An orally-agent agent with potential antineoplastic activity. S-3304 inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
S-adenosyl-L-methionine disulfate p-toluene-sulfonate
The disulfate salt of the stable p-toluene-sulfonate complex of s-adenosyl-L-methionine (SAMe) with chemopreventive activity. SAMe disulfate p-toluene-sulfonate undergoes hydrolytic conversion to its active compound SAMe within cells. Although the mechanism of action is largely unknown, SAMe attenuates experimental liver damage and prevents experimental hepatocarcinogenesis. In addition, SAMe may reduce mitochondrial cytochrome C release, caspase 3 activation, and poly(ADP-ribose) polymerase cleavage, and attenuate okadaic acid-mediated hepatocyte apoptosis in a dose-dependent manner. SAMe is an essential compound in cellular transmethylation reactions and a precursor of polyamine and glutathione synthesis in the liver; SAMe deficiency is associated with chronic liver disease-associated decreases in the activity of methionine adenosyltransferase 1A (MAT1A), the enzyme that catalyzes the production of SAMe as the first step in methionine catabolism.
A disaccharide analogue of the anthracycline antineoplastic antibiotic doxorubicin. Sabarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent also induces apoptosis through a p53-independent mechanism. Sabarubicin is less cardiotoxic than doxorubicin.
A fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites was originally isolated from the myxobacterium Solangium cellulosum.
(Other name for: pilocarpine hydrochloride)
A salicylic acid derivative with potential antineoplastic activity. Salirasib dislodges all Ras isoforms from their membrane-anchoring sites, thereby preventing activation of RAS signaling cascades that mediated cell proliferation, differentiation, and senescence. RAS signaling is believed to be abnormally activated in one-third of human cancers, including cancers of the pancreas, colon, lung and breast.
A genetically stable Salmonella typhimurium strain, attenuated by chromosomal deletion of the purI and msbB genes, with tumor-targeting activity. In rodent models, salmonella VNP20009 has been shown to selectively accumulate and grow in a variety of tumor types, inhibiting the growth of primary and metastatic tumors. This agent may be genetically engineered to contain trangenes that express therapeutic agents or cell surface tumor-associated antigen-specific antibodies, such as CEA-specific antibodies, which may improve its tumor targeting and therapeutic potential.
Salvia officinalis extract tablet
An oral tablet containing an extract of the plant Salvia officinalis (common sage) with reported antihydrotic, antibiotic, antihypertensive, anti-inflammatory, antioxidant, astringent, antispasmodic, estrogenic, and hypoglycemic properties. The primary biologically active component of common sage appears to be its essential oil which contains mainly cineol, borneol, and alpha- and beta-thujone. In addition, sage leaf contains numerous other substances including tannic acid; resins with oleic, ursonic, and ursolic acids; bitter substances with cornsole and cornsolic acid; fumaric, chlorogenic, caffeic and nicotinic acids; nicotinamide; flavones; flavone glycosides; and estrogenic substances. However, the mechanism(s) of action of common sage in the treatment of various disorders is unclear.
(Other name for: granisetron transdermal system)
(Other name for: cyclosporine)
(Other name for: cyclosporine)
(Other name for: therapeutic immune globulin)
(Other name for: octreotide acetate)
Sandostatin Lar Depot
(Other name for: octreotide acetate)
(Other name for: octreotide pamoate)
Sandostatin pamoate LAR
(Other name for: octreotide pamoate)
(Other name for: cyclosporine)
An orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity. Sapacitabine is hydrolyzed by amidases to the deoxycytosine analogue CNDAC (2'-Cyano-2'-deoxyarabinofuranosylcytosine), which is then phosphorylated into the active triphosphate form. As an analogue of deoxycytidine triphosphate, CNDAC triphosphate incorporates into DNA strands during replication, resulting in single-stranded DNA breaks during polymerization due to beta-elimination during the fidelity checkpoint process; cell cycle arrest in the G2 phase and apoptosis ensue. The unmetabolized prodrug may exhibit antineoplastic activity as well.
An adjuvant comprised of saponin, derived from the bark of Quillaia saponaria Molina, cholesterol and phospholipid with antigen-delivery and immunostimulatory activities. This saponin-based adjuvant in combination with various antigens, including those for human papilloma virus (HPV), hepatitis C virus (HCV), and the human cancer antigen NY-ESO-1, may result in potent antibody, CD4+ T-helper-cell, and CD8+ cytotoxic T-cell responses against the targeted antigen. In addition, this agent may reduce the amount of antigen necessary to induce an efficient immune response in the host.
