The metabolic drug-drug interaction profile of Dabrafenib: in vitro investigations and quantitative extrapolation of the P450-mediated DDI risk.

@article{Lawrence2014TheMD,
  title={The metabolic drug-drug interaction profile of Dabrafenib: in vitro investigations and quantitative extrapolation of the P450-mediated DDI risk.},
  author={Sarah K Lawrence and Dung Tien Nguyen and Chet Bowen and Lauren Richards-Peterson and Konstantine W. Skordos},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2014},
  volume={42 7},
  pages={1180-90}
}
Dabrafenib is a potent ATP-competitive inhibitor for the V600 mutant b-rapidly accelerated fibrosarcoma (b-raf) kinase currently approved in the United States for the treatment of metastatic melanoma. Studies were conducted in human liver microsomes, recombinant human cytochrome P450 (P450) enzymes, and human hepatocytes to investigate the potential of dabrafenib and its major circulating metabolites to perpetrate pharmacokinetic drug-drug interactions (DDIs) as well as have their own… CONTINUE READING

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A study of the effects of inhibition of CYP3A4 by ketoconazole (K) and CYP2C8 by gemfibrozil (G) on the pharmacokinetics of dabrafenib (D)

  • B Suttle, K Grossman, +7 authors K Kendra
  • Clin Pharmacol Ther
  • 2014
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