| Attributes | Values |
|---|
| rdf:type
| |
| http://linked.open...gbank/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. (en)
|
| http://linked.open...y/drugbank/dosage
| |
| http://linked.open...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 (en)
|
| http://linked.open...gy/drugbank/group
| |
| http://linked.open...drugbank/halfLife
| - Elimination half-life = 57 hours (range of 30-120 hours) (en)
|
| http://linked.open...ugbank/indication
| - Treatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation. (en)
|
| sameAs
| |
| Title
| |
| adms:identifier
| |
| http://linked.open...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. (en)
|
| http://linked.open...y/drugbank/patent
| |
| http://linked.open...outeOfElimination
| - Excreted via feces (94%) and urine (1%). (en)
|
| http://linked.open.../drugbank/synonym
| - PLX4032 (en)
- BRAF(V600E) Kinase Inhibitor RO5185426 (en)
- Zelboraf (en)
|
| http://linked.open...umeOfDistribution
| |
| http://linked.open.../drug/hasAHFSCode
| |
| http://linked.open...nk/proteinBinding
| - >99% protein bound to serum albumin and alpha-1 acid glycoprotein. (en)
|
| foaf:page
| |
| http://linked.open...ugbank/IUPAC-Name
| |
| http://linked.open...gy/drugbank/InChI
| |
| http://linked.open...Molecular-Formula
| |
| http://linked.open.../Molecular-Weight
| |
| http://linked.open...noisotopic-Weight
| |
| http://linked.open...y/drugbank/SMILES
| |
| http://linked.open.../Water-Solubility
| |
| http://linked.open...ogy/drugbank/logP
| |
| http://linked.open...ogy/drugbank/logS
| |
| http://linked.open...l/drug/hasATCCode
| |
| http://linked.open...nd-Acceptor-Count
| |
| http://linked.open...-Bond-Donor-Count
| |
| http://linked.open...drugbank/InChIKey
| |
| http://linked.open...urface-Area--PSA-
| |
| http://linked.open...nk/Polarizability
| |
| http://linked.open...bank/Refractivity
| |
| http://linked.open...atable-Bond-Count
| |
| http://linked.open...ugbank/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 (en)
|
| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
|
| http://linked.open...casRegistryNumber
| |
| http://linked.open...rugbank/clearance
| - Total body clearance = 31 L/day (en)
|
| http://linked.open...k/Bioavailability
| |
| http://linked.open...bank/Ghose-Filter
| |
| http://linked.open...nk/MDDR-Like-Rule
| |
| http://linked.open...ank/Melting-Point
| |
| http://linked.open...k/Number-of-Rings
| |
| http://linked.open...siological-Charge
| |
| http://linked.open...bank/Rule-of-Five
| |
| http://linked.open...tional-IUPAC-Name
| |
| http://linked.open...strongest-acidic-
| |
| http://linked.open...-strongest-basic-
| |
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