About: Dabrafenib     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Dabrafenib mesylate is a reversible ATP-competitive kinase inhibitor and targets the MAPK pathway. FDA approved on May 29, 2013. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Gibney GT, Zager JS: Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies. Expert Opin Drug Metab Toxicol. 2013 Jul;9(7):893-9. doi: 10.1517/17425255.2013.794220. Epub 2013 Apr 29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23621583 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • Dabrafenib = 8 hours; Hydroxy-dabrafenib = 10 hours; Carboxy-dabrafenib = 21-22 hours; Desmethyl-dabrafenib = 21- 22 hours. (en)
http://linked.open...ugbank/indication
  • Dabrafenib is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. (en)
sameAs
Title
  • Dabrafenib (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. (en)
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • 71% of the dose is excreted in feces. 23% of the dose is excreted in the urine as metabolites only. (en)
http://linked.open.../drugbank/synonym
  • Dabrafenib (en)
  • GSK2118436a (en)
http://linked.open...drugbank/toxicity
  • Most common adverse reactions (≥20%) for dabrafenib are hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, and palmar-plantar erythrodysesthesia syndrome. (en)
http://linked.open...umeOfDistribution
  • Apparent volume of distribution (Vd/F) = 70.3 L. Distribution to the brain is restricted because dabrafenib is a substrate and undergoes efflux by P-glycoprotein and breast cancer resistance protein. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • When taken with a fatty meal, Cmax and AUC decreased. Tmax is also prolonged compared to the fasted condition. (en)
http://linked.open...nk/proteinBinding
  • 99.7% bound to human plasma protein. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
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http://linked.open...ugbank/absorption
  • After oral administration, median time to achieve peak plasma concentration (Tmax) is 2 hours. Mean absolute bioavailability of oral dabrafenib is 95%. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...rugbank/clearance
  • The apparent clearance of dabrafenib is 17.0 L/h after single dosing and 34.4 L/h after 2 weeks of twice daily dosing. (en)
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
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http://linked.open...strongest-acidic-
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