An orally available 5-, 7-substituted anilinoquinazoline with anti-invasive and anti-tumor activities. Saracatinib is a dual-specific inhibitor of Src and Abl, protein tyrosine kinases that are overexpressed in chronic myeloid leukemia cells. This agent binds to and inhibits these tyrosine kinases and their effects on cell motility, cell migration, adhesion, invasion, proliferation, differentiation, and survival. Specifically, saracatinib inhibits Src kinase-mediated osteoclast bone resorption.
(Other name for: lonafarnib)
sargramostim plasmid DNA hepatocellular carcinoma vaccine adjuvant
A vaccine adjuvant consisting of a plasmid DNA encoding sargramostim (granulocyte-macrophage colony-stimulating factor). Upon administration, expressed sargramostim may stimulate a cytotoxic T cell response enhancing the host immune response to a concomitantly administered hepatocellular carcinoma vaccine.
sargramostim plasmid DNA melanoma vaccine adjuvant
A vaccine adjuvant consisting of a plasmid DNA encoding sargramostim (a granulocyte macrophage-colony stimulating factor). Upon administration, expressed sargramostim may stimulate a cytotoxic T cell response enhancing the host immune response to a concomitantly administered melanoma vaccine.
sargramostim plasmid DNA pancreatic tumor cell vaccine
A whole cell vaccine comprised of irradiated allogenic pancreatic tumor cells transfected with a plasmid DNA encoding human sargramostim (GM-CSF). Vaccination results in expression of GM-CSF, which induces proliferation and differentiation hematopoietic lineage cells as well as stimulating macrophage and dendritic cell functions in antigen presentation and antitumor cell-mediated immunity. Furthermore, administration of this pancreatic tumor cell vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor growth.
(Other name for: nabiximols)
(Other name for: metronidazole hydrochloride)
A synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis.
A proprietary oil-in-water emulsion specifically designed for combining protein preparations used in vaccines. SB-AS02B adjuvant contains monophosphoryl lipid A and QS21, a saponin extracted from the South American tree Quillaja saponaria Molina. This agent may be used for formulating cancer-specific vaccine preparations such as those containing MAGE-3 melanoma protein.
A vaccine adjuvant containing CpG 7909, monophosphoryl lipid, and QS-21 with potential antineoplastic and immunostimulatory activities. CpG 7909 is a synthetic 24-mer oligonucleotide containing 3 CpG motifs that selectively targets Toll-like receptor 9 (TLR9), thereby activating dendritic and B cells and stimulating cytotoxic T cell and antibody responses against tumor cells bearing tumor antigens. Monophosphoryl lipid is a detoxified derivative of lipid A, a component of Salmonella minnesota lipopolysaccharide (LPS); this agent may enhance humoral and cellular responses to various antigens. QS-21 is a purified, naturally occurring saponin derived from the South American tree Quillaja saponaria Molina and exhibits various immunostimulatory activities. Combinations of monophosphoryl lipid and QS-21 may be synergistic in inducing humoral and cellular immune responses.
Sclerosol Intrapleural Aerosol
(Other name for: talc)
(Other name for: lactobacillus fermented extract)
selective androgen receptor modulator GTx-024
A non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.
selective androgen receptor modulator MDV3100
An orally bioavailable, organic, non-steroidal small molecule targeting the androgen receptor (AR) with potential antineoplastic activity. Through a mechanism that is reported to be different from other approved AR antagonists, selective androgen receptor modulator MDV3100 inhibits the activity of prostate cancer cell ARs, which may result in a reduction in prostate cancer cell proliferation and, correspondingly, a reduction in the serum prostate specific antigen (PSA) level. AR over-expression in prostate cancer represents a key mechanism associated with prostate cancer hormone resistance.
An orally bioavailable, small-molecule cyclin-dependent kinase (CDK) inhibitor with potential proapoptotic and antineoplastic activities. Seliciclib primarily inhibits CDK2/E, CDK2/A, CDK7 and CDK9 by competing for their ATP binding sites, leading to a disruption of cell cycle progression. In addition, this agent appears to interfere with CDK-mediated phosphorylation of the carboxy-terminal domain of RNA polymerase II, inhibiting RNA polymerase II-dependent transcription, which may result in the down-regulation of antiapoptotic proteins such as induced myeloid leukemia cell differentiation protein Mcl-1. CDKs, serine/threonine kinases that play an important role in cell cycle regulation, are overexpressed in various malignancies. Mcl-1 belongs to the Bcl-2 family of antiapoptotic proteins and is a protein crucial to the survival of a range of tumor cell types.
An orally bioavailable small molecule with potential antineoplastic activity. Selumetinib inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, and so may inhibit cellular proliferation in MEK-overexpressing tumor cells. MEK 1 and 2 are dual-specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various tumor cell types, and are drivers of diverse cellular activities, including cellular proliferation.
An ultralow-molecular-weight heparin (ULMWH) (Mw: 2000-3000 daltons) consisting of a polydisperse mixture of oligomeric heparin fragments with potential anticoagulant activity. Semuloparin binds to and activates antithrombin III (ATIII), which may result in the inhibition of activated factor Xa and, to a much lesser extent, factor IIa (thrombin) and so the inhibition of fibrin formation. Compared to low-molecular-weight heparins (LMWHs), AVE5026 exhibits an even higher ratio of anti-Factor Xa to anti-Factor IIa activity (>30:1). Compared to unfractionated heparins, the use of LMWHs is associated with lower incidences of major bleeding, osteoporosis and heparin-induced thrombocytopenia. Like LMWHs, this agent may inhibit tumor growth by regulating angiogenesis and apoptosis. AVE5026 is prepared by partial depolymerization of unfractionated porcine mucosal heparin.
An extract made from the dried leaflets on the pods of Cassia angustifolia or Cassia acutifolia with cathartic activity. Dimeric glycosides in dried senna extract are converted to the active monoanthrones by bacterial action in the colon. Through direct effects on enterocytes, enteric neurons, and muscle, monoanthrones produce giant migrating colonic contractions in addition to water and electrolyte secretion. As do other stimulant laxatives, monoanthrones may induce a limited low-grade inflammation in the colon through activation of prostaglandin/cyclic AMP and nitric oxide/cyclic GMP pathways and perhaps inhibition of Na+, K+-ATPase.
The fruit of Cassia acutifolia and Cassia angustifolia (Cassia) with laxative and purgative activities. The active ingredients in senna fruit include the hydroxyanthracene glycosides sennosides A and B (rhein dianthrones) and sennosides C and D (rhein aloe-emodin heterodianthrones).
Sennosides irritate the bowel lining and stimulate the bowel muscular coat, particularly in the colon, resulting in accelerated bowel transit and evacuation.
(Other name for: cinacalcet hydrochloride)
(Other name for: bupivacaine hydrochloride)
A small-molecule proapoptotic agent with potential antineoplastic activity. Sepantronium bromide selectively inhibits survivin expression in tumor cells, resulting in inhibition of survivin antiapoptotic activity (via the
extrinsic or intrinsic apoptotic pathways) and tumor cell apoptosis. Survivin, a member of the inhibitor of apoptosis (IAP) gene family, is expressed during embryonal development and is absent in most normal, terminally differentiated tissues; upregulated in a variety of human cancers, its expression in tumors is associated with a more aggressive phenotype, shorter survival times, and a decreased response to chemotherapy.
(Other name for: trimethoprim-sulfamethoxazole)
serine protease inhibitor WX-671
An orally bioavailable, 3-amidinophenylalanine-derived, second generation serine protease inhibitor prodrug targeting the human urokinase plasminogen activator (uPA) system with potential antineoplastic and antimetastatic activities. After oral administration, serine protease inhibitor WX-671 is converted to the active N?-(2,4,6-triisopropylphenylsulfonyl)-3-amidino-(L)-phenyla lanine-4-ethoxycarbonylpiperazide (WX-UK1), which inhibits several serine proteases, particularly uPA; inhibition of uPA may result in the inhibition of tumor growth and metastasis. uPA is a serine protease involved in degradation of the extracellular matrix and tumor cell migration and proliferation.
serine/threonine kinase inhibitor XL418
A selective, orally active small molecule, targeting protein kinase B (PKB or AKT) and ribosomal protein S6 Kinase (p70S6K), with potential antineoplastic activity. XL418 inhibits the activities of PKB and p70S6K, both acting downstream of phosphoinosotide-3 kinase (PI3K). These kinases are often upregulated in a variety of cancers. Inhibition of PKB by this agent will induce apoptosis, while inhibition of p70S6K will result in the inhibition of translation within tumor cells.
