A quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature. This agent also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells.
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.
A methylated derivative of carmustine with antineoplastic activity. As an alkylating agent, semustine forms covalent linkages with nucleophilic centers in DNA, causing depurination, base-pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity.
Seneca Valley virus-001
A native, replication-competent oncolytic picornavirus with potential antineoplastic activity. Administered systemically, Seneca Valley virus-001 (SVV-001) specifically targets and infects tumor cells with neuroendocrine characteristics. Upon infection, this agent replicates intracellularly, resulting in tumor cell lysis and reduced tumor cell proliferation. The selective tropism of virus replication may involve receptor-mediated internalization.
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: D-cycloserine)
(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.
silicon phthalocyanine 4
A synthetic photosensitizer agent containing a large macrocyclic ring chelated with silicon. Silicon phthalocyanine 4 localizes primarily in mitochondrial cytosolic membranes and, after photoexcitation, forms reactive oxygen species that induce apoptosis.
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)
A mixture of flavonolignans isolated from the milk thistle plant Silybum marianum. Silymarin may act as an antioxidant, protecting hepatic cells from chemotherapy-related free radical damage. This agent may also promote the growth of new hepatic cells.
(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)
(Other name for: montelukast sodium)
A monoclonal immunoglobulin G1 antibody with potential antineoplastic activity. Siplizumab binds to CD2, a specific receptor found in T cells and NK cells, thereby triggering a host immune response that results in lysis of CD2+ cells, selective suppression of the immune system, and control of activated T cell growth.
A cell-based vaccine composed of autologous antigen-presenting peripheral blood mononuclear cells (enriched for a dendritic cell fraction) that have been exposed to a recombinant protein consisting of granulocyte-macrophage colony-stimulating factor (GM-CSF) fused to prostatic-acid phosphatase (PAP), a protein expressed by prostate cancer cells. Upon administration, the vaccine may stimulate an antitumor T-cell response against tumor cells expressing PAP.
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.
A natural macrocyclic lactone produced by the bacterium Streptomyces hygroscopicus, with immunosuppressant properties. In cells, sirolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This results in inhibition of T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation and inhibition of antibody production.
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).
A pyrrolobenzodiazepine dimer with potential antineoplastic activity. SJG-136 binds to the minor groove of DNA and induces interstrand cross-links between two N-2 guanine positions, thereby inhibiting DNA replication and transcription. With a preference for binding to purine-GATC-pyrimidine sequences, SJG-136 adducts do not appear to be subject to p53-mediated DNA excision repair mechanisms.
(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.
A dolastatin-10 derivative. Soblidotin inhibits tubulin polymerization, resulting in cell cycle arrest and induction of apoptosis.
SOD1 inhibitor ATN-224
An orally bioavailable, second-generation tetrathiomolybdate analog with potnetial antiangiogenic and antineoplastic activities. SOD1 inhibitor ATN-224 selectively chelates the copper ion in copper-zinc superoxide dismutase 1 (SOD1), inhibiting SOD1 activity; this may result in a decrease in intra-cellular H2O2 levels and, in turn, increased activity of intracellular phosphatases. The ATN-224-mediated increase in phosphatase activity may interfere with the activation of multiple kinase signaling pathways required for cellular proliferation and angiogenesis. This agent has been shown to inhibit VEGF and FGF-2 signaling in endothelial cells,
IGF-1, EGF, NF-kB, and integrin signaling in tumor cells,
and PDGF signaling in pericytes.
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.
A boron-carrying compound. After parenteral administration, borocaptate sodium accumulates preferentially in tumor cells. When exposed to neutron irradiation, borocaptate absorbs neutrons and self-destructs releasing short-range alpha radiation and 'recoil' lithium in tumor cells, resulting in alpha radiation-induced tumor cell death. This highly selective, localized radiotargeting of tumor cells, known as boron neutron capture therapy (BNCT), spares adjacent normal tissues.
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.
The sodium salt of salicylic acid. As a nonsteroidal anti-inflammatory drug (NSAID), sodium salicylate irreversibly acetylates cyclooxygenases I and II, thereby inhibiting prostaglandin synthesis and associated inflammation and pain. This agent may also activate mitogen-activated protein kinase (p38MAPK), thereby inducing apoptosis in cancer cells.
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.
Pentavalent antimony (Sb) in differential complex formation with gluconic acid with leishmanicidal and potential antineoplastic activities. The Sb moiety of sodium stibogluconate (SSG) may inhibit protein tyrosine phophorylases (PTPases) by covalently modifying sulfhydryl groups in PTPase cysteine residues, resulting in specific inactivation of SH2 domain-containing tyrosine phosphatases-1 and -2 (SHP-1 and SHP-2), PTPases which negatively regulate interferon (IFN) signaling; enhancement of IFN-induced Stat1 tyrosine phosphorylation; and induction of cellular protein tyrosine phosphorylation. SSG in combination with IFN-alpha may synergize to overcome tumor cell resistance to IFN-alpha-mediated apoptosis.
A water soluble salt and reducing agent that reacts with oxidizing agents. Although its exact mechanism of action is unknown, thiosulfate likely provides an exogenous source of sulfur, thereby hastening the detoxification of cyanide through the enzyme rhodanese (thiosulfate cyanide sulfurtransferase) which converts cyanide to the relatively nontoxic, excretable thiocyanate ion. In addition, this agent neutralizes the reactive alkylating species of nitrogen mustard, thereby decreasing skin toxicity related to nitrogen mustard extravasation.
(Other name for: sodium thiosulfate)
(Other name for: diclofenac sodium gel)
(Other name for: beta carotene)
(Other name for: eculizumab)
(Other name for: hydrocortisone sodium succinate)
(Other name for: methylprednisolone)
A recombinant form of endogenous human growth hormone (GH), a polypeptide produced by the anterior lobe of the human pituitary gland. GH exhibits growth-promoting effects and metabolic effects on carbohydrate, fat, protein and bone metabolism. GH stimulates protein synthesis and the uptake of amino acids into cells, and induces lipolysis in adipose tissues. The secretion of GH increases with sexual maturation and then declines steadily.
(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).
The tosylate salt of sorafenib, a synthetic compound targeting growth signaling and angiogenesis. Sorafenib blocks the enzyme RAF kinase, a critical component of the RAF/MEK/ERK signaling pathway that controls cell division and proliferation; in addition, sorafenib inhibits the VEGFR-2/PDGFR-beta signaling cascade, thereby blocking tumor angiogenesis.
(Other name for: acitretin)
(Other name for: isotretinoin)
A dietary supplement isolated from soybeans containing phytoestrogen isoflavones. Although the mechanism of action is unclear, soy isoflavones mimic estrogen action mediated through estrogen receptors. In addition, this agent also modulates estrogen metabolism. As a result, soy isoflavones have been shown to reduce tumor cell proliferation and induce tumor cell apoptosis, as well as to be able to regulate hormone balance and reduce the risks of breast cancer, heart disease, and osteoporosis.
soy protein isolate
A dietary protein isolated from soybeans that contains isoflavone phytoestrogens. Soy protein isolate has been shown to reduce tumor incidence and growth in some animal studies, possibly by modulating estrogen metabolism, reducing tumor cell proliferation, and inducing tumor cell apoptosis. Soy protein isolate may also inhibit endothelial cell proliferation. Isoflavone phytoestrogens display mild estrogen-like activities which may regulate hormone balance and reduce the risks of breast cancer, heart disease, and osteoporosis.
A stable transition state analogue for an aspartate transcarbamylase- cartalyzed reaction with antineoplastic activity. Sparfosic acid is a stable transition analogue of the activated complex for the reaction catalyzed by aspartate transcarbamylase, the first step in the pyrimidine biosynthetic pathway. This agent inhibits de novo pyrimidine biosynthesis and increases the extent to which fluorouracil metabolites are incorporated into RNA.
(Other name for: tiotropium bromide monohydrate)
A synthetic organometallic compound containing the element germanium with possible antineoplastic activity. Spirogermanium exhibits significant toxicity, particularly neurotoxicity.
A bifunctional nitrogen alkylating agent with antineoplastic activity and lipophilic properties. Containing a lipophilic hydantoin group that serves as a carrier to cross the blood brain barrier, spiromustine forms covalent linkages with nucleophilic centers in DNA, causing depurination, base-pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity.
A synthetic 17-spironolactone corticosteroid with potassium-sparing diuretic, antihypertensive, and antiandrogen activities. Spironolactone competitively inhibits adrenocortical hormone aldosterone activity in the distal renal tubules, myocardium, and vasculature. This agent may inhibit the pathophysiologic effects of aldosterone produced in excess by various types of malignant and benign tumors.
A synthetic derivative of cyclohexane sulfatoplatinum with antineoplastic properties. Spiroplatin induces DNA cross-links, thereby inhibiting DNA replication and RNA and protein synthesis. Similar to other platinum compounds, this agent has been shown to be mutagenic and carcinogenic.
(Other name for: itraconazole)
(Other name for: dasatinib)
(Other name for: trientine hydrochloride)
A synthetic peripheral sigma receptor ligand with immunomodulatory and potential antitumor activities. Although the exact mechanism by which SR31747A exerts its antitumor effects has not been fully established, SR31747A binds to and inhibits the sigma1 receptor (SR31747A-binding protein-1 or SR-BP1), human sterol isomerase (emopamil-binding protein) and the sigma2 receptor, which may result in a reduction in tumor cell proliferation and tumor cell apoptosis. In addition, this agent inhibits the production of pro-inflammatory cytokines while increasing anti-inflammatory cytokines. Upregulated in various cancers, the sigma1 and sigma2 receptors and human sterol isomerase are proteins that are involved in the regulation of cell proliferation and survival.
Src kinase inhibitor KX2-391
An orally bioavailable small molecule Src kinase inhibitor with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase; inhibition of kinase activity may result in the inhibition of primary tumor growth and the suppression of metastasis. Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis.