Dictionary of drugs: N
Dictionary of pharmaceutical drugs/medications sorted alphabetically
- A page 1 | A page 2 | A page 3
- C | C1 | C2
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- 0 - 9
Dictionary of drugs N
A peptide cancer vaccine comprised of human leukocyte antigen HLA-A2-restricted peptide derived from a metastatic melanoma cell line of patient NA17, with potential immunomodulating and antineoplastic activity. NA17.A2 peptide vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tumors that express this antigen, which may result in a reduction in tumor size. This NA17 specific antigen, encoded by an intron sequence of N-acetylglucosaminyltransferase V (GnT-V) gene, is expressed in about 50% of melanomas.
A peptide cancer vaccine consisting of peptides derived from the melanoma antigen NA-17, the human leukocyte antigen HLA-A2-restricted human melanoma antigen 3 (MAGE-3.A2) and the cancer-testis antigen (NY-ESO-1), with potential immunostimulating and antineoplastic activities. Upon administration, the NA-17/MAGE-3.A2/NY-ESO-1 peptide vaccine may stimulate the immune system to mount a cytotoxic T-cell (CTL) response against tumor cells expressing NA-17, MAGE-3.A2 and NY-ESO-1, resulting in tumor cell lysis. The tumor-associated antigens (TAAs) NA-17, MAGE-3.A2 and NY-ESO-1 are overexpressed in a variety of cancer cell types.
A specific melanoma antigen protein derived from a patient (NA17) with cutaneous melanoma metastases. When administered in a vaccine formulation, NA17-A antigen may stimulate a cytotoxic T lymphocyte (CTL) response against tumors that express this antigen, which may result in a reduction in tumor size. The NA17-A antigen is part of the enzyme N-acetyl glucosaminyl-transferase V (GnT-V). Approximately half of melanomas have been found to express significant levels of this atypical protein, which is not expressed by normal tissues.
A synthetic cannabinoid and dibenzopyrane derivative with anti-emetic activity. Although the mechanism of action has not been fully elucidated yet, it has been suggested that nabilone is a highly selective and strong agonist for the cannabinoid receptors CB1 and CB2, both of which are coupled to Gi/o proteins. The CB1 receptors are expressed predominantly in central and peripheral neurons and receptor stimulation has been implicated in the reduction of chemotherapy-induced nausea.
An herbal preparation containing a defined quantity of specific cannabinoids formulated for oromucosal spray administration with potential analgesic activity. Nabiximols contains a standardized extract of tetrahydrocannabinol (THC), the non-psychoactive cannabinoid cannabidiol (CBD), other minor cannabinoids, flavonoids, and terpenes from two cannabis plant varieties. Cannabinoids interact with G protein-coupled cannabinoid 1 (CB1) receptors in the central nervous system, resulting in analgesic, euphoric, and anticonvulsive effects.
A formulation composed of nanoparticle albumin-bound (nab) paclitaxel, which is an albumin-stabilized nanoparticle containing the natural taxane paclitaxel, non-covalently coated with rituximab, a recombinant chimeric murine/human antibody directed against the CD20 antigen found on B-lymphocytes, with potential antineoplastic activity. Upon administration of nab-paclitaxel/rituximab nanoparticle AR160, the rituximab moiety specifically binds to CD20 and targets this formulation to CD20-positive tumor cells. Paclitaxel binds to and stabilizes microtubules, which prevents depolymerization and inhibits cellular motility, mitosis, and replication. This leads to cell death of the CD20-expressing tumor cells that were targeted by this agent. The combination of albumin-stabilization and rituximab-targeting allows for higher efficacy and decreased paclitaxel-induced toxicity as it specifically targets CD20-expressing tumor cells. Rituximab may also induce complement-dependent cytotoxicity and antibody-dependent cellular toxicity.
An oral solution composed of N-acetylcysteine, a synthetic N-acetyl derivative of the endogenous amino acid L-cysteine, and simethicone, a mixture of polydimethylsiloxanes and hydrated silica gel, with mucolytic and antifoaming activities. Upon oral administration of the mucolytic solution, N-acetylcysteine breaks down disulfide bonds in mucoproteins, resulting in liquification of mucus in the upper respiratory tract. Simethicone reduces the surface tension of gas bubbles causing them to coalesce into larger bubbles that can be passed more easily. This increases the passage of mucus and gas bubbles from the upper digestive tract. This may also increase visibility of the gastric mucosa during upper endoscopy.
A replication-deficient recombinant adenovirus encoding human interferon alpha-2b with potential antineoplastic activity. Upon intravesical administration, nadofaragene firadenovec infects nearby tumor cells and expresses INF alpha-2b intracellularly which activates the transcription and translation of genes whose products mediate antiviral, antiproliferative, antitumor, and immune-modulating effects.
A non-selective beta-adrenergic antagonist with antihypertensive and antiarrhythmic activities. Nadolol competitively blocks beta-1 adrenergic receptors located in the heart and vascular smooth muscle, inhibiting the activities of the catecholamines epinephrine and norepinephrine and producing negative inotropic and chronotropic effects. This agent exhibits antiarrhythmic activity via the impairment of atrioventricular (AV) node conduction and a corresponding reduction in sinus rate. In the kidney, inhibition of the beta-2 receptor within the juxtaglomerular apparatus results in the inhibition of renin production and a subsequent reduction in angiotensin II and aldosterone levels, thus inhibiting angiotensin II-dependent vasoconstriction and aldosterone-dependent water retention.
A low molecular weight heparin (LMWH) composed of a heterogeneous mixture of sulfated polysaccharide glycosaminoglycan chains obtained by depolymerisation of porcine mucosal sodium heparin, extraction/purification and conversion to the calcium salt. Nadroparin binds to antithrombin III (ATIII) and inhibits the activity of activated factor X (factor Xa), thereby inhibiting the final common pathway of the coagulation cascade and preventing the formation of a cross-linked fibrin clot.
The hydrochloride salt of the partial estrogen antagonist nafoxidine. Nafoxidine competes with endogenous estrogen for binding to specific estrogen receptors. This agent also inhibits angiogenesis in some tissues by blocking the effects of fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF); paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces oxidative stress, protein kinase C and calcium signaling.
A synthetic mixed opioid agonist-antagonist with analgesic properties. Although its exact mechanism has not been fully delineated, it is hypothesized that upon administration, nalbuphine binds to kappa receptors in the central nervous system (CNS), thereby inhibiting the release of neurotransmitters that mediate pain, such as substance P. Additionally, nalbuphine exerts post-synaptic inhibitory effects on interneurons and output neurons of the spinothalamic tract, responsible for transporting nociceptive information. Compared to other opioid agents that stimulate mu receptors, nalbuphine antagonizes mu receptors, thereby potentially producing less intense respiratory depression.
A pegylated form of naloxone, a peripherally-acting mu-opioid receptor antagonist, that can be used to reduce opioid-induced symptoms. Upon administration, naloxegol binds to and blocks mu-opioid receptors in the peripheral nervous system. This prevents peripheral opioid receptor activation and abrogates opioid-induced side effects, such as opioid-induced constipation (OIC). Pegylation of naloxone reduces permeability across the blood-brain barrier (BBB) and prevents this agent from interfering with the analgesic activity of opioid receptor agonists.
The hydrochloride salt of naloxone, a thebaine derivate with opioid antagonist activity. Naloxone binds to opioid receptors in the CNS in a competitive manner, reversing or inhibiting characteristic opioid effects, including analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence. This agent binds to mu-opioid receptors with a high affinity, and a lesser degree to kappa- and gamma-opioid receptors.
The hydrochloride salt of naltrexone, a noroxymorphone derivative with competitive opioid antagonistic activity. Naltrexone and its metabolite 6-beta-naltrexol reverse the effects of opioids by binding to various opioid receptors in the central nervous system CNS), including the mu-, kappa- and gamma-opioid receptors; opioid effects of analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence are inhibited. Naltrexone is longer-acting and more potent compared to naloxone.
Brand name for memantine hydrochloride
The decanoate salt form of nandrolone, an anabolic steroid analog of testosterone with androgenic, anabolic, and erythropoietin stimulating effects. Nandrolone enters the cell and binds to and activates specific nuclear androgen receptors in responsive tissue, including the prostate, seminal vesicles, scrotum, penis, larynx, hair follicles, muscle, and bone. The resulting activated hormone receptor complex translocates into the nucleus and binds to androgen response elements (ARE) in the promoter region of targeted genes, where the complex promotes gene expression necessary for maintaining male sex characteristics. Mimicking the negative feedback mechanism of testosterone, nandrolone decanoate also suppresses the secretion of luteinizing hormone (LH). Furthermore, this agent also stimulates erythropoietin production by enhancing the production of erythropoietic stimulating factors.
A nanoparticle-based formulation composed of a microRNA 16 (miR-16) mimic, a double-stranded, 23 base pair, synthetic RNA molecule, encapsulated in nonliving bacterial minicells and coated with anti-epidermal growth factor receptor (EGFR) antibodies, with potential antineoplastic activity. Upon intravenous administration and subsequent transfection, nanocell-encapsulated miR-16-based microRNA mimic targets EGFR-expressing tumor cells and facilitates the restoration of expression of the miR-16 family. This leads to the downregulation of the expression of tumor-promoting genes and the inhibition of tumor cell growth. In addition, restoration of miR-16 expression sensitizes the tumor cell to certain chemotherapeutic agents. miR-16, a family of microRNAs, is critical to the regulation of gene expression and appears to have a tumor suppressor function; its expression is downregulated in various cancer cell types.
A nanoparticle albumin-bound formulation of the taxane docetaxel with antineoplastic activity. Docetaxel is a semi-synthetic, second-generation taxane derived from a compound found in the European yew tree Taxus baccata. Docetaxel binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell-cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and displays immunomodulatory and pro-inflammatory properties by inducing various mediators of the inflammatory response. In nanoparticle albumin-bound docetaxel ABI-008 docetaxel is solubilized without the use of the nonionic solubilizer Cremophor ELP, permitting the administration of larger doses of docetaxel while avoiding Cremophor ELP-associated toxicity.
The macrolide antibiotic rapamycin bound to nanoparticle albumin with immunosuppressant (see sirolimus) and potential antiangiogenic and antineoplastic activities. Rapamycin binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate a complex that binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. In turn, inhibition of mTOR may result in the inhibition of the phosphatidylinositol 3 (PI-3) kinase/Akt pathway and vascular endothelial cell growth factor (VEGF) secretion, which may result in decreased tumor cell proliferation and tumor angiogenesis. The binding of water-insoluble rapamycin to nanoparticle albumin permits the albumin-mediated endocytosis of rapamycin by tumor cells and endothelial cells.
A topical ointment composed of the water-insoluble taxane paclitaxel that has been processed to form uncoated nanoparticles, with potential antineoplastic activity. Upon topical administration of nanoparticle paclitaxel ointment SOR007 to the affected area, and following epithelial and dermal penetration, paclitaxel binds to tubulin and inhibits the disassembly of microtubules, which leads to the inhibition of cell division, thereby halting the proliferation of rapidly-dividing tumor cells. The nanoparticles in the nanoparticle paclitaxel ointment are produced through a specific proprietary submicron particle production.
A nanoparticle-based formulation consisting of polymeric micelles, composed of triblock copolymers, loaded with the bioactive hydrophobic irinotecan metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38), with potential antineoplastic activity. Upon administration, nanoparticle SN-38-encapsulated micelle formulation IT141 diffuses into the tumor site and the SN-38 moiety binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, which results in DNA breaks, inhibition of DNA replication, and apoptosis. Compared to SN-38 alone, this formulation increases the water solubility of SN-38 and allows the delivery of higher doses of SN-38. IT-141 also has a much longer circulation time and reduces toxicity to normal, healthy tissues.
A formulation of nanoparticles encapsulating the hydrochloride salt form of the anthracycline antibiotic doxorubicin, with potential antitumor activity. Upon intravenous administration, doxorubicin intercalates DNA, interferes with the activity of topoisomerase II, and causes DNA adducts and other DNA damage, resulting in tumor cell growth inhibition and apoptosis. This agent also interacts with cell membrane lipids causing lipid peroxidation. Delivery of doxorubicin in nanoparticles may improve drug penetration into tumors and may circumvent the tumor cells' multidrug resistance mechanisms and may therefore be effective in chemoresistant tumor cells.
A preparation of self-assembled core-shell nanoscale coordination polymer (NCP) nanoparticles containing an as of yet undisclosed payload with potential immunostimulating and antineoplastic activities. Upon intravenous administration, NCP nanoparticle formulation CPI-100 delivers its payload to tumor cells, which may lead to enhanced immune-mediated killing and regression of tumor cells.
A lipid-based nanosomal formulation of the poorly soluble, semi-synthetic, second-generation taxane docetaxel, with potential antineoplastic activity. Upon intravenous injection, docetaxel binds to and stabilizes tubulin, which inhibits microtubule disassembly and results in both cell cycle arrest at the G2/M phase and cell death. This liposomal formulation solubilizes docetaxel without the use of toxic solvents, such as polysorbate 80. This permits the administration of larger doses of docetaxel and improves the drug’s safety profile by avoiding solvent-associated toxicities, such as hypersensitivity reactions and neurotoxicity. In addition, the nanosomal lipid-based delivery of docetaxel improves drug penetration into tumors and decreases drug clearance, all of which prolong the duration of docetaxel’s therapeutic effects.
An orally available cancer cell stemness inhibitor with potential antineoplastic activity. Even though the exact target has yet to be fully elucidated, napabucasin appears to target and inhibit multiple pathways involved in cancer cell stemness. This may ultimately inhibit cancer stemness cell (CSC) growth as well as heterogeneous cancer cell growth. CSCs, self-replicating cells that are able to differentiate into heterogeneous cancer cells, appear to be responsible for the malignant growth, recurrence and resistance to conventional chemotherapies.
An amonafide (naphthalimide) derivative and pan-antagonist of chemokine ligand (CXCL) expression, with potential anti-angiogenic activity. Although UNBS5162 is a derivative of amonafide, this agent appears to have a different profile than that of amonafide and its exact mechanism of action remains to be fully elucidated. This agent seems to decrease the expression of various proangiogenic CXCL chemokines in vitro and may have synergistic effects with radiotherapy or chemotherapy. CXCLs are small cytokines in the CXC chemokine family that are overexpressed in certain cancers; CXCL-mediated signaling plays a key role in angiogenesis and tumor progression.
Brand name for naproxen
A propionic acid derivative and a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic and analgesic activities. Naproxen inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of naproxen. Naproxen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation.
A recombinant fusion protein consisting of the antigen-binding fragment of a monoclonal antibody directed towards the tumor-associated oncofetal trophoblast glycoprotein antigen 5T4 attached to a mutated form of superantigen staphylococcal enterotoxin E (SEA/E-120), with immunomodulating and antineoplastic activities. The Fab moiety of naptumomab estafenatox binds to 5T4, an antigen expressed by various tumor cells. In turn, the superantigen binds to both major histocompatibility complex class II molecules and to the T-cell receptor beta chain, which results in a massive activation of T lymphocytes and induces a potent T-cell-mediated killing of tumor cells.
Brand name for naloxone hydrochloride
Brand name for phenelzine sulfate
A monoclonal antibody against RON (recepteur d'origine nantais; macrophage stimulating 1 receptor), with potential antineoplastic activity. Narnatumab binds to RON, thereby preventing binding of its ligand hepatocyte growth factor-like protein (HGFL or macrophage-stimulating protein (MSP)). This may prevent RON receptor-mediated signaling and may prevent cellular proliferation in tumor cells overexpressing RON. RON, a receptor tyrosine kinase, is overexpressed in a variety of epithelial cancer cell types and plays an important role in cellular proliferation, migration and invasion.
Brand name for ropivacaine hydrochloride
Brand name for triamcinolone acetonide
A solution containing sodium chloride that can be used to cleanse the nasal passages. Upon nasal irrigation, the saline washes out thick or dry mucus, and irritants, such as pollen, dust particles, pollutants and bacteria, from the nasal cavities. This reduces nasal blockage, improves nasal airflow and helps keep nasal passages clean and clear, which decreases the risk of irritation and inflammation. The saline solution also moisturizes and soothes irritated mucus membranes.
Brand name for fentanyl citrate pectin-based nasal spray
A humanized recombinant IgG4 monoclonal antibody directed against the alpha4 subunit of the integrins alpha4beta1 and alpha4beta7 with immunomodulating, anti-inflammatory, and potential antineoplastic activities. Natalizumab binds to the apha4-subunit of alpha4beta1 and alpha4beta7 integrins expressed on the surface of all leukocytes except neutrophils, inhibiting the alpha4-mediated adhesion of leukocytes to counter-receptor(s) such as vascular cell adhesion molecule-1 (VCAM-1); natalizumab –mediated disruption of VCAM-1 binding by these integrins may prevent the transmigration of leukocytes across the endothelium into inflamed parenchymal tissue. Integrins are cellular adhesion molecules (CAMs) that are upregulated in various types of cancer and some autoimmune diseases; alpha4beta1 integrin (VLA4) has been implicated in the survival of myeloma cells, possibly by mediating their adhesion to stromal cells.
A phenylalanine derivative of the meglitinide class of agents with hypoglycemic activity. Nateglinide, compared to repaglitinide, binds with a higher affinity to the SUR1 subunit and with a faster onset of action and a shorter duration of action. This agent is metabolized by the cytochrome P450 isoenzyme CYP2C9, and, to a lesser extent, by CYP3A4. The parent drug and metabolites are mainly excreted in the urine and its half-life is about 1.5 hours.
Brand name for nesiritide
A proprietary preparation of natural human interferon alpha (IFN alpha) with potential immunomodulatory and antineoplastic activities. Natural human interferon alpha OPC-18 binds to cell-surface IFN alpha receptors (IFNARs), resulting in the transcription and translation of genes whose products mediate antiviral, antiproliferative, and immune-modulating effects. IFN alpha is a type I interferon produced by peripheral blood leukocytes or lymphoblastoid cells when exposed to live or inactivated virus, double-stranded RNA, or bacterial products and is the primary interferon produced by virus-induced leukocyte cultures. In addition to its pronounced antiviral activity, it activates NK cells.
A population of activated, immortalized, interleukin-2 (IL-2)-dependent, cytotoxic natural killer (NK) cells with potential antitumor activity. Natural killer cells ZRx101 are derived from NK-92 cells, having been modified to target tumor-associated antigens (TAAs) upregulated in certain types of cancer. The NK-92 cell line was originally isolated from a patient with large granular lymphocytic (LGL) leukemia/lymphoma.
Brand name for vinorelbine tartrate
An orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. BcI-2 family protein inhibitor ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. Bcl-2, Bcl-XL, and Bcl-w are frequently overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon, and have been linked to tumor drug resistance.
The powder form of the cooked navy bean with potential antioxidant and chemopreventive activities. Navy beans are rich in fiber, minerals, vitamins, and phytochemicals such as flavonoids and phytosterols. They appear to prevent carcinogenesis by inducing tumor cell apoptosis. Intake of navy bean powder may have a beneficial effect on intestinal microflora.
A humanized monoclonal antibody directed against the human tumor-associated antigen GD2, with potential antineoplastic activity. Upon vaccination, naxitamab stimulates antibody-dependent cell-mediated cytotoxicity (ADCC) against GD2-expressing tumor cells. GD2, a disialoganglioside with expression in normal tissues restricted primarily to the cerebellum and peripheral nerves, is commonly expressed at high levels on tumors of neuroectodermal origins such as melanomas and neuroblastomas. Compared to the murine monoclonal antibody 3F8 (m3F8), the humanized form does not cause a human anti-mouse antibody (HAMA) response and shows enhanced ADCC activity.
A proprietary antisense oligonucleotide targeting a novel non-coding mitochondrial RNA (ncmtRNA), with potential antineoplastic activity. Upon administration, Andes-1537 binds to ncmtRNA, which is overexpressed in rapidly proliferating cells, such as cancer cells, and not expressed in resting cells. This may decrease the expression of the ncmtRNA, which may inhibit cell proliferation and eventually induce apoptosis in susceptible cancer cells. The proprietary mitochondrial RNA (mtRNA) belongs to the family of non-coding RNAs (ncRNA); it contains an inverted repeat (IR) of 815 nucleotides (nt), which can form a covalent link to the 5’ end of the mitochondrial 16S ribosomal RNA (16S mtrRNA).
An imaging agent containing a human heat shock protein 90 (Hsp90) inhibitor connected by a linker to a near infrared (NIR) fluorescent dye. Upon intravenous administration, HS-196 selectively and competitively binds to Hsp90 in cells. As Hsp90 is upregulated in a variety of tumor cells, the accumulation of the NIR-tethered imaging agent allows for in vivo detection due to enhanced uptake of HS-196. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation, stability and function of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation and/or immune responses.
Brand name for pentamidine isethionate
A fully human IgG1 monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Necitumumab binds to and blocks the ligand binding site of EGFR, thereby preventing the activation and subsequent dimerization of the receptor. This may lead to an inhibition of EGFR-dependent downstream pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various tumor cell types.
A second-generation cisplatin analogue with antineoplastic activity. Containing a novel ring structure in which glycolate is bound to the platinum by a bidentate ligand, nedaplatin forms reactive platinum complexes that bind to nucelophillic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death. This agent appears to be less nephrotoxic and neurotoxic compared to both cisplatin and carboplatin.
An inhibitor of NEDD8 (neural precursor cell expressed, developmentally down-regulated 8) activating enzyme E1 (NAE), with potential antineoplastic activity. Upon administration, TAS4464 selectively binds to and inhibits NAE, which prevents NAE/NEDD8-mediated signaling and prevents the NEDD8 conjugation of cullin-RING ligase complexes (CRLs). This inactivates the CRLs leading to an accumulation of CRL substrate proteins, such as CDT1, p27, p21 and phosphorylated IkappaB, and inactivates nuclear factor-kappaB (NF-kB) as well as downregulates anti-apoptotic proteins. This causes cell cycle dysregulation, induces apoptosis, and inhibits tumor cell proliferation and survival. NAE catalyzes the first step in the NEDD8 conjugation (neddylation) pathway which controls cancer cell growth and survival through activation of CRLs.
An orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with potential antineoplastic activity, and potential sensitizing and enhancing activities for both chemo- and radiotherapies. Upon administration, nedisertib binds to and inhibits the activity of DNA-PK, thereby interfering with the non-homologous end joining (NHEJ) process and preventing repair of DNA double strand breaks (DSBs) caused by ionizing radiation or chemotherapeutic treatment. This increases chemo- and radiotherapy cytotoxicity and leads to enhanced tumor cell death. The enhanced ability of tumor cells to repair DSBs plays a major role in the resistance of tumor cells to chemo- and radiotherapy; DNA-PK plays a key role in the NHEJ pathway and DSB repair.
The hydrochloride salt form of nefopam, a centrally-acting, non-opioid benzoxazocine with analgesic activity. The mechanism of action through which nefopam exerts its analgesic effects is, as of yet, largely unknown but may involve inhibition of serotonin, dopamine and noradrenaline reuptake.
A humanized, agonistic monoclonal antibody against P selectin glycoprotein ligand-1 (PSGL-1; SELPLG; CD162), with potential immunosuppressive activity. Upon administration, neihulizumab specifically targets and binds to CD162 expressed on activated T-lymphocytes. This induces apoptosis of activated T-cells and reduces T-cell-mediated immune responses. This may halt disease progression of T-cell-mediated autoimmune diseases and acute graft-versus-host disease (GvHD).
An arabinonucleoside antimetabolite with antineoplastic activity. Nelarabine is demethoxylated by adenosine deaminase to become biologically active 9-beta-D-arabinosylguanine (ara-G); ara-G incorporates into DNA, thereby inhibiting DNA synthesis and inducing an S phase-dependent apoptosis of tumor cells.
The mesylate salt form of the antiviral agent nelfinavir. Nelfinavir selectively inhibits human immunodeficiency virus (HIV) protease, thereby preventing cleavage of the gag-pol viral polyprotein and resulting in the release of immature, noninfectious virions. In vivo, this agent exhibits broad tissue distribution compared to related agents.
A cancer peptide vaccine comprised of a human leukocyte antigen (HLA) A2/A3 restricted HER2/neu (ERBB2) peptide from the extracellular domain of the HER2 protein (E75 peptide) and combined with the immunoadjuvant granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunomodulating and antineoplastic activity. Upon intradermal injection, nelipepimut-S plus GM-CSF vaccine may induce a specific cytotoxic T-lymphocyte (CTL) response against HER2/neu-expressing tumor cell types. HER2/neu, a tumor-associated antigen and a member of the epidermal growth factor receptor family of tyrosine kinases, is overexpressed in various tumor cell types. GM-CSF potentiates the antitumor immune response.
A personalized, polyepitope DNA vaccine composed of a DNA plasmid encoding multiple, highly immunogenic tumor associated antigens (TAAs) that are specifically expressed by a patient's pancreatic cancer cells, including personalized epitopes of the TAA mesothelin, with potential immunostimulatory and antineoplastic activities. Upon intramuscular administration and electroporation of the neoantigen DNA-based pancreatic cancer vaccine, the expressed TAAs induce a specific cytotoxic T-lymphocyte (CTL) immune response against tumor cells expressing the neoantigens.
A peptide-based, personalized glioblastoma cancer vaccine consisting of patient-specific glioblastoma-derived immunogenic mutated epitopes (neoantigens), with potential immunomodulating and antineoplastic activities. Vaccination with the neoantigen-based glioblastoma vaccine stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the neoantigens, which results in tumor cell lysis. Neoantigens are tumor-specific antigens derived from mutated proteins that are present only in a specific tumor.
A peptide-based melanoma cancer vaccine consisting of neoantigens and peptides derived from patient-specific melanoma immunogenic epitopes, combined with the immunostimulant poly-ICLC with potential immunomodulating and antineoplastic activities. Vaccination with the neoantigen-based melanoma vaccine stimulates the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the neoantigens, which results in tumor cell lysis. The adjuvant poly-ICLC, composed of double-stranded RNA molecules of polyinosinic-polycytidylic acid stabilized with poly L-lysine in carboxymethylcellulose, is a ligand for toll-like receptor-3 (TLR3) and induces the release of cytokines which may help to boost the immune response against the selected neoantigens.
A peptide-based renal cell carcinoma (RCC) vaccine consisting of neoantigens and peptides derived from immunogenic epitopes identified through DNA and RNA sequencing of a patient's tumor cells, combined with the immunostimulant poly-ICLC with potential immunomodulating and antineoplastic activities. Vaccination with the neoantigen-based RCC vaccine stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the neoantigens, leading to tumor cell lysis. The adjuvant poly-ICLC, composed of double-stranded RNA molecules of polyinosinic-polycytidylic acid stabilized with poly L-lysine in carboxymethylcellulose, is a ligand for toll-like receptor-3 (TLR3) and induces the release of cytokines which may help to boost the immune response against the selected neoantigens.
A personalized cancer vaccine comprised of a not yet disclosed oncolytic virus encoding tumor-specific neoantigens that have been identified through genetic sequencing of a patient’s tumor cells, with potential immunostimulatory and antineoplastic activities. Upon administration, the neoantigen-encoding personalized virus-2 (PSV-2) infects cells and expresses the tumor-specific neoantigens (TSNAs). This stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the TSNAs, leading to tumor cell lysis.
A proprietary, personalized autologous synthetic cancer vaccine composed of patient-specific synthetic cancer neo-epitopes complexed with heat shock protein 70 (HSP 70; HSP70), with potential immunostimulating and antineoplastic activities. Upon administration of the autologous neoantigen-HSP70 cancer vaccine, the HSPs present the neoantigens to antigen presenting cells (APCs) and help elicit a potent neoantigen-specific T-cell-based anti-tumor immune response, thereby killing the neoantigen-expressing cancer cells. HSP70 is able to the transport the neo-epitopes, activate APCs and enhance the T-cell-mediated immune response.
A personalized, peptide-based therapeutic dendritic cell (DC) vaccine consisting of autologous DCs loaded with immunogenic peptides derived from autologous cancer cells, with potential immunomodulating and antineoplastic activities. Upon leukapheresis, mature DCs are loaded with immunogenic neoantigens. Vaccination with the neoantigen-loaded autologous DC vaccine stimulates the host immune system to mount a cytotoxic T-lymphocyte (CTL) response against tumor cells expressing the neoantigens, which results in tumor cell lysis.
Brand name for norgestrel
An autologous dendritic cell (DC) vaccine composed of DCs loaded with multiple distinct neoantigens, with potential immunomodulating and antineoplastic activities. Upon administration, the neo-multiple tumor-associated antigens (TAA)-loaded DC vaccine may stimulate a cytotoxic T-lymphocyte (CTL)-mediated immune response against the tumor cells expressing these neoantigens.
A broad spectrum aminoglycoside antibiotic derived from Streptomyces fradiae with antibacterial activity. Neomycin is an antibiotic complex consisting of 3 components: the two isomeric components B and C are the active components, and neomycin A is the minor component. Neomycin irreversibly binds to the 16S rRNA and S12 protein of the bacterial 30S ribosomal subunit. As a result, this agent interferes with the assembly of initiation complex between mRNA and the bacterial ribosome, thereby inhibiting the initiation of protein synthesis. In addition, neomycin induces misreading of the mRNA template and causes translational frameshift, thereby results in premature termination. This eventually leads to bacterial cell death.
Brand name for diethylstilbestrol
Brand name for apaziquone
Brand name for cyclosporine
Brand name for gallium citrate Ga 67
Brand name for shark cartilage extract AE-941
Brand name for methazolamide
The maleate salt form of neratinib, an orally available, quinazoline-based, irreversible inhibitor of both the receptor tyrosine kinases (RTKs) human epidermal growth factor receptor 2 (HER2; ERBB2) and human epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon administration, neratinib targets and covalently binds to the cysteine residue in the ATP-binding pockets of both HER2 and EGFR. This inhibits their activity and results in the inhibition of downstream signal transduction events, induces cell cycle arrest, apoptosis and decreases cellular proliferation in HER2- and EGFR-expressing tumor cells. EGFR and HER2, RTKs that are mutated or overactivated in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization.
Brand name for neratinib maleate
A recombinant version of the cardiac neurohormone, human B-type natriuretic peptide (hBNP) produced by the ventricular myocardium. Nesiritide binds to natriuretic peptide receptors on vascular smooth muscle and endothelial cells, through which it triggers guanylate cyclase dependent signal transduction resulting in increase of intracellular concentrations of cGMP. This leads to smooth muscle cell relaxation causing arterial and venous dilatation.
A fully human monoclonal antibody directed against angiopoietin 2 (ANG2) with potential antiangiogenic and antineoplastic activities. Nesvacumab binds to ANG2 and interferes with the interaction between Ang2 and its receptor TEK tyrosine kinas e (Tie2), which may inhibit tumor cell angiogenesis and tumor cell proliferation. ANG2 is upregulated in a variety of cancer cell types and plays a crucial role in angiogenesis.
An orally active, benzodiazepine type, selective cholecystokinin B receptor (CCKBR; CCK2R; gastrin receptor) antagonist with potential gastric acid reducing and antiproliferative activity. Upon administration of netazepide, this agent selectively binds to and blocks the CCKBR, thereby preventing the binding of gastrin and cholecystokinin. This may prevent gastric neuroendocrine enterochromaffin-like (ECL) cell-induced secretion of histamine, ultimately preventing gastric acid secretion from adjacent parietal cells. In addition, YF476 may inhibit ECL cell proliferation and ECL-derived gastric carcinoids.
A selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK-receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema.
An orally available combination formulation containing netupitant, a selective neurokinin 1 (NK1) receptor antagonist, and the hydrochloride salt form of palonosetron, a selective serotonin (5-hydroxytryptamine; 5-HT) receptor subtype 3 (5-HT3) antagonist, with antiemetic activity. Upon oral administration, palonosetron competitively blocks the action of 5-HT at 5-HT3 receptors located on vagal afferent nerves in the chemoreceptor trigger zone (CTZ). This inhibits acute emesis associated with 5-HT secretion and subsequent 5-HT3 activation. Netupitant competitively binds to and blocks the activity of the human NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1 receptor binding of the endogenous tachykinin neuropeptide substance P (SP). This prevents delayed emesis, which is associated with SP secretion. Altogether, this results in the prevention of chemotherapy-induced nausea and vomiting (CINV).
Brand name for pegfilgrastim
Brand name for oprelvekin
Brand name for filgrastim
Brand name for iodine I 131 monoclonal antibody 81C6
Neural stem cells (NSCs) that are transfected with the gliomatropic oncolytic adenovirus (OV) CRAd-S-pk7, a conditionally replicative oncolytic adenoviral (CRAd) vector that contains the tumor-specific survivin promoter (S) and a fiber protein polylysine modification (pk7), with potential antineoplastic activity. Upon intracerebral administration of NSC loaded with CRAd-S-pk7, the NSCs preferentially migrate towards tumor cells, and the polylysine moiety of the modified fiber protein expressed by the viral vector specifically targets and binds to tumor-specific heparan sulfate proteoglycans. Subsequently, the virus can infect the tumor cells and viral replication is initiated because E1 gene expression is controlled by the tumor-specific promoter for survivin. This results in the specific lysis of the glioma cells. The pk7 fiber modification and the survivin promoter enable tumor-specific infectivity, and transcriptional targeting and preferential replication in glioma cells, while sparing the surrounding normal brain parenchyma. The pK7 is comprised of a heparan sulfate binding domain incorporated into the fiber protein of the adenovirus.j
Brand name for gabapentin
Brand name for trimetrexate glucuronate
A fluorescence imaging agent composed of a fluorescent agent linked, via a human neutrophil elastase (HNE) cleavable peptide, to a dequencher molecule, with imaging activity for diagnostic purposes. Upon local administration, the neutrophil activation probe (NAP) imaging agent, initially quenched, is quickly taken up by activated neutrophils. In turn, the HNE expressed by these cells specifically cleaves the linker and dequenches the fluorescent agent. The activated fluorescent moiety allows for visualization of activated neutrophils and HNE activity upon using a fluorescence imaging device. Activated neutrophils are upregulated at sites of inflammation and in inflammation-induced cancers, and express high levels of HNE.
