor-associated antigens (TAAs) from the tumor cells activate the immune system to exert an anti-tumor immune response against the tumor cells, thereby further killing the tumor cells. The virus itself also elicits a tumor-specific systemic immune and cytotoxic T-lymphocyte (CTL) response, thereby killing nearby non-infected tumor cells. In RP1, ICP34.5 and 47 proteins of the HSV1 strain have been deleted; RP1 expresses a fusogenic protein for optimal tumor cell infection and killing.
Brand name for ranpirnase
Brand name for vitespen
Brand name for PSA prostate cancer vaccine
Brand name for green tea extract-based antioxidant supplement
A carbazole derivative with antiemetic activity. As a selective serotonin receptor antagonist, ondansetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
The hydrochloride salt of the racemic form of ondansetron, a carbazole derivative and a selective, competitive serotonin 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist with antiemetic activity. Although its mechanism of action has not been fully characterized, ondansetron appears to competitively block the action of serotonin at 5HT3 receptors peripherally in the gastrointestinal tract as well as centrally in the area postrema of the CNS, where the chemoreceptor trigger zone (CTZ) for vomiting is located, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
Brand name for irinotecan hydrochloride liposome
Brand name for laromustine
Brand name for fentanyl buccal soluble film
Brand name for denileukin diftitox
An orally bioavailable, adenosine triphosphate (ATP) competitive inhibitor of polo-like kinase 1 (PLK1; PLK-1; STPK13), with potential antineoplastic activity. Upon administration, onvansertib selectively binds to and inhibits PLK1, which disrupts mitosis and induces selective G2/M cell-cycle arrest followed by apoptosis in PLK1-overexpressing tumor cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine kinase that is crucial for the regulation of mitosis, and plays a key role in tumor cell proliferation. PLK1 expression is upregulated in a variety of tumor cell types and high expression is associated with increased aggressiveness and poor prognosis.
Brand name for ethylene-vinyl alcohol copolymer-based embolic agent
An E1B-55kDa-deleted adenovirus that is able to selectively replicate in and lyse TP53-deficient human tumor cells. After tumor cell lysis, released viruses infect neighboring tumor cells, tripping a chain of ONYX-015-mediated tumor cell cytotoxicity.
An orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. Upon administration, opaganib competitively binds to and inhibits SK2, thereby preventing the phosphorylation of the pro-apoptotic amino alcohol sphingosine to sphingosine 1-phosphate (S1P), the lipid mediator that is pro-survival and critical for immunomodulation. This may eventually lead to the induction of apoptosis and may result in an inhibition of cell proliferation in cancer cells overexpressing SK2. SK2 and its isoenzyme SK1 are overexpressed in numerous cancer cell types.
Brand name for oxymorphone hydrochloride
OPCs/green tea,/spirullina/curcumin/antrodia camphorate/fermented soymilk extract capsule A capsule containing a fermented soymilk extract and oligomeric proanthocyanidins (OPCs), green tea, spirullina, curcumin and antrodia camphorate powder, with potential antioxidant, immunomodulating, anti-infective and anti-cancer activities. OPCs/green tea/spirullina/curcumin/antrodia camphorate/fermented soymilk extract capsule may boost the immune system and may alleviate fatigue and poor appetite in cancer chemotherapy patients.
An injectable formulation composed of opebacan, a 21 kDa recombinant fragment of human bactericidal/permeability-increasing protein (BPI), with potential anti-infective activity. Upon intravenous administration, opebacan is able to mimic BPI and binds to and neutralizes lipopolysaccharides (LPS or endotoxins), which are components of the cell wall of gram-negative bacteria that induce a potent innate immune response. This may prevent an endotoxin-mediated inflammatory response and may prevent graft-versus-host-disease (GvHD) after myeloablative allogeneic hematopoietic stem cell transplantation (aHSCT). BPI, a host-defense protein against microbial infection, is naturally produced by neutrophils. Chemotherapy and radiation therapy induce neutropenia and depletion of endogenous BPI. These therapies also cause intestinal damage and release of bacterial endotoxins into the bloodstream, which initiate a systemic inflammatory response, activate donor T-lymphocytes and possibly cause GvHD following aHSCT.
A sulfonate-based salt form of a trimebutine derivative, an orally available, peripherally-acting opioid agonist and muscarinic antagonist, with potential visceral analgesic activity. Upon oral administration of GIC-1001, this agent may exert its therapeutic effects through the potential mechanisms of action for the trimebutine and sulfonate moieties: The trimebutine moiety can act as a motility enhancer in the gastrointestinal (GI) tract, as an antispasmodic agent to reduce colonic spasms, as an agonist of colonic mu and kappa opioid receptors, which could provide an analgesic effect, and blocks sodium channels and the release of a variety of GI peptides, which modulates the activity of visceral afferents. The sulfonate moiety releases hydrogen sulfide (H2S), which is involved, through an as of yet not fully elucidated mechanism of action, in the modulation of visceral perception and pain, possibly through the activation of ATP-sensitive potassium (KATP) ion channels and mu opioid receptors. Altogether, administration of this agent may both facilitate the insertion of the colonoscope during a colonoscopy and reduce colonic spasms and pain.
An orally available, peripherally-acting opioid agonist, with potential visceral analgesic activity. Upon oral administration of GIC-1002, this agent binds to colonic mu and kappa opioid receptors causing analgesic effects.
An endogenous pentapeptide with potential antineoplastic and antiangiogenic activities. Opioid growth factor (OGF) binds to and activates the opioid growth factor receptor (OGFr), present on some tumor cells and vascular cells, thereby inhibiting tumor cell proliferation and angiogenesis.
Also known as laudanum and formulated for oral administration, opium tincture is made of air-dried poppy (Papaver somniferum) latex and contains alkaloids such as morphine and codeine. As an antidiarrheal agent, it slows transit of intestinal contents by increasing intestinal smooth muscle tone and inhibiting motility; water is absorbed from fecal contents, decreasing diarrhea.
A fusion protein immunotoxin consisting of a humanized, single-chain monoclonal antibody fragment specific for the epithelial cell adhesion molecule (EpCAM) conjugated with a truncated form of Pseudomonas exotoxin A with potential antineoplastic activity. Oportuzumab monatox binds to Ep-CAM-positive tumor cells, thereby delivering the Pseudomonas exotoxin A moiety specifically; the Pseudomonas exotoxin A moiety then inactivates elongation factor 2 (EF-2) through ADP ribosylation, resulting in inhibition of protein synthesis in target cells. EpCAM, a cell surface protein, is expressed by a variety of tumor cells and is frequently found in head and neck cancers.
A regimen consisting of vincristine, prednisone, procarbazine and doxorubicin (OPPA) used in combination with radiation therapy for the treatment of female patients with childhood Hodgkin lymphoma with low-risk features.
A recombinant therapeutic agent which is chemically identical to or similar to the endogenous cytokine interleukin 11 (IL-11). Secreted by bone marrow stromal cells and a number of mesenchymal cells, IL-11 binds to and activates its cell-surface receptor, promoting primary and secondary immune responses, modulating antigen-specific antibody reactions, and preventing apoptotic cell death. This agent also stimulates the T-cell-dependent development of IgG-secreting B-cells in spleen cell cultures and may be an important regulator of megakaryocytopoiesis.
An orally bioavailable proteasome inhibitor with potential antineoplastic activity. Oprozomib inhibits the activity of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome; this may result in an accumulation of unwanted or misfolded proteins. Disruption of various cell signaling pathways may follow, eventually leading to the induction of apoptosis and inhibition of tumor growth. Proteasomes are large protease complexes that degrade unneeded or damaged proteins that have been ubiquitinated.
Brand name for iodixanol
Brand name for Ioversol
Brand name for perflutren protein-type A microspheres
Brand name for sodium citrate
Brand name for oral docetaxel
A powder for an oral solution comprised of the hydrochloride salt of 5-aminolevulinic acid (ALA) with a potential application for photodynamic therapy. After oral administration, ALA is converted intracellularly into the photosensitizer protoporphyrin IX (PpIX). Upon exposure to light of appropriate wavelength (violet to blue range), excited PpIX emits a characteristic red fluorescence which could facilitate guided resection, and generates excited singlet oxygen molecules that could kill cells when appropriate laser dosage is applied. ALA is preferentially taken up by and accumulates in many types of cancer cells compared to normal, healthy cells. Consequently, cancer cells can be visualized and can be distinguished from normal, healthy cells.
An orally bioavailable formulation of azacitidine, a pyrimidine nucleoside analogue of cytidine, with antineoplastic activity. Upon oral administration, azacitidine is taken up by cells and metabolized to 5-azadeoxycitidine triphosphate. The incorporation of 5-azadeoxycitidine triphosphate into DNA reversibly inhibits DNA methyltransferase, and blocks DNA methylation. Hypomethylation of DNA by azacitidine may re-activate tumor suppressor genes previously silenced by hypermethylation, resulting in an antitumor effect. In addition, the incorporation of 5-azacitidine triphosphate into RNA disrupts normal RNA function and impairs tRNA (cytosine-5)-methyltransferase activity, resulting in an inhibition of RNA and protein synthesis.
An orally bioavailable, therapeutic cancer vaccine composed of the carbohydrate antigen sialyl-Lewis A (carbohydrate antigen 19-9; CA19.9; CA19-9) that is derived from pooled blood of pancreatic cancer patients, with potential immunomodulating activity. Upon oral administration of the oral pancreatic cancer vaccine V3-P, the CA19.9 antigens may stimulate the host immune system to mount a cytotoxic T-lymphocyte (CTL)-mediated immune response against pancreatic cancer cells expressing the CA19.9 antigen. CA19.9 is overexpressed on a number of different tumor cell types and plays a key role in tumor cell survival and metastasis.
An oral proprietary P-glycoprotein (P-gp) pump inhibitor-based formulation containing the taxane docetaxel, a semisynthetic analogue of paclitaxel, and a P-gp pump inhibitor, with potential antineoplastic activity. Upon administration of oral docetaxel, the P-gp pump inhibitor moiety, which is not absorbed, binds to the P-gp pump in the gastrointestinal (GI) tract and prevents the P-gp pump-mediated efflux of docetaxel from cells the docetaxel has been internalized by back into the GI tract. This decreases P-gp-mediated excretion and enhances absorption of docetaxel. Upon absorption, docetaxel binds specifically to the beta-tubulin subunit of the microtubule, stabilizes tubulin and inhibits microtubule disassembly, which results in cell-cycle arrest at the G2/M phase and cell death. The P-gp pump inhibitor enhances the bioavailability of certain poorly bioavailable agents and thereby allows oral administration of those agents. P-gp, an efflux membrane transporter, plays a key role in active drug export, and prevents cellular uptake and accumulation of certain substances.
An oral formulation of the phosphate salt of fludarabine, a synthetic purine nucleoside analogue antimetabolite with antineoplastic activity. Fudarabine is preferentially transported into malignant cells and metabolized by deoxycytidine kinase to its active form, 2-fluoro-ara-ATP; 2-fluoro-ara-ATP competes directly with deoxyadenosine triphosphate (dATP) and inhibits alpha DNA polymerase, RNA reductase, and DNA primase, which may result in inhibition of DNA synthesis and cell death.
An orally bioavailable formulation of the ansamycin derivative 17-amino-17-demethoxygeldanamycin (17-AG) with potential antineoplastic activity. Oral Hsp90 inhibitor IPI-493 binds to and inhibits Hsp90, which may result the in growth inhibition in sensitive tumor cell populations. Hsp90, a 90 kDa molecular chaperone, may be highly expressed in tumor cells, playing a key role in the conformational maturation, stability and function of other substrate or "client" proteins within the cell; many of these client proteins are involved in signal transduction, cell cycle regulation and apoptosis, and may include kinases, transcription factors and hormone receptors.
An orally bioavailable microencapsulated formulation of diindolylmethane, an indole phytonutrient found in cruciferous vegetables, with estrogen-modulating, antiandrogenic, and potential antineoplastic activities. As a dimer of indole-3-carbinol, diindolylmethane (DIM) modulates estrogen balance by reducing the levels of 16-hydroxy estrogen metabolites and increasing the formation of beneficial 2-hydroxy estrogen metabolites. DIM also antagonizes androgen receptor activity, which may result in diminished cell proliferation and apoptosis in susceptible tumor cell populations. Pure DIM, which is relatively hydrophobic, is poorly absorbed after oral administration. This oral formulation, which consists of DIM, d-alpha-tocopheryl acid succinate, phosphatidylcholine, and silica microencapsulated in starch, significantly improves the gastrointestinal absorption of DIM.
An orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors.
An edible, gel-based formulation containing an artificial saliva substitute, composed of water, electrolytes and buffering agents, with potential anti-xerostomia and protective activities. Upon application of the oral moisturizing jelly (OMJ), the natural electrolyte and pH balance of human saliva is restored, which increases moisture of mucosal tissues of the mouth, tongue and oropharynx. This relieves dryness, enhances lubrication, and increases salivary flow. OMJ makes it easier to chew, swallow and talk, and also prevents xerostomia-induced infections, as well as tooth decay.
An orally available therapeutic myoma vaccine containing pooled antigens derived from hydrolyzed, inactivated blood and tumor tissue samples from patients with uterine myoma, with potential antineoplastic and immunomodulatory activities. Upon oral administration, V3-myoma may stimulate the immune system to mount a cytotoxic T-lymphocyte-mediated response against cells expressing myoma-associated antigens. This may reduce the myoma growth and improve myoma-related symptoms.
An oral preparation of picoplatin, a third generation platinum compound with antineoplastic activity. Designed to overcome platinum drug resistance, picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and RNA transcription and the induction of apoptosis. Because of the increase in steric bulk around the platinum center, there is a relative reduction in the inactivation of picoplatin by thiol-containing species such as glutathione and metallothionein in comparison to cisplatin.
An aqueous solution composed of glucose and electrolytes, including sodium, potassium, chloride, magnesium, and phosphorus, with dehydration preventative and rehydration activities. Upon oral administration of the oral rehydration solution (ORS), water, electrolytes and glucose are absorbed from the gastrointestinal (GI) tract into the systemic circulation. This replenishes the body's supply of water, carbohydrates and electrolytes, and prevents both dehydration and renal dysfunction.
An orally active derivative of the short-chain fatty acid butyrate with potential antineoplastic activity. 4-Phenylbutyrate inhibits histone deacetylase, resulting in cell cycle gene expression modulation, reduced cell proliferation, increased cell differentiation, and apoptosis. This agent also initiates fragmentation of genomic DNA, resulting in decreased DNA synthesis and the inhibition of tumor cell migration and invasion.
An orally bioavailable therapeutic vaccine consisting of the tumor-associated antigen (TAA) oligosaccharide antigen sialyl Lewis A (CA19-9; sialylated Lewis A antigen; carbohydrate antigen 19-9; cancer antigen 19-9), with potential immunostimulating and antineoplastic activities. Upon oral administration, oral therapeutic vaccine V3-X induces a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells expressing CA19-9. CA19-9 is an antigen that is overexpressed in a variety of cancer cell types, and plays a key role in tumor cell survival and metastasis.
An oral formulation of the hydrochloride salt of topotecan, a semisynthetic derivative of the quinoline alkaloid camptothecin, with potential antineoplastic activity. Topotecan selectively inhibits topoisomerase I activity by stabilizing topoisomerase I-DNA covalent complexes during the S phase of the cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery.
Brand name for fentanyl citrate
Brand name for morphine sulfate
Brand name for morphine sulfate
An orally bioavailable receptor tyrosine kinase inhibitor. Orantinib binds to and inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), and fibroblast growth factor receptor (FGFR), thereby inhibiting angiogenesis and cell proliferation. Orantinib also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells.
Brand name for fluoxymesterone
Brand name for rubitecan
A combination formulation composed of a capsule containing the taxane compound paclitaxel and a tablet containing the multidrug resistance (MDR) efflux pump P-glycoprotein (P-gp) inhibitor HM30181A, with potential antineoplastic activity. Upon oral administration of oraxol, the HM30181A moiety binds to and inhibits P-gp, which prevents P-gp-mediated efflux of paclitaxel, therefore enhancing its oral bioavailability. In turn, paclitaxel binds to and stabilizes microtubules, preventing their depolymerization, which results in the inhibition of cellular motility, mitosis, and replication. Altogether, this may result in greater intracellular concentration of paclitaxel, and enhanced cytotoxicity against tumor cells, when compared to the administration of paclitaxel alone. P-gp, encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily of transmembrane transporters; it prevents the intestinal uptake and intracellular accumulation of various cytotoxic agents.
Brand name for enteric-coated zoledronic acid tablet MER-101
A murine monoclonal antibody that attaches to the tumor-associated antigen CA125. Vaccination with monoclonal antibody B43.13 may stimulate a host cytotoxic immune response against tumor cells that express CA125.
Brand name for abatacept
Brand name for ethinyl estradiol
Brand name for elagolix
A platinum(IV) analogue with antineoplastic activity. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity.
The citrate salt form of orphenadrine with a muscle relaxant property. Although the mechanism of action has not been fully elucidated, orphenadrine citrate appears to block cholinergic receptors, thereby interfering with the transmission of nerve impulses from the spinal cord to the muscles. It does not produce myoneural block, nor does it affect crossed extensor reflexes.
Brand name for satraplatin
A semisynthetic, second-generation taxane derivative with potential antineoplastic activity. Ortataxel binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in the inhibition of cell division and cellular proliferation. As it represents a poor substrate for P-glycoprotein (P-gp), multi-drug resistance protein (MRP-1) and breast cancer resistance protein (BCRP) mediated efflux, ortataxel modulates multi-drug resistance mechanisms and may be useful for treating multi-drug resistant tumors that express Pgp, MRP-1 and BCRP.
An orally bioavailable non-steroidal androgen synthesis inhibitor of steroid 17alpha-monooxygenase (17,20 lyase) with potential antiandrogen activity. Orteronel binds to and inhibits the steroid 17alpha-monooxygenase in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells. The cytochrome P450 enzyme CYP17A1 (P450C17), localized to the endoplasmic reticulum (ER), exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces steroidal hormones, such as progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.
Brand name for muromonab-CD3
Brand name for ethinyl estradiol/norethindrone
Brand name for ketoprofen
Brand name for ketoprofen
A proprietary cancer DNA vaccine that contains multiple natural and modified epitopes derived from the four tumor associated antigens, CEA, HER2/neu, p53, and MAGE 2/3. OSE 2101 also includes CAP1-6D, a heteroclitic CEA analog, and PADRE, a proprietary universal T-cell epitope that serves to enhance the immunogenicity of the epitopes. This agent has been shown to elicit cytotoxic T-lymphocyte responses against tumor cells expressing these multiple epitopes.
The phosphate salt of oseltamivir, a synthetic derivative prodrug of ethyl ester with antiviral activity. By blocking neuraminidases on the surfaces of influenza viruses, oseltamivir interferes with host cell release of complete viral particles.
A liposome-encapsulated formulation of the benzoquinazoline folate analog OSI-7904 with antineoplastic activity. As a thymidylate synthase inhibitor, OSI-7904 noncompetitively binds to thymidylate synthase, resulting in inhibition of thymine nucleotide synthesis and DNA replication. Liposome encapsulation improves the efficacy and increases the half-life of OSI-7904.
An orally bioavailable inhibitor of both steroid 11beta-hydroxylase (cytochrome P450 (CYP) 11B1) and aldosterone synthase (CYP11B2; steroid 18-hydroxylase), with potential anti-adrenal activity and ability to treat Cushing disease (CD). Upon administration, osilodrostat binds to and inhibits the activity of CYP11B1, the enzyme that catalyzes the final step of cortisol synthesis from the precursor 11-deoxycortisol, and CYP11B2, the enzyme that catalyzes aldosterone synthesis from corticosterone and 11-deoxycorticosterone in the adrenal gland. The inhibition of CYP11B1 prevents the production of excess cortisol, thereby decreasing and normalizing the levels of cortisol. CD is most often caused by an adrenocorticotropic hormone (ACTH)-secreting pituitary tumor.
