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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB01268
rdf:type
n3:Drug
n3:description
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3.
n3:dosage
n32:271B6179-363D-11E5-9242-09173F13E4C5 n32:271B617A-363D-11E5-9242-09173F13E4C5 n32:271B617B-363D-11E5-9242-09173F13E4C5 n32:271B6178-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Motzer RJ, Hutson TE, Tomczak P, Michaelson MD, Bukowski RM, Rixe O, Oudard S, Negrier S, Szczylik C, Kim ST, Chen I, Bycott PW, Baum CM, Figlin RA: Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007 Jan 11;356(2):115-24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17215529 # Demetri GD, van Oosterom AT, Garrett CR, Blackstein ME, Shah MH, Verweij J, McArthur G, Judson IR, Heinrich MC, Morgan JA, Desai J, Fletcher CD, George S, Bello CL, Huang X, Baum CM, Casali PG: Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006 Oct 14;368(9544):1329-38. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17046465 # FDA label
n3:group
approved investigational
n3:halfLife
Following administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively.
n3:indication
For the treatment of advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
owl:sameAs
n29:DB01268 n30:DB01268
dcterms:title
Sunitinib
adms:identifier
n11:Sunitinib n12:PA162372840 n16:4814 n18:46507140 n19:DB01268 n20:38940 n21:4486264 n23:B49 n24:5329102 n25:D06402 n26:0069-0550-38
n3:mechanismOfAction
Sunitinib is a small molecule that inhibits multiple RTKs, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET). Sunitinib inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.
n3:packager
n17:271B6174-363D-11E5-9242-09173F13E4C5
n3:patent
n22:2395461 n22:2399358 n22:6573293 n22:7211600
n3:routeOfElimination
Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. Elimination is primarily via feces. In a human mass balance study of [14C]sunitinib, 61% of the dose was eliminated in feces, with renal elimination accounting for 16% of the administered dose.
n3:synonym
Sutent Sunitinib Sunitinibum SU-11248
n3:toxicity
The maximally tolerated dose for rat, mouse, and dog when given orally is greater than 500 mg/kg. The maximally tolerated dose of a non-human primate is greater 1200 mg/kg.
n3:volumeOfDistribution
* 2230 L (apparent volume of distribution, Vd/F)
n13:hasAHFSCode
n14:92-00-00
n3:proteinBinding
Binding of sunitinib and its primary metabolite to human plasma protein in vitro was 95% and 90%, respectively.
n3:salt
n3:synthesisReference
Ettore BIGATTI, Augusto CANAVESI, Peter Lindsay MACDONALD, Francesca Scarpitta, "PROCESSES FOR PREPARING SUNITINIB AND SALTS THEREOF." U.S. Patent US20090247767, issued October 01, 2009.
n5:hasConcept
n6:M0448793
foaf:page
n9:sunitinib.html n27:sutent.htm
n3:IUPAC-Name
n7:271B6180-363D-11E5-9242-09173F13E4C5
n3:InChI
n7:271B6186-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n7:271B6185-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n7:271B6182-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n7:271B6183-363D-11E5-9242-09173F13E4C5
n3:SMILES
n7:271B6184-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n7:271B6196-363D-11E5-9242-09173F13E4C5 n7:271B617E-363D-11E5-9242-09173F13E4C5
n3:logP
n7:271B617F-363D-11E5-9242-09173F13E4C5 n7:271B617C-363D-11E5-9242-09173F13E4C5 n7:271B6197-363D-11E5-9242-09173F13E4C5
n3:logS
n7:271B617D-363D-11E5-9242-09173F13E4C5
n3:pKa
n7:271B6198-363D-11E5-9242-09173F13E4C5
n13:hasATCCode
n15:L01XE04
n3:H-Bond-Acceptor-Count
n7:271B618C-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n7:271B618D-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n7:271B6187-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n7:271B6188-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n7:271B618A-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n7:271B6189-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n7:271B618B-363D-11E5-9242-09173F13E4C5
n3:absorption
Maximum plasma concentrations (Cmax) of sunitinib are generally observed between 6 and 12 hours (Tmax) following oral administration. Food has no effect on the bioavailability of sunitinib. Sunitinib may be taken with or without food. The pharmacokinetics were similar in healthy volunteers and in the solid tumor patient populations tested, including patients with GIST and RCC.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
557795-19-4
n3:clearance
* 34 - 62 L/h [Total oral clearance]
n3:containedIn
n4:271B6175-363D-11E5-9242-09173F13E4C5 n4:271B6176-363D-11E5-9242-09173F13E4C5 n4:271B6177-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n7:271B6192-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n7:271B6194-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n7:271B6195-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n7:271B6191-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n7:271B6190-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n7:271B6193-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n7:271B6181-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n7:271B618E-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n7:271B618F-363D-11E5-9242-09173F13E4C5