Brand name for lapuleucel-T
A non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against human immunodeficiency virus 1. Nevirapine binds directly to the human immunodeficiency virus type 1 (HIV-1) reverse transcriptase, an RNA-dependent DNA polymerase, blocking its function in viral DNA replication. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.
Brand name for sorafenib tosylate
Brand name for esomeprazole magnesium
Brand name for Phellodendron amurense bark extract
Brand name for amiodarone hydrochloride
An amino acid derivative and nitric oxide synthase (NOS) inhibitor with potential antineoplastic and antiangiogenic activities. Upon administration, NG-nitro-L-arginine inhibits the enzyme nitric oxide synthase, thereby preventing the formation of nitric oxide (NO). By preventing NO generation, the vasodilatory effects of NO are abrogated leading to vasoconstriction, reduction in vascular permeability and an inhibition of angiogenesis. As blood flow to tumors is restricted, this may result in an inhibition of tumor cell proliferation. NO plays an important role in tumor blood flow and stimulation of angiogenesis, tumor progression, survival, migration and invasiveness.
A water-soluble vitamin belonging to the vitamin B family, which occurs in many animal and plant tissues, with antihyperlipidemic activity. Niacin is converted to its active form niacinamide, which is a component of the coenzymes nicotinamide adenine dinucleotide (NAD) and its phosphate form, NADP. These coenzymes play an important role in tissue respiration and in glycogen, lipid, amino acid, protein, and purine metabolism. Although the exact mechanism of action by which niacin lowers cholesterol is not fully understood, it may act by inhibiting the synthesis of very low density lipoproteins (VLDL), inhibiting the release of free fatty acids from adipose tissue, increasing lipoprotein lipase activity, and reducing the hepatic synthesis of VLDL-C and LDL-C.
The active form of vitamin B3 and a component of the coenzyme nicotinamide adenine dinucleotide (NAD). Niacinamide acts as a chemo- and radio-sensitizing agent by enhancing tumor blood flow, thereby reducing tumor hypoxia. This agent also inhibits poly(ADP-ribose) polymerases, enzymes involved in the rejoining of DNA strand breaks induced by radiation or chemotherapy.
Brand name for nicotinamide riboside
A synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator.
An orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Upon oral administration, niclosamide specifically induces degradation of the androgen receptor (AR) variant V7 (AR-V7) through the proteasome-mediated pathway. This downregulates the expression of the AR variant, inhibits AR-V7-mediated transcriptional activity, and reduces AR-V7 recruitment to the prostate-specific antigen (PSA) gene promoter. Niclosamide also prevents AR-V7-mediated STAT3 phosphorylation and activation. This inhibits AR/STAT3-mediated signaling and prevents expression of STAT3 target genes. Altogether, this may inhibit growth of AR-V7-overexpressing cancer cells. The AR-V7 variant, which is encoded by contiguous splicing of AR exons 1/2/3/CE3, is upregulated in a variety of cancer cell types, and is associated with both cancer progression and resistance to AR-targeted therapies.
Brand name for nicotine patch
A niacinamide derivative, a plasma membrane adenosine triphosphate (ATP)-sensitive potassium (K+) (KATP) channel activator and a nitric oxide (NO) donor, with vasodilatory, antihypertensive and potential cardio- and lung-protective activities. Upon administration, nicorandil binds to and opens KATP channels, which causes relaxation of vascular smooth muscles, stimulates vasodilatation, reduces vasoresistance, decreases blood pressure and protects the myocardium against ischemia. In addition, nicorandil exerts nitrate-like properties, through the stimulation of guanylate cyclase, the downregulation of Rho-kinase activity and the further promotion of venous vasodilation. Although the mechanism of action has not been fully elucidated, nicorandil may exhibit protective activity against radiation-induced lung and heart toxicity, possibly by preventing both accumulation of reactive oxygen species (ROS) and ROS-induced cellular damage.
Brand name for nicotine gum
An orally available form of vitamin B3 and precursor of nicotinamide adenine dinucleotide (NAD+) with potential use in the treatment of chemotherapy induced peripheral neuropathy (CIPN). Upon oral administration, nicotinamide riboside (NR) is converted to nicotinamide mononucleotide by the NR kinases, nicotinamide riboside kinase 1 (NRK 1) and nicotinamide riboside kinase 2 (NRK 2), to which a second adenine is transferred by nicotinamide mononucleotide adenylyl transferase to generate NAD+. NAD+, an essential redox coenzyme, may offer protective effects against axonal injury from both mechanical and neurotoxic injury, and maintenance of NAD+ may be protective in mitochondrial disease. NR may help elevate and maintain NAD+ levels, which may ameliorate potential mechanisms implicated in the development of CIPN including mitochondrial dysfunction and peripheral nerve degeneration.
A plant alkaloid, found in the tobacco plant, and addictive central nervous system (CNS) stimulant that causes either ganglionic stimulation in low doses or ganglionic blockage in high doses. Nicotine acts as an agonist at the nicotinic cholinergic receptors in the autonomic ganglia, at neuromuscular junctions, and in the adrenal medulla and the brain. Nicotine's CNS-stimulating activities may be mediated through the release of several neurotransmitters, including acetylcholine, beta-endorphin, dopamine, norepinephrine, serotonin, and ACTH. As a result, peripheral vasoconstriction, tachycardia, and elevated blood pressure may be observed with nicotine intake. This agent may also stimulate the chemoreceptor trigger zone, thereby inducing nausea and vomiting.
A chewing gum containing nicotine used as a substitute for the active ingredient in tobacco. Nicotine chewing gum reduces the withdrawal symptoms associated with smoking cessation.
A lozenge preparation containing the alkaloid nicotine with nicotine replacement activity. Upon administration of the lozenge, nicotine is released and, although nicotine binds to nicotinic cholinergic receptors at the autonomic ganglia, adrenal medulla and at neuromuscular junctions as well, the binding of nicotine to the receptors in the central nervous system (CNS) appears to be responsible for the addictive nature of nicotine. Binding to CNS nicotinic acetylcholine receptors causes the release of the neurotransmitter dopamine which appears to be responsible for the addiction of nicotine. Administration of nicotine may prevent nicotine craving and may help with the withdrawal symptoms associated with smoking cessation.
A method for nicotine replacement.
A transepidermal patch designed to deliver nicotine, the addictive substance contained in cigarettes, directly through the skin and into the blood stream. Used for cessation of smoking.
Brand name for nicotine nasal spray
A low fucose, fully-humanized monoclonal immunoglobulin G1 (IgG1) antibody (hmAb) against the interleukin 1 receptor accessory protein (interleukin-1 receptor associated protein; IL1RAP), with potential immunomodulating, anti-inflammatory and antineoplastic activities. Upon intravenous administration, nidanilimab targets and binds to IL1RAP, thereby preventing IL1RAP-mediated signaling, and disrupting IL-1 and IL-33 mediated nuclear factor kappa beta (NFkB) activation. This prevents the secretion of tumor stimulating cytokines, decreases tumor inflammation and inhibits tumor cell proliferation. In addition, nidanilimab induces antibody-dependent cellular cytotoxicity (ADCC), and stimulates natural killer (NK) cells to attack tumor cells, thereby killing the IL1RAP-poisitive tumor cells. IL1RAP, a co-receptor of the IL-1 receptor (IL1R1) and the IL-33 receptor (ST2), is upregulated in certain tumor cells, and plays a key role in tumor cell proliferation.
Brand name for iron
A nitrofuran derivative with antiprotozoal and potential antineoplastic activities. Nifurtimox is reduced by cytosol enzymes or flavin-containing microsomal enzymes to a highly reactive nitro anion free radical; autooxidation of the nitro anion free radical generates cytotoxic superoxide anion (02-). In addition, nifurtimox-derived nitro anion free radicals may alkylate macromolecules such as nucleic acids and proteins, resulting in the disruption of their structure and function.
Brand name for nilutamide
The monohydrate monohydrochloride form of nilotinib, an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance resulting from Bcr-Abl kinase mutations, upon administration, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl portion of the Bcr-Abl fusion protein, resulting in the inhibition of the constitutive kinase activity of Bcr-Abl protein. This inhibits the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. Nilotinib also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R; PDGFR), mast/stem cell growth factor receptor Kit (c-Kit), and, to a lesser extent, colony-stimulating factor 1 receptor (CSF-1R; CSF1R), and discoidin domain-containing receptor 1 (DDR1).
