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Namespace Prefixes

PrefixIRI
n2http://linked.opendata.cz/resource/drugbank/drug/
dctermshttp://purl.org/dc/terms/
n17http://linked.opendata.cz/resource/AHFS/
foafhttp://xmlns.com/foaf/0.1/
n6http://linked.opendata.cz/resource/drugbank/drug/DB08881/identifier/chebi/
n20http://linked.opendata.cz/resource/drugbank/dosage/
n7http://linked.opendata.cz/resource/drugbank/drug/DB08881/identifier/wikipedia/
n15http://www.rxlist.com/
n9http://linked.opendata.cz/resource/drugbank/drug/DB08881/identifier/pharmgkb/
n11http://bio2rdf.org/drugbank:
admshttp://www.w3.org/ns/adms#
n18http://www.drugs.com/mtm/
n16http://linked.opendata.cz/resource/drugbank/patent/
rdfhttp://www.w3.org/1999/02/22-rdf-syntax-ns#
n22http://linked.opendata.cz/resource/drugbank/drug/DB08881/identifier/kegg-drug/
owlhttp://www.w3.org/2002/07/owl#
n21http://linked.opendata.cz/resource/drugbank/drug/DB08881/identifier/drugbank/
n3http://linked.opendata.cz/ontology/drugbank/
n4http://linked.opendata.cz/resource/drugbank/property/
n8http://linked.opendata.cz/resource/drugbank/drug/DB08881/identifier/national-drug-code-directory/
xsdhhttp://www.w3.org/2001/XMLSchema#
n13http://linked.opendata.cz/resource/atc/
n12http://linked.opendata.cz/ontology/sukl/drug/

Statements

Subject Item
n2:DB08881
rdf:type
n3:Drug
n3:description
Vemurafenib is a BRAF enzyme inhibitor developed by Plexxikon and Genentech for the treatment of late-stage melanoma. [Wikipedia] The cobas® 4800 BRAF B600 mutation test provided by Roche Molecular Systems is the diagnostic test to confirm eligibility for treatment. FDA approved on August 17, 2011 under the company Hoffmann La Roche.
n3:dosage
n20:271B5A4A-363D-11E5-9242-09173F13E4C5 n20:271B5A4B-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23094782
n3:group
approved
n3:halfLife
Elimination half-life = 57 hours (range of 30-120 hours)
n3:indication
Treatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
owl:sameAs
n11:DB08881
dcterms:title
Vemurafenib
adms:identifier
n6:63637 n7:Vemurafenib n8:50242-090-01 n9:PA165946873 n21:DB08881 n22:D09996
n3:mechanismOfAction
Vemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. It is especially potent against the BRAF V600E mutation. This mutation involves the substitution of glutamic acid for valine at codon 600. The BRAF oncogene, most of which have the V600E mutation, activates mitogen-activated kinase (MAPK) pathway which results in cell growth, proliferation, and metastasis. Vemurafenib blocks these downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.
n3:patent
n16:7504509 n16:8143271 n16:7863288
n3:routeOfElimination
Excreted via feces (94%) and urine (1%).
n3:synonym
BRAF(V600E) Kinase Inhibitor RO5185426 PLX4032 Zelboraf
n3:volumeOfDistribution
106 L
n12:hasAHFSCode
n17:10-00
n3:proteinBinding
>99% protein bound to serum albumin and alpha-1 acid glycoprotein.
foaf:page
n15:zelboraf-drug.htm n18:vemurafenib.html
n3:IUPAC-Name
n4:271B5A50-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B5A56-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B5A55-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B5A52-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B5A53-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B5A54-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B5A4E-363D-11E5-9242-09173F13E4C5 n4:271B5A66-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B5A4C-363D-11E5-9242-09173F13E4C5 n4:271B5A4F-363D-11E5-9242-09173F13E4C5 n4:271B5A68-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B5A4D-363D-11E5-9242-09173F13E4C5
n12:hasATCCode
n13:L01XE15
n3:H-Bond-Acceptor-Count
n4:271B5A5C-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B5A5D-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B5A57-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B5A58-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B5A5A-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B5A59-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B5A5B-363D-11E5-9242-09173F13E4C5
n3:absorption
After oral administration of vemurafenib, it is well absorbed. Bioavailability is unknown. Peak concentrations are reached in 3 hours when an oral dose of 960 mg twice daily for 15 days has been given to patients. Exposure is highly variable between different patients. Gastrointestinal fluid content, pH, volumes, motility, transition time and bile composition may be factors affecting exposure. It is unknown how food affects the absorption of vemurafenib. Time to steady state = 15 - 22 days
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
918504-65-1
n3:clearance
Total body clearance = 31 L/day
n3:Bioavailability
n4:271B5A62-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B5A64-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B5A65-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B5A67-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B5A61-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B5A60-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B5A63-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B5A51-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B5A5E-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B5A5F-363D-11E5-9242-09173F13E4C5