The mesylate salt of an orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib mesylate selectively and covalently binds to and inhibits the activity of the mutant forms of EGFR, including the T790M EGFR mutant form, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase overexpressed or mutated in many types of cancers, plays a key role in tumor cell proliferation and tumor vascularization. As osimertinib inhibits T790M, a secondarily acquired resistance mutation, this agent may have therapeutic benefits in tumors with T790M-mediated resistance. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR.
Brand name for mannitol
Brand name for ammonium trichlorotellurate
Brand name for enobosarm
Brand name for magnesium-based bone void filler
A recombinant single-chain polypeptide engineered to exhibit the full binding and activity of an anti-CD37 monoclonal antibody with potential immunostimulatory and antineoplastic activities. Otlertuzumab binds to CD37 on B-cells, which may result in antibody-dependent cell-mediated cytotoxicity (ADCC) and apoptosis. CD37 is a transmembrane glycoprotein expressed at high-levels on B cells and to a lesser extent on T cells and myeloid cells. This agent may have a longer half-life in vivo than conventional monoclonal antibodies.
A cancer vaccine consisting of autologous dendritic cells (DCs) loaded with autologous, lethally irradiated cancer cells and mixed with the cytokine granulocyte-macrophage colony stimulating factor (GM-CSF), with potential immunostimulatory and antineoplastic activities. Upon vaccination, ovapuldencel-T may stimulate the immune system to exert a cytotoxic T-lymphocyte (CTL) immune response against the repertoire of tumor associated antigens (TAAs) found in the irradiated cancer cells. GM-CSF enhances the activation of dendritic cells (DCs) and promotes antigen presentation to both B- and T-lymphocytes.
Brand name for oregovomab
A cancer vaccine comprised of synthetic peptides corresponding to naturally-occurring peptides derived from ovarian cancer cell antigens. Ovarian cancer peptide vaccine may elicit a cytotoxic T-cell response against tumor cells expressing the related ovarian cancer cell antigens.
A cancer vaccine containing autologous dendritic cells (DCs) that are transfected with mRNAs extracted from amplified ovarian cancer stem cells, and mRNAs of the universal tumor antigens human telomerase reverse transcriptase (hTERT) and survivin with potential immunostimulatory and antineoplastic activities. Upon administration, ovarian cancer stem cell/hTERT/survivin mRNAs-loaded autologous DC-006 vaccine may elicit a highly specific cytotoxic T-cell (CTL) response against ovarian cancer cells expressing hTERT, survivin, and specific ovarian cancer stem cell antigens. hTERT, the catalytic subunit of human telomerase, and survivin, a member of the inhibitor of apoptosis (IAP) family of proteins, may be upregulated in certain tumor cell types, playing key roles in tumor cell growth and survival. Ovarian cancer stem cells contain a specific range of antigens that are essential for the neoplastic growth and survival of ovarian cancer cells.
A dendritic cell (DC)-based cancer vaccine composed of autologous dendritic cells (DCs) activated with an ovarian tumor cell lysate containing tumor-associated antigens (TAAs) with potential immunostimulatory and antineoplastic activities. Upon administration, the ovarian tumor antigen-activated autologous DC vaccine may stimulate an anti-tumoral cytotoxic T-lymphocyte (CTL) response against ovarian cancer cells expressing ovarian tumor cell-specific antigens, which may result in ovarian tumor cell lysis.