A synthetic, nonsteroidal agent with antiandrogenic properties. Nilutamide preferentially binds to androgen receptors and blocks androgen receptor activation by testosterone and other androgens; this agent may inhibit androgen-dependent growth of normal and neoplastic prostate cells.
Brand name for cisatracurium besylate
A dihydropyridine derivative and an analogue of the calcium channel blocker nifedipine, with antihypertensive activity. Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably because this agent can cross the blood brain barrier due to its lipophilic nature. Furthermore, this agent also inhibits the drug efflux pump P-glycoprotein, which is overexpressed in some multi-drug resistant tumors, and may improve the efficacy of some antineoplastic agents.
Brand name for nimodipine
A humanized monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Nimotuzumab binds to and inhibits EGFR, resulting in growth inhibition of tumor cells that overexpress EGFR. This agent may act synergistically with radiation therapy.
A nitrosourea with antineoplastic activity. Nimustine alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death.
The tosylate salt form of ningetinib, an orally available inhibitor of the receptor tyrosine kinases c-MET/hepatocyte growth factor receptor (HGFR), vascular endothelial growth factor receptor 2 (VEGFR2 KDR), Axl (UFO), Mer, and Fms-like tyrosine kinase 3 (Flt3; CD135; STK1; FLK2), with antineoplastic activity. Upon administration, ningetinib binds to a variety of kinases, including c-Met, VEGFR2, Axl, Mer and Flt3, thereby inhibiting their signaling pathways. This inhibits growth, angiogenesis and metastasis of tumor cells that overexpress these kinases. c-Met, VEGFR2, Axl, Mer and Flt3 are overexpressed by many tumor cell types and play key roles in tumor cell proliferation, survival, invasion and metastasis.
Brand name for ixazomib citrate
An orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhibitor BIBF 1120 selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. In addition, this agent also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (fms-like tyrosine kinase 3). VEGFR, FGFR and PDGFR RTKs play key roles in tumor angiogenesis.
Brand name for pentostatin
A synthetic near infrared fluorescent (NIRF) imaging agent that can potentially be used to detect the presence of certain cancers. Upon intravenous administration, VM110 is specifically cleaved by certain proteases, including cathepsins B, L, and S, and plasmin, which are highly expressed in various types of cancer. Proteolysis liberates a highly fluorescent cleavage product, which can be detected in vivo by NIRF imaging techniques. Thus, tumor cells can be visualized and the presence of micrometastases may be assessed.
An orally bioavailable, hydrated, tosylate salt form of niraparib, an inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2 (PARP-1 and -2), with antineoplastic activity. Upon administration, niraparib binds to and inhibits the activity of PARP-1 and -2, thereby inhibiting PARP-1 and -2-mediated DNA repair, enhancing the accumulation of DNA strand breaks, promoting genomic instability and resulting in apoptosis. The PARP family of proteins catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks.
A selective gamma secretase (GS) inhibitor with potential antitumor activity. Nirogacestat binds to GS, blocking proteolytic activation of Notch receptors; Notch signaling pathway inhibition may follow, which may result in the induction of apoptosis in tumor cells that overexpress Notch. The integral membrane protein GS is a multi-subunit protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors, at residues within their transmembrane domains. Overexpression of the Notch signaling pathway has been correlated with increased tumor cell growth and survival.
A synthetic benzamide with antiprotozoal activity. Nitazoxanide exerts its antiprotozoal activity by interfering with the pyruvate ferredoxin/flavodoxin oxidoreductase dependent electron transfer reaction, which is essential to anaerobic energy metabolism. PFOR enzyme reduces nitazoxanide, thereby impairing the energy metabolism. However, interference with the PFOR enzyme-dependent electron transfer reaction may not be the only pathway by which nitazoxanide exhibits antiprotozoal activity. Nitazoxanide is active against Giardia lamblia and Cryptosporidium parvum.
A nitric oxide (NO) donating derivative of acetylsalicyclic acid with anti-inflammatory, analgesic, antipyretic, antithrombotic, gastroprotective and potential antitumor activities. The acetylsalicylic acid derivative moiety of this agent inhibits the activities of cyclooxygenase (COX) I and II, preventing the formation of prostaglandins and thromboxanes. A reduction in prostaglandin synthesis accounts for this agent's anti-inflammatory, anti-pyretic and analgesic activities; a reduction in thromboxane A2 synthesis results in an irreversible inhibition of platelet aggregation. NO donation by this agent, after cleavage from the acetylsalicylic acid derivative in vivo, may protect the gastric mucosa against the damaging effects of the aspirin derivative by modulating prostaglandins. In tumor cells, the NO donating moiety may block the cell cycle in the G1 and G2 phases and may induce apoptosis through caspase-mediated mechanisms.
An organic nitrate with vasodilator activity. Nitroglycerin is converted into nitric oxide (NO) in smooth muscle and activates guanylyl cyclase, thereby increasing cGMP concentration, and resulting in smooth muscle relaxation. Dilatation of the veins results in decreased venous return to the heart, thereby decreasing left ventricular volume (reduced preload) and decreasing myocardial oxygen requirements. Arteriolar relaxation reduces arteriolar resistance (reduced afterload), thereby decreasing myocardial oxygen demands. In addition, nitroglycerin causes coronary artery dilatation, thereby improving myocardial blood distribution.
A sustained-release transdermal patch containing the organic nitrate nitroglycerin, with vasodilator and potential immunomodulating activities. Upon application to the skin, nitroglycerin is continuously released from the patch and absorbed. In turn, nitroglycerin is converted into nitric oxide (NO), which activates guanylyl cyclase, increasing cyclic guanosine monophosphate concentration thus resulting in smooth muscle relaxation. In addition, activation of NO-mediated signaling pathways may inhibit hypoxia-induced tumor cell invasiveness, chemoresistance, evasion of immune cell recognition and cancer cell progression. Particularly, reactivation of NO-mediated signaling appears to inhibit the increased tumor cell shedding of the major histocompatibility complex class I chain-related (MIC) molecules MICA and MICB as is seen in hypoxic tumor environments; MIC molecules play key roles in tumor cell immune surveillance through their interaction with the C-type lectin-like NKG2D receptor on natural killer, lymphokine-activated killer and effector T cells.
An antimicrobial lock solution (ALS) containing the nitrate nitroglycerin, sodium citrate and ethanol, with potential antimicrobial and anticoagulant activities. Upon application to the catheter as an ALS, the nitroglycerin is converted into nitric oxide (NO), which exerts antimicrobial activity. The citrate exerts anticoagulant activity, thereby preventing blood clotting and occlusion and maintaining the fluidity of the administered solution. In addition, both citrate and ethanol exert antimicrobial activity. This may prevent bacterial colonization on the surface of the catheter, biofilm formation, and catheter-associated infections.
A Chinese herbal medicine (CHM) composed of the dried root from the herbaceous plant Ox-Knee (Achyranthes bidentata Blume) belonging to the Amaranthaceae family. Niu Xi may regulate the blood, may help relieve certain pains, and it may tonify the liver and kidneys.
A fully human immunoglobulin (Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed death-1 (PD-1, PCD-1) with immune checkpoint inhibitory and antineoplastic activities. Upon administration, nivolumab binds to and blocks the activation of PD-1, an immunoglobulin superfamily (IgSF) transmembrane protein, by its ligands programmed cell death ligand 1 (PD-L1), which is overexpressed on certain cancer cells, and programmed cell death ligand 2 (PD-L2), which is primarily expressed on antigen-presenting cells (APCs). This results in the activation of T cells and cell-mediated immune responses against tumor cells. Activated PD-1 negatively regulates T-cell activation and plays a key role in tumor evasion from host immunity.
Brand name for ketoconazole
A nucleotide-binding domain and leucine-rich repeat (NLR) family pyrin domain containing 3 (NLRP3; NACHT, LRR and PYD Containing Protein 3; NALP3) agonist with potential immunomodulatory and antineoplastic activities. Upon administration, NLRP3 agonist BMS-986299 binds to and activates NLRP3, potentially promoting NLRP3 inflammasome-mediated secretion of interleukin-8 (IL-8), which may induce tumoricidal activity of natural killer (NK) cells against tumor cells. NLRP3, a sensor component of the NLRP3 inflammasome plays a significant role in immunity and inflammation, and may protect against tumorigenesis in some cancers.
An orally bioavailable antiangiogenic isocoumarin with potential antineoplastic activity. NM-3 inhibits vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor, thereby inhibiting endothelial cell proliferation. This agent also induces apoptosis by a mechanism involving reactive oxygen species.
