Metabolism and disposition of oral dabrafenib in cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via decarboxylation following enzymatic oxidation.

@article{Bershas2013MetabolismAD,
  title={Metabolism and disposition of oral dabrafenib in cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via decarboxylation following enzymatic oxidation.},
  author={David A. Bershas and Daniele Ouellet and Donna B. Mamaril-Fishman and Noelia Nebot and Stanley W. Carson and Samuel C. Blackman and Royce A. Morrison and Jerry Leroy Adams and Kristen E