Brand name for autologous dinitrophenyl-modified ovarian cancer vaccine
Brand name for ethinyl estradiol/norethindrone
Brand name for norgestrel
A selectively replication competent oncolytic adenovirus that is engineered to express OX40 ligand (OX40L) with potential oncolytic and immunostimulatory activities. Upon administration, OX40L-expressing oncolytic adenovirus DNX-2440, which contains an integrin binding RGD-4C motif, infects tumor cells in a Coxsackievirus-adenovirus receptor-independent manner and selectively replicates in tumor cells that are defective in retinoblastoma gene (Rb) or cyclin-dependent kinase inhibitor-2A (p16). Tumor cell selectivity is achieved through a 24-base pair deletion in the E1A gene, which renders the oncolytic adenovirus unable to replicate in normal cells that maintain a functional Rb pathway, but fully replication competent in Rb/p16 defective tumor cells. Active replication of the OX40L-expressing oncolytic adenovirus DNX-2440 within tumor cells may induce oncolysis and release of OX40L. OX40L may then bind to and activate signaling pathways downstream of its cognate receptor, tumor necrosis factor receptor superfamily member 4 (TNFRSF4; OX40), which is expressed on activated T cells. OX40L/OX40 binding promotes increased cytokine production, which can induce proliferation of memory and effector T lymphocytes and promote the killing of nearby tumor cells. OX40L, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) ligand family, provides a co-stimulatory signal for the proliferation and survival of activated T cells. The Rb gene product and p16 are negative regulators of the cell cycle and are defective in certain tumor types.
An organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a 'leaving group.' A 'leaving group' is an atom or a group of atoms that is displaced as a stable species taking with it the bonding electrons. After displacement of the labile oxalate ligand leaving group, active oxaliplatin derivatives, such as monoaquo and diaquo DACH platinum, alkylate macromolecules, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. The DACH side chain appears to inhibit alkylating-agent resistance.
A nanoparticle formulation containing N-glutaryl phosphatidylethanolamine (NGPE)-liposomes encapsulating oxaliplatin and conjugated to the human transferrin (Tf) ligand, with potential antineoplastic activity. Upon infusion of oxaliplatin-encapsulated transferrin-conjugated NGPE liposomes, the transferrin moiety targets and binds to the Tf receptor, which is overexpressed on a variety of human cancer cells. Upon binding and internalization, oxaliplatin is released and its active derivatives alkylate macromolecules, forming both inter- and intra-strand platinum-DNA crosslinks, resulting in an inhibition of DNA replication and transcription. By extending the circulation time and specifically targeting transferrin receptors, this formulation may improve the efficacy and safety of oxaliplatin therapy, compared to administration of oxaliplatin alone. NGPE, a reactive phospholipid, is used as a linker to attach the Tf ligand, to the liposome.
Brand name for oxandrolone
A synthetic, anabolic steroid hormone analog of testosterone. Similar to testosterone, oxandrolone binds to and activates specific nuclear receptors. This agent may be used for testosterone replacement therapy in hypogonadal men, in HIV-wasting syndrome, and in other conditions in order to increase nitrogen retention and fat-free muscle mass.
A dibenzazepine carboxamide derivative with an anticonvulsant property. As a prodrug, oxcarbazepine is converted to its active metabolite, 10-monohydroxy. Although the mechanism of action has not been fully elucidated, electrophysiological studies indicate this agent blocks voltage-gated sodium channels, thereby stabilizing hyper-excited neural membranes, inhibiting repetitive neuronal firing, and decreasing the propagation of synaptic impulses.
Brand name for oxycodone hydrochloride
Brand name for gluten-free DHA/EPA/GLA/antioxidant-rich nutritional liquid oxidative phosphorylation inhibitor IACS-010759]] An orally bioavailable oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon administration of the OxPhos inhibitor IACS-010759, this agent binds to and inhibits complex I of the electron transport chain (NADH ubiquinone oxidoreductase), thereby selectively depriving tumor cells of nutrients, and energy, and inhibiting nucleotide and amino acid production, which induces autophagy, causes tumor cell death and inhibits cell proliferation. Mitochondrial complex I, which is hyperactivated in cancer cells to meet their increased demands for energy, plays a key role in the promotion of cancer cell proliferation.
An orally bioavailable biguanide compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon administration, IM156 inhibits oxidative phosphorylation, decreases mitochondrial function, prevents tumor cell metabolism and deprives tumor cells of energy, thereby preventing tumor cell proliferation. Mitochondrial OxPhos is overactivated in cancer cells and plays a key role in tumor cell proliferation. Drug resistant tumor cells are very susceptible to decreased mitochondrial OxPhos as they cannot easily compensate for the decrease in mitochondrial function by increasing glycolysis.