A water-soluble organic solvent. As an adjuvant antineoplastic agent, N-methylformamide depletes cellular glutathione, a key molecule involved in the antioxidation of reactive oxygen species (ROS) and other free radicals, thereby enhancing ionizing radiation-induced DNA cross-linking in and terminal differentiation of tumor cells.
The dihydrochloride salt of nolatrexed, a water-soluble lipophilic quinazoline folate analog with antineoplastic activity. Nolatrexed occupies the folate binding site of thymidylate synthase, resulting in inhibition of thymidylate synthase activity and thymine nucleotide synthesis with subsequent inhibition of DNA replication, DNA damage, S-phase cell cycle arrest, and caspase-dependent apoptosis. This agent also exhibits radiosensitizing activity.
A monovalent vaccine containing hemagglutinin (HA) of influenza A (H1N1)-like virus with potential immunomodulating activity. Upon administration, non-adjuvanted A(H1N1) influenza vaccine may stimulate the immune system to mount an antibody response against H1N1.
A non-small cell lung cancer (NSCLC) vaccine containing modified mRNAs encoding cancer-testis antigen NY-ESO-1, melanoma-associated antigens C1 (MAGE-C1/CT7) and C2 (MAGE-C2/CT10), survivin, and the oncofetal antigen 5T4 with potential antitumor and immunomodulatory activities. Upon subcutaneous administration, non-small cell lung cancer mRNA-derived vaccine CV9201 may stimulate the immune system to mount a cytotoxic, antigen-specific T lymphocyte response (CTL) against NSCLC cells. The modified mRNAs in this vaccine are taken up by cells after injection and exhibit enhanced translational potency. The five tumor-associated antigens (TAAs) encoded by these mRNAs are frequently expressed by NSCLC cells.
Brand name for ethinyl estradiol/norethindrone
Brand name for vecuronium bromide
Brand name for ethinyl estradiol/levonorgestrel
A synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine. Norepinephrine acts directly on the alpha- and beta-adrenergic receptors. Clinically, norepinephrine is used as a peripheral vasoconstrictor that causes constriction of arterial and venous beds via its alpha-adrenergic action. It is also used as a potent inotropic and chronotropic stimulator of the heart mediated through its beta-1 adrenergic action.
Brand name for ethinyl estradiol/norethindrone
The orally bioavailable acetate salt of norethindrone, a synthetic progestin with some anabolic, estrogenic, and androgenic activities. As do all progestins, norethindrone binds to and activates nuclear progesterone receptors (PRs) in target tissues such as the pituitary and reproductive system; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes, followed by various transcriptional events and histone acetylation. Physiological effects include the inhibition of luteinizing hormone (LH) release, an increase in the endometrial luteal-phase, and alterations in endocervical mucus secretion.
Brand name for orphenadrine citrate
A synthetic progestin commonly used alone or in combination with an estrogen for contraception. Norgestrel suppresses the secretion of luteinizing and follicle-stimulating hormones (LH and FSH), thickens cervical mucus, and slows the transit of ova through the fallopian tubes. This agent also exhibits antiproliferative activity in endometrial tissue and may exhibit chemopreventive and antineoplastic activities in endometrial carcinoma.
Brand name for tolazamide
Brand name for ethinyl estradiol/norethindrone
Brand name for norethindrone acetate
Brand name for levoketoconazole
Brand name for levonorgestrel
Brand name for desipramine hydrochloride
An orally available proprietary aqueous extract from the North American ginseng (Panax quinquefolius) dried root, primarily containing poly-furanosyl-pyranosyl-saccharides, with potential immunostimulating activity. Upon administration, North American ginseng extract AFX-2 may stimulate the proliferation and activation of B-lymphocytes and stimulates IgG production by B cells. Also, this agent induces maturation of dendritic cells, induces T cell proliferation and activates peritoneal exudate macrophages leading to an increase in the production of the cytokines interleukin -1 and -6, tumor necrosis factor-alpha, interferon-gamma and nitric oxide.
Brand name for ethinyl estradiol/norethindrone
Brand name for ritonavir
The orally bioavailable hydrochloride salt of the opioid agonist noscapine, a phthalideisoquinoline alkaloid derived from the opium poppy Papaver somniferum, with mild analgesic, antitussive, and potential antineoplastic activities. Noscapine binds to tubulin and alters its conformation, resulting in a disruption of the dynamics of microtubule assembly (by increasing the time that microtubules spend idle in a paused state) and, subsequently, the inhibition of mitosis and tumor cell death. Unlike other tubulin inhibitors such as the taxanes and vinca alkaloids, noscapine does not affect microtubule polymerization.
A synthetic small molecule with potential antineoplastic activity. MK0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. The Notch signaling pathway plays an important role in cell-fate determination, cell survival, and cell proliferation.
Brand name for tropisetron hydrochloride
Brand name for recombinant human chorionic gonadotropin
Brand name for soy isoflavones
Brand name for hydromorphone hydrochloride
Brand name for insulin, NPH
Brand name for posaconazole
Brand name for romiplostim
A member of the synthetic oleanane triterpenoid class of compounds and an activator of nuclear factor erythroid 2 [NF-E2]-related factor 2 (Nrf2, Nfe2l2), with potential chemopreventive activity. Upon administration, RTA 408 activates the cytoprotective transcription factor Nrf2. In turn, Nrf2 translocates to the nucleus, dimerizes with a small Maf protein (sMaf), and binds to the antioxidant response element (ARE). This induces the expression of a number of cytoprotective genes, including NAD(P)H quinone oxidoreductase 1 (NQO1), sulfiredoxin 1 (Srxn1), heme oxygenase-1 (HO1, HMOX1), superoxide dismutase 1 (SOD1), gamma-glutamylcysteine synthetase (gamma-GCS), thioredoxin reductase-1 (TXNRD1), glutathione S-transferase (GST), glutamate-cysteine ligase catalytic subunit (Gclc) and glutamate-cysteine ligase regulatory subunit (Gclm), and increases the synthesis of the antioxidant glutathione (GSH). Nrf2, a leucine zipper transcription factor, plays a key role in the maintenance of redox balance and cytoprotection against oxidative stress.
A non-nucleoside, polymerase inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B), a RNA-dependent RNA polymerase, with potential activity against HCV. Upon administration and after intracellular uptake, BMS-791325 allosterically binds to the non-catalytic Thumb 1 site of viral HCV NS5B polymerase and causes a decrease in viral RNA synthesis and replication. The HCV NS5B protein is essential for the replication of the viral HCV RNA genome. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family.
Exosomes loaded with non-small cell lung cancer (NSCLC)-specific antigens, with potential immunostimulating and antineoplastic activities. Exosomes derived from autologous maturing dendritic cells (DCs) are pulsed with HLA-DP04-restricted MAGE-3, and HLA-A02-restricted peptides NY-ESO-1, MAGE-1, MAGE-3, and MART-1. Upon vaccination, these exosomes may stimulate natural killer (NK) cell activation and proliferation, restoration of NKG2D expression on NK cells, and antigen-specific T-cell responses. This may eventually lead to inhibition of tumor cell proliferation in NSCLC expressing these specific tumor antigens. These exosomes, nanovesicles secreted from DCs, are embedded with molecules necessary for potent immune responses on the exosomal surface, such as MHC class II molecules, CD40, ICAM-1, IL-15Ralpha, and NKG2D ligands.
An orally available inhibitor of the receptor tyrosine kinases C-ros oncogene 1 (ROS1) and the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, with potential antineoplastic activity. Upon oral administration, DS-6051b binds to and inhibits ROS1 and the NTRK family members. This inhibition leads to a disruption of ROS1- and NTRK-mediated signaling and eventually inhibits the growth of tumor cells that are overexpressing ROS1 and/or NTRKs. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells. NTRK mutations or rearrangements play a key role in cancer progression.
Brand name for mepolizumab
A deoxycytosine analog with potential antineoplastic activity. Upon administration, DFP-10917 is phosphorylated to generate its nucleotide form, which functions as a deoxycytosine mimic and is incorporated into DNA in tumor cells. This causes DNA strand breaks during polymerization due to beta-elimination during the fidelity checkpoint, which results in G2/M phase-arrest and tumor cell apoptosis.
A phosphoramidate-based prodrug of the monophosphate (MP) form of 5-fluoro-2'-deoxyuridine (FUdR; FUDR), the active metabolite of fluorouracil (5-FU), an antimetabolite fluoropyrimidine analog of the pyrimidine nucleoside, with potential antineoplastic activity. Upon administration of the nucleotide analog prodrug NUC-3373, NUC-3373 is readily taken up by tumor cells. In the tumor cell, the phosphoramidate moiety is removed and NUC-3373 is converted to its active form FUDR-MP. In turn, FUDR-MP binds to and inhibits thymidylate synthase (TS), resulting in the depletion of thymidine triphosphate (TTP) and thus DNA synthesis. With the phosphoramidate moiety attached to FUDR-MP, NUC-3373, compared to 5-FU, is more lipophilic and accumulates in cancer cells by passive diffusion and does not require a nucleoside transporter, thereby generating higher intracellular concentrations. In addition, compared to 5-FU, once inside the cell FUDR-MP does not need to be phosphorylated and is already in its active form. Unlike 5-FU, NUC-3373 does not get deactivated or converted into toxic metabolites by dihydropyrimidine dehydrogenase (DPD) and thymidine phosphorylase (TP), which leads to both a longer half-life and less toxicity.
A prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations.
Brand name for oxymorphone hydrochloride
An orally available nutritional supplement and proprietary formulation containing extracts from the sea cucumber, sea sponge, shark fin, sea urchin and the marine grass Sargassum, with potential antioxidant, antitumor, anti-angiogenic and immunomodulating activities. TBL-12 contains various amino acids, minerals, vitamins and omega-3 fatty acids.
Brand name for therapeutic hydrocortisone
Brand name for glutamine
A nutritional supplement composed of nutrient-rich whole wheat flour-based bread mix, with potential anti-cachexia activity. Following the production of an unleavened bread from the mix and upon oral intake of the nutrient-rich whole wheat flour supplement, the various nutrients in the bread may improve cachexia symptoms. The bread is made from the flour of pulverized whole wheat from an Indian crop.
Brand name for nutritious semisolid food gel
Brand name for nutritious semisolid food gel with phenethyl isothiocyanate
A calorie-dense nutritional supplement drink containing a variety of vitamins and minerals. Nutritional supplement drink contains vitamin A, vitamin C, D, E and K, calcium, iron, thiamin, riboflavin, niacin, folate, vitamin B6, vitamin B12, pantothenic acid, biotin, phosphorus, iodine, magnesium, zinc, selenium, copper, manganese, chromium, molybdenum, chloride and choline. In addition, this drink contains protein, fiber and fa, including omega-3 fatty acids.
A liquid, milk protein-based, pediatric nutritional supplement containing a variety of vitamins and minerals. Nutritional supplement drink (pediatric) contains vitamins and minerals such as vitamin A, vitamin C, D, E and K, calcium, iron, thiamin, riboflavin, niacin, folate, vitamin B6, vitamin B12, pantothenic acid, biotin, phosphorus, iodine, magnesium, zinc, selenium, copper, manganese, chromium, molybdenum, chloride and choline. In addition, this supplement contains soy protein isolate and medium-chain triglycerides (MCTs), sucrose and short-chain oligofructosaccharides.
A proprietary, flavored, semisolid food gel-based nutritional supplement containing a variety of vitamins, iron, calcium, protein, fat and carbohydrates, that can be consumed for nutritional support. Upon oral intake, the nutritious semisolid food gel may prevent malnutrition and weight loss. The food gel has a semisolid texture and is specifically formulated for patients who have difficulty chewing and swallowing.
A proprietary, flavored, semisolid food gel-based nutritional supplement containing a variety of vitamins, iron, calcium, protein, fat and carbohydrates, in combination with the phytochemical phenethyl isothiocyanate (PEITC), that can be consumed for nutritional support, and with chemopreventive and anti-cancer activities. Upon oral intake, the nutritious semisolid food gel may aid in the prevention of malnutrition and weight loss. The food gel has a semisolid texture and is specifically formulated for patients who have difficulty chewing and swallowing. PEITC may delay cancer growth, and inhibit cancer cell migration and invasion.
Brand name for armodafinil
Brand name for visilizumab
A cancer vaccine consisting of an immunogenic peptide derived from the cancer-testis antigen (NY-ESO-1), an antigen found in normal testis and various tumors. Vaccination with NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response to cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis.
A plasmid DNA encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1 with potential immunostimulating and antitumor activities. Upon adninstration, NY-ESO-1 plasmid DNA cancer vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing the NY-ESO-1 antigen, resulting in tumor cell lysis. NY-ESO-1 is a tumor associated antigen (TAA) found in normal testes and expressed on the surfaces of various tumor cells, including melanoma, breast, bladder, prostate, lung, ovarian, and hepatocellular tumor cells.
A cancer vaccine consisting of an immunogenic peptide derived from the cancer-testis antigen (NY-ESO-1) and emulsified in the immunoadjuvant Montanide ISA-51 VG, with potential immunomodulating and antineoplastic activities. Upon subcutaneous vaccination, the NY-ESO-1 protein vaccine emulsified in Montanide ISA-51 VG may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing the NY-ESO-1 antigen, resulting in tumor cell lysis. NY-ESO-1, an antigen found in normal testes and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. The surfactant mannide monooleate in Montanide ISA 51 VG is derived from vegetable-grade (VG) oleic acid that was purified from olive oil.
A combination preparation composed of a protein derived from the human tumor-associated antigen (TAA) cancer-testis antigen 1 (NY-ESO-1) and a microparticle combining two immune-modifying components derived from the bacterium Propionibacterium acnes, a bacterial cell wall component that is rich in muramyl dipeptide (MDP) and bacteria-derived single-stranded DNA fragments, with potential immunomodulating, immunoadjuvant and antineoplastic activities. Upon administration of NY-ESO-1 protein/microparticle MDP/bacterial DNA-containing MIS416 vaccine, MIS416 localizes in and is taken up mainly by the liver, thereby forming a liver depot. MIS416 is then taken up by immune cells, such as monocytes and dendritic cells (DCs), where MDP and the bacterial DNA target and bind to the cytosolic innate pattern recognition receptors (PRRs) nucleotide-binding oligomerization domain-containing protein 2 (NOD2), and toll-like receptor 9 (TLR9), respectively. The simultaneous binding and activation of both NOD2 and TLR9, leads to activation of both NOD2 and TLR9 signaling pathways. This stimulates the innate immune system, induces secretion of cytokines, particularly interferon (IFN), and modulates the activation of various immune cells. In the presence of the NY-ESO-1 peptide, MIS416 enhances the cytotoxic T-lymphocyte (CTL)-mediated immune response against NY-ESO-1, resulting in an increased anti-tumor immune response. NY-ESO-1 is expressed in normal testes and on the surfaces of various tumor cells, and plays a key role in tumor cell proliferation and survival.
Human autologous peripheral blood lymphocytes (PBLs) transduced with a retroviral vector encoding a T cell receptor (TCR) specific for the cancer-testis antigen NY-ESO-1, with potential antineoplastic activity. Upon isolation, transduction, expansion ex vivo, and reintroduction into the patient, the NY-ESO-1 reactive TCR-transduced autologous PBLs bind to NY-ESO-1-overexpressing tumor cells. This may result in a specific cytotoxic T-lymphocyte (CTL) killing of NY-ESO-1-positive cancer cells. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cell types; the TCR is specific for NY-ESO-1:157-165.
A cell-based cancer vaccine composed of autologous dendritic cells (DCs) pulsed with a peptide derived from the tumor associated antigen human cancer-testis antigen NY-ESO-1 (NY-ESO-1(157-165)), with potential immunostimulatory and antineoplastic activities. Upon administration, the NY-ESO-1(157-165) peptide-pulsed autologous dendritic cell vaccine may stimulate the immune system to mount both an anti-tumoral cytotoxic T-lymphocyte (CTL) and an antibody-mediated immune response against NY-ESO-1-expressing tumor cells, which may result in tumor cell lysis. NY-ESO-1 is expressed both in normal testes and on the surfaces of various tumor cells, and plays a key role in tumor cell proliferation and survival.
A cancer vaccine composed of a recombinant form of the tumor antigen NY-ESO-1 and glucopyranosyl lipid adjuvant (GLA)-stable emulsion (GLA-SE), with potential antineoplastic and immunomodulating activities. Upon intramuscular injection, the adjuvant portion of the NY-ESO-1/GLA-SE vaccine ID-G30 binds to toll-like receptor subtype 4 (TLR-4) expressed on dendritic cells (DCs), monocytes, macrophages and B cells. The activated DCs present the NY-ESO-1 antigen to Th1 CD4 T-lymphocytes. This leads to the induction of cytotoxic T lymphocytes (CTLs) and the killing of NY-ESO-1-expressing tumor cells. This vaccine also induces specific antibody responses and increases the production of inflammatory cytokines.