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Price of Dabrafenib
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Dabrafenib volume of distribution
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.
What is Dabrafenib
Dabrafenib mesylate is a reversible ATP-competitive kinase inhibitor and targets the MAPK pathway. FDA approved on May 29, 2013.
Dabrafenib mechanism of action
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.
Dosage forms of Dabrafenib
Novartis Pharmaceuticals Corporation
Humans and other mammals
Indication of Dabrafenib
Dabrafenib is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test.
Toxicity of Dabrafenib
Most common adverse reactions ( 20%) for dabrafenib are hyperkeratosis, headache, pyrexia, arthralgia, papilloma, alopecia, and palmar-plantar erythrodysesthesia syndrome.
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