An oxidized form of the glycoprotein avidin, that can be used as a linking agent for tissue-pretargeted radionuclide therapy. Upon intralesional administration, the aldehyde groups of oxidized avidin strongly bind to the amino groups on tissue proteins, via the formation of Schiff bases. As avidin is able to strongly bind to biotin, intravenous administration of radiolabeled biotin may lead to the selective eradication of the pre-targeted tumor cells.
An aromatic amino acid with antidepressant activity. In vivo, oxitriptan is converted into 5-hydroxytryptamine (5-HT or serotonin) as well as other neurotransmitters. Oxitriptan may exert its antidepressant activity via conversion to serotonin or directly by binding to serotonin (5-HT) receptors within the central nervous system (CNS). Endogenous 5-hydroxytryptophan (5-HTP) is produced from the essential amino acid L-tryptophan. Exogenous therapeutic 5-HTP is isolated from the seeds of the African plant Griffonia simplicifolia.
A lipophilic cation-based triazinoindolyl-hydrazone compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon infusion, in normal cells and proliferating tumor cells where glucose is readily available, inhibition of OxPhos by VLX600 induces a hypoxia-inducible factor 1-alpha (HIF-1alpha)-dependent shift to, and an increase in glycolysis. Glycolysis alone does not produce enough energy to support the growth of tumor cells in this environment, and the induction of autophagy occurs. In the metabolically compromised tumor microenvironment, the availability of oxygen and glucose is limited due to poor vascularization and perfusion of tumor micro-areas. Tumor cells growing in this environment are thus unable to compensate for decreased mitochondrial function by increasing glycolysis. This leads to nutrient depletion, decreased energy production, induction of autophagy, tumor cell death and an inhibition of cell proliferation in quiescent tumor cells. Mitochondrial OxPhos, which is hyperactivated in cancer cells, plays a key role in the promotion of cancer cell proliferation.
Brand name for methoxsalen
Brand name for methoxsalen
The chloride salt form of oxybutynin, a tertiary amine and anticholinergic agent with antispasmodic activity. Oxybutynin chloride exerts its antimuscarinic effect on bladder smooth muscle by blocking muscarinic receptors in smooth muscle, thereby inhibiting acetylcholine binding. This results in a relaxation of bladder smooth muscle, a reduction of involuntary muscle contractions and delays the initial desire to void.
The hydrochloride salt of oxycodone, a methylether of oxymorphone and semisynthetic opioid agonist with analgesic and antitussive properties. Oxycodone binds to mu-receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. In addition to analgesia and a depressive effect on the cough center in the medulla, this agent may cause euphoria, anxiolysis, miosis, sedation, physical dependence, constipation, and respiratory depression, depending on dosage and variations in individual metabolism.
A prolonged-release tablet formulation composed of the hydrochloride salt form of the opioid receptor agonist oxycodone and the hydrochloride salt form of the opioid receptor antagonist naloxone which may produce analgesia while relieving opioid-mediated gastrointestinal (GI) side effects. Upon oral administration, oxycodone binds to opioid receptors, thereby mimicking the effects of endogenous opiates to provide analgesia. As naloxone is very poorly absorbed, this agent binds locally to opiate receptors in the GI tract, thereby preventing oxycodone from binding to these receptors. This relieves the opioid-related side effects on the GI tract, including opioid-induced constipation.
A combination preparation of the analgesic and antipyretic acetaminophen and the semisynthetic opioid agonist oxycodone with analgesic and antitussive properties. Acetaminophen exerts its analgesic activity by inhibiting prostaglandin synthesis, while oxycodone exerts its analgesic activity by binding to the mu-receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opioids.
Brand name for oxycodone hydrochloride
The hydrochloride salt form of oxymorphone, a semisynthetic opioid with a potent analgesic property. Oxymorphone hydrochloride binds to and activates opiate receptors, specifically mu-receptors, in the central nervous system (CNS). This results in sedation, analgesia, decreased gastrointestinal motility, and respiratory depression.
A highly modified, fourth generation linear decapeptide with gonadotropin-releasing hormone (GnRH or LHRH) antagonizing properties. Ozarelix competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with hormonally dependent disease states such as hormone-dependent prostate cancer.
Brand name for dexamethasone intravitreal implant