(Other name for: clomiphene citrate)
The hydrochloride salt of sertraline, a synthetic derivative of naphthalenamine with anti-serotoninergic and anti-depressant properties. Sertraline appears to selectively inhibit the neuronal uptake of serotonin, raising serotonin levels in the CNS.
A fluorinated isopropyl ether with general anesthetic activity. Although the mechanism of action has not been fully elucidated, sevoflurane may interfere with the release and re-uptake of neurotransmitters at post-synaptic terminals, and/or alter ionic conductance following receptor activation by a neurotransmitter. This agent may also interact directly with the lipid matrix of neuronal membranes, thereby affecting gating properties of ion channels. In addition, sevoflurane may activate gamma-aminobutyric acid (GABA) receptors, hyperpolarizing cell membranes and resulting in a general anesthetic effect, a decrease in myocardial contractility and mean arterial pressure, and an increased respiratory rate.
A nutritional supplement gleaned from the exoskeleton of the shark. Shark cartilage inhibits metalloproteinases (MMPs) and possesses antiangiogenic and antimetastatic properties.
shark cartilage extract AE-941
A multifunctional antiangiogenic agent derived from shark cartilage with potential antineoplastic activity. Shark cartilage extract AE-941 competitively inhibits the binding of pro-angiogenic vascular endothelial growth factor (VEGF) to its cell receptor, thereby inhibiting endothelial cell proliferation. This agent also inhibits matrix metalloproteinases (MMPs), stimulates tissue plasminogen activator (tPA), and activates caspase-mediated apoptotic pathways in endothelial cells.
sheddase inhibitor INCB007839
An orally bioavailable inhibitor of the ADAM (A Disintegrin And Metalloprotease) family of multifunctional membrane-bound proteins with potential antineoplastic activity. Sheddase inhibitor INCB007839 represses the metalloproteinase "sheddase" activities of ADAM10 and ADAM17, which may result in the inhibition of tumor cell proliferation. The metalloproteinase domains of ADAMs cleave cell surface proteins at extracellular sites proximal to the cell membrane, releasing or "shedding" soluble protein etcodomains from the cell surface; the disintegrin domains of these multifunctional proteins interact with various components of the extracellular matrix (ECM). ADAM10 processes particular epithelial growth factor receptor (EGFR) ligands and appears to regulate Notch signaling through the cleavage of Notch and its related ligand delta-like ligand-1 (Dll-1). ADAM17 (also known as Tumor necrosis factor-Converting Enzyme or TACE) is involved in processing tumor
necrosis factor (TNF) from its membrane bound precursor to its soluble circulating form and in processing ligands for the epidermal growth factor receptor (EGFR) family.
short chain fatty acid HQK-1004
A short chain fatty acid (SCFA) with potential herpes simplex virus thymidine kinase gene (HSV-TK)-inducing activity. Upon administration, short chain fatty acid HQK-1004 may induce the expression of thymidine kinase (TK) by a silenced HSV-TK, which may activate a co-administered antiviral prodrug such as ganciclovir, resulting in the destruction of virally-infected cancer cells.
sialyl Lewis™-keyhole limpet hemocyanin conjugate vaccine
A vaccine consisting of the oligosaccharide antigen sialyl Lewis™ (CA19-9) conjugated to the nonspecific immunomodulator keyhole limpet hemocyanin (KLH), with potential antineoplastic activity. Upon administration, sialyl Lewis™-keyhole limpet hemocyanin conjugate vaccine may induce production of IgG and IgM antibodies as well as trigger an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells expressing the sialyl Lewis™ antigen.
Sialyl Lewis™ is a blood group antigen and a tumor-associated antigen associated with epithelial cancers such as breast cancer and various digestive cancers. Sialyl Lewis™ serves as a ligand for the cytokine-inducible cell adhesion molecule (CAM) E-selectin, an endothelial cell-specific type I transmembrane surface protein, thus facilitating hematogenous metastasis by mediating the adhesion of circulating cancer cells to vascular endothelium.
A proprietary, miniature biodegradable polymeric matrix containing small-interfering RNAs for the mutated KRAS oncogene, KRASG12D, (siG12D), with potential antitumor activity. Upon intratumoral injection, siG12D is released locally, thereby preventing translation of KRAS proteins and potentially inhibiting growth of tumor cells overexpressing KRAS. KRAS, a member of the small GTPase superfamily, is mutated in over 90% of human pancreatic ductal adenocarcinomas (PDAC) and is associated with tumor cell proliferation and reduced survival.
(Other name for: recombinant interleukin-6)
A synthetic, highly lipophilic derivative of camptothecin, with potential antineoplastic and radiosensitizing activities. Silatecan DB-67 binds to and stabilizes the topoisomerase I-DNA covalent complex, inhibiting the religation of topoisomerase I-mediated single-stranded DNA breaks and producing lethal double-stranded DNA breaks when encountered by the DNA replication machinery; inhibition of DNA replication and apoptosis follow. Camptothecin readily undergoes hydrolysis at physiological pH, changing its conformation from the active lactone structure to an inactive carboxylate form. Modifications on the E ring of camptothecin prevent binding of human serum albumin, which prefers the inactive carboxylate form, thereby enhancing the stability of the active lactone structure and resulting in prolonged agent activity. In addition, this agent may radiosensitize tumor cells.
The citrate salt of a pyrazolopyrimidinone derivative structurally related to zaprinast. Sildenafil selectively inhibits cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase, resulting in vasodilation in the corpus cavernosum of the penis and penile erection.
A human-mouse chimeric antibody, constructed from a murine antiinterleukin 6 (IL-6) monoclonal antibody, with antitumor and antiinflammatory activities. Containing the antigen-binding variable region of the murine antibody, CLB-IL-6-8, and the constant region of a human IgG1kappa immunoglobulin, siltuximab has high affinity for recombinant as well as native IL-6 and inhibits the binding of IL-6 to the IL-6 receptor (IL-6R), resulting in the blockade of the IL-6/IL-6R/gp130 signal transduction pathway, and, subsequently, antitumor and antiinflammatory activities.
An inorganic chemical with antiseptic activity. Silver nitrate can potentially be used as a cauterizing or sclerosing agent.
(Other name for: phosphatidylcholine-bound silybin)
(Other name for: basiliximab)
A lipid-lowering agent derived synthetically from a fermentation product of the fungus Aspergillus terreus. Hydrolyzed in vivo to an active metabolite, simvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells.
(Other name for: doxepin hydrochloride)
siRNA-expressing SV40 vector
A simian virus 40 (SV40)-based shuttle vector, encoding small interfering RNA (siRNA), with potential antineoplastic activity. The expression of siRNA in target tumor cells transfected with an siRNA-expressing SV40 vector may result in siRNA-mediated silencing of target oncogenes and, so, the inhibition of tumor cell growth and the induction of tumor cell death.
The phenylhydrazone 4,4'-dihydroxybenzophenone-2,4-dinitrophenylhydrazone formulated as a topical agent with immunomodulating and potential antineoplastic activities. Applied topically as a gel, sivifene may stimulate a local immune response against human papillomavirus (HPV)-induced cervical intraepithelial neoplasia (CIN).
(Other name for: dexamethasone)
(Other name for: diphenhydramine hydrochloride)
(Other name for: furosemide)
(Other name for: probenecid)
(Other name for: theophylline)
(Other name for: theophylline)
Smac mimetic GDC-0152
A second mitochondrial activator of caspases (Smac) mimetic inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic GDC-0152 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2, which may inhibit their activities and promote the induction of apoptosis through apoptotic signaling pathways. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding to and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains. Smac, the endogenous IAP antagonist, relies on its N-terminal four amino-acid motif for binding to IAPs.
SMAC mimetic LCL161
An orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity. SMAC mimetic LCL161 binds to IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9, which play essential roles in apoptosis (programmed cell death), necrosis and inflammation.
Smac mimetic TL32711
A synthetic small molecule and peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity. As a SMAC mimetic and IAP antagonist, TL32711 binds to and inhibits the activity of IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains.
SMO antagonist BMS 833923
An orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity. SMO antagonist BMS-833923 inhibits the sonic hedgehog (SHH) pathway protein SMO, which may result in a suppression of the SHH signaling pathway. SMO is a G-protein coupled receptor that lies just downstream of the SHH ligand cell surface receptor Patched-1 in the SHH pathway; in the absence of ligand Patched-1 inhibits SMO and ligand binding to Patched-1 results in increased levels of SMO. The SHH signaling pathway plays an important role in cellular growth, differentiation and repair; constitutive activation of this pathway is associated with uncontrolled cellular proliferation and has been observed in a variety of cancers.
Smoothened antagonist LDE225 topical
A topical formulation of the small-molecule Smoothened (Smo) antagonist LDE225 with potential antineoplastic activity. Upon topical application, smoothened antagonist LDE225 topical selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway and, so, the inhibition of tumor cells in which this pathway is abnormally activated. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Inappropriate activation of Hh pathway signaling and uncontrolled cellular proliferation, as is observed in a variety of cancers, may be associated with mutations in the Hh-ligand cell surface receptor Smo.
Smoothened antagonist LEQ506
An orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Smoothened antagonist LEQ506 selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway, thereby inhibiting tumor cell growth. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Dysregulated activation of Hh pathway signaling and uncontrolled cellular proliferation, as is observed in a variety of cancers, may be associated with mutations in the Hh-ligand cell surface receptor Smo.
SN-38-loaded polymeric micelles NK012
A formulation consisting of polymeric micelles loaded with the irinotecan metabolite SN-38 with potential antineoplastic activity. SN-38-loaded polymeric micelles NK012 is an SN-38-releasing nanodevice constructed by covalently attaching SN-38 to the block copolymer PEG-PGlu, followed by self-assembly of amphiphilic block copolymers in an aqueous milieu. SN-38 (7-ethyl-10-hydroxy-camptothecin), a biological active metabolite of the prodrug irinotecan (CPT-11), binds to and inhibits topoisomerase I by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication, and apoptosis. SN-38 has been reported to exhibit up to 1,000-fold more cytotoxic activity against various cancer cells in vitro than irinotecan. This formulation increases the water-solubility of SN-38 and allows the delivery of higher doses of SN-38 than those achievable with SN-38 alone.
sodium bicarbonate solution
An aqueous oral mouthwash solution containing the monosodium salt of carbonic acid with alkalinizing and antimucositis activities. Upon introduction into the mouth, the sodium bicarbonate dissociates, forming sodium and bicarbonate ions, which buffer excess hydrogen ion and elevates the oral pH. An alkaline oral environment is less prone to colonization with yeast and aciduric bacteria. In addition, this solution may help relieve mucositis and mucositis-induced pain by diluting human saliva, and cleansing and lubricating mucosal tissues of the mouth, tongue and oropharynx.
sodium bicarbonate/potassium bicarbonate/anhydrous citric acid
A combination preparation containing sodium bicarbonate, potassium bicarbonate, and anhydrous citric acid, with acid-neutralizing properties. This combination in water principally contains the antacids potassium citrate and sodium citrate, and is used for the relief of acid indigestion and heartburn. This combination does not contain aspirin, and therefore does not exert aspirin's analgesic or anti-inflammatory effects.
sodium biphosphate/sodium phosphate oral laxative
An oral hyperosmotic saline laxative containing sodium biphosphate and sodium phosphate. Sodium phosphate/sodium biphosphate oral laxative promotes retention of water in the bowel, thereby increasing stool water content and volume, which results in increased gastrointestinal motility and stool transit time and evacuation of colonic contents.
sodium carboxymethylcellulose dressing
A textile fiber dressing composed of sodium carboxymethylcellulose with potential wound-healing activity. Sodium carboxymethylcellulose dressing protects the wound site from external factors that may cause pain, promote infection, or slow the natural wound healing process. Sodium carboxymethylcellulose is a non-toxic, non-allergenic, anionic water-soluble polymer derived from cellulose.
The sodium salt of citrate with alkalinizing activity. Upon absorption, sodium citrate dissociates into sodium cations and citrate anions; organic citrate ions are metabolized to bicarbonate ions, resulting in an increase in the plasma bicarbonate concentration, the buffering of excess hydrogen ion, the raising of blood pH, and potentially the reversal of acidosis. In addition, increases in free sodium load due to sodium citrate administration may increase intravascular blood volume, facilitating the excretion of bicarbonate compounds and an anti-urolithic effect.
The sodium salt of dichloroacetic acid with potential antineoplastic activity. Dichloroacetate ion inhibits pyruvate dehydrogenase kinase, resulting in the inhibition of glycolysis and a decrease in lactate production. This agent may stimulate apoptosis in cancer cells by restoring normal mitochondrial-induced apoptotic signaling.
sodium ferric gluconate complex in sucrose
A compound containing elemental iron as the sodium salt of a ferric ion carbohydrate complex in an alkaline aqueous solution with approximately 20% sucrose w/v in water for injection, used to replete the total body content of iron. Iron is critical for normal hemoglobin and myoglobin syntheses to maintain
oxygen transport and various enzymatic processes, including the biosynthesis of deoxyribonucleotides catalyzed by ribonucleotide reductase (RNR).
An inorganic salt of fluoride used topically or in municipal water fluoridation systems to prevent dental caries. Fluoride appears to bind to calcium ions in the hydroxyapatite of surface tooth enamel, preventing corrosion of tooth enamel by acids. This agent may also inhibit acid production by commensal oral bacteria.
The sodium salt of glycididazole with potential radiosensitizing activity. Due to its low redox potential, glycididazole is selectively activated via bioreduction in hypoxic tumor cells and may sensitize hypoxic tumor cells to the cytotoxic effects of ionizing radiation.
sodium hyaluronate topical hydrogel
A proprietary topical gel formulation containing sodium hyaluronate with wound repair and skin moisturizing properties. Upon application, sodium hyaluronate topical hydrogel adheres to injured tissues, hydrates skin, and provides protection from further chemical or mechanical irritation. Hyaluronate, a non-sulfated glucosaminoglycan, is a chief component of the extracellular matrix in connective, epithelial, and neural tissues and contributes significantly to cell proliferation and migration.
A highly soluble, orally available trivalent arsenic-containing telomerase inhibitor with potential antitumor activity. Although the exact mechanism through which sodium metaarsenite exerts its effect has yet to be fully elucidated, this agent appears to target and bind to telomeric sequences, specifically TTAGGG repeats, leading to a shortening of telomeres, and subsequent induction of apoptosis and inhibition of tumor cell growth. In addition, sodium metaarsenite also leads to the translocation of the catalytic subunit of telomerase into the cytoplasm and inhibition of the activity of telomerase. Telomerase is active in most tumors cells and is responsible for the maintenance of telomere length and plays a key role in cellular proliferation, but is quiescent in normal, healthy cells. The susceptibility to sodium metaarsenite seems to be inversely correlated with initial length of telomeres.
The sodium salt of phenylbutyrate, a derivative of the short-chain fatty acid butyrate, with potential antineoplastic activity. Phenylbutyrate reversibly inhibits class I and II histone deacetylases (HDACs), which may result in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations.
sodium picosulfate/magnesium oxide/citric acid oral laxative
An oral laxative formulation containing the stimulant cathartic sodium picosulfate as the primary active ingredient . Picosulfate acts on the enteric nerves in the intestinal wall to increase muscle contractions, thereby stimulating peristaltic action and promoting defecation. Other active ingredients are osmotic agents that increase stool water content.
An inorganic form of the trace element selenium with potential antineoplastic activity. Selenium, administered in the form of sodium selenite, is reduced to hydrogen selenide (H2Se) in the presence of glutathione (GSH) and subsequently generates superoxide radicals upon reaction with oxygen. This may inhibit the expression and activity of the transcription factor Sp1; in turn Sp1 down-regulates androgen receptor (AR) expression and blocks AR signaling. Eventually, selenium may induce apoptosis in prostate cancer cells and inhibit tumor cell proliferation.
(Other name for: sodium thiosulfate)
(Other name for: diclofenac sodium gel)
(Other name for: beta carotene)
(Other name for: hydrocortisone sodium succinate)
(Other name for: methylprednisolone)
(Other name for: pegvisomant)
(Other name for: theophylline)
(Other name for: theophylline)
A humanized monoclonal antibody directed against sphingosine 1-phosphate (S1P) with potential antiangiogenic and antineoplastic activities. Upon administration, sonepcizumab binds S1P, which may result in the inhibition of tumor angiogenesis. S1P is the extracellular ligand for the G protein-coupled lysophospholipid receptor EDG-1 (endothelial differentiation gene-1).