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Namespace Prefixes

PrefixIRI
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n15http://linked.opendata.cz/resource/drugbank/drug/DB06589/identifier/chebi/
n21http://www.rxlist.com/
n18http://linked.opendata.cz/resource/drugbank/drug/DB06589/identifier/wikipedia/
n13http://bio2rdf.org/drugbank:
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owlhttp://www.w3.org/2002/07/owl#
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n20http://linked.opendata.cz/resource/drugbank/drug/DB06589/identifier/national-drug-code-directory/
n8http://linked.opendata.cz/resource/atc/
n6http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB06589
rdf:type
n3:Drug
n3:description
Pazopanib is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is developed by GlaxoSmithKline and was FDA approved on October 19, 2009.
n3:dosage
n17:271B4CD5-363D-11E5-9242-09173F13E4C5 n17:271B4CD6-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Sonpavde G, Hutson TE, Sternberg CN: Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma. Expert Opin Investig Drugs. 2008 Feb;17(2):253-61. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18230058 # Verweij J, Sleijfer S: Pazopanib , a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23488774 # Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23548165 # Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23072642
n3:group
approved
n3:halfLife
35 hours. Oral absorption is not the rate limiting step of elimination from the plasma.
n3:indication
Treatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)
owl:sameAs
n13:DB06589
dcterms:title
Pazopanib
adms:identifier
n15:71219 n16:DB06589 n18:Pazopanib n19:D05380 n20:0173-0804-09
n3:mechanismOfAction
Pazopanib is a second-generation multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor-1, -2, and -3, platelet-derived growth factor receptor-alpha, platelet-derived growth factor receptor-beta, and c-kit. These receptor targets are part of the angiogenesis pathway that facilitates the formation of tumour blood vessel for tumour survival and growth.
n3:patent
n4:8114885 n4:7105530 n4:7262203
n3:routeOfElimination
Primarily excreted via feces (82.2%) and to a negligible extent via urine (<4%) in cancer patients. Most of the administered dose is excreted unchanged. Approximately 10% of dose are oxidative metabolites and are mostly eliminated via the feces.
n3:synonym
GW786034 GW 78603 Pazopanibum
n3:volumeOfDistribution
Vd steady state, IV administration 5 mg, cancer patient = 11.1 L (range of 9.15 - 13.4)
n6:hasAHFSCode
n7:10-00
n3:foodInteraction
Bioavailability increases with food. Take pazopanib on empty stomach. Avoid drinking grapefruit juice as it is a CYP 3A4 inhibitor and will increase exposure of pazopanib
n3:proteinBinding
>99% protein bound, independent of concentrations over a range of 10-100 μg/mL.
n3:salt
foaf:page
n11:pazopanib.html n21:votrient-drug.htm
n3:IUPAC-Name
n5:271B4CDB-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B4CE1-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B4CE0-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B4CDD-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B4CDE-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B4CDF-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4CD9-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B4CDA-363D-11E5-9242-09173F13E4C5 n5:271B4CD7-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B4CD8-363D-11E5-9242-09173F13E4C5
n6:hasATCCode
n8:L01XE11
n3:H-Bond-Acceptor-Count
n5:271B4CE7-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B4CE8-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B4CE2-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B4CE3-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B4CE5-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B4CE4-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B4CE6-363D-11E5-9242-09173F13E4C5
n3:absorption
Absorption of pazopanib in cancer patients is slow and incomplete. In patients with solid tumour, over a dose range of 50-2000 mg, absorption is nonlinear. Significant accumulation of pazopanib can also be observed in patients receiving 800 mg once daily for 22 days. Crushing tablets may increase exposure (increase in Cmax and AUC, while Tmax decreases by 2 hours). Bioavailability, oral tablet 800 mg, cancer patient = 21%; Bioavailability may be low due to incomplete absorption from the gastrointestinal tract. The major circulating component of the drug in the systemic is pazopanib, and not its metabolites. Mean maximum plasma concentration= 58.1 µg/mL; Mean AUC= 1037 µg · h/mL;
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
444731-52-6
n3:clearance
CL, cancer patient, IV administration 5 mg = 4mL/min Half of the absorbed dose is cleared via oxidative metabolism.
n3:Bioavailability
n5:271B4CED-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B4CEF-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B4CF0-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B4CEC-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B4CEB-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B4CEE-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B4CDC-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B4CE9-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B4CEA-363D-11E5-9242-09173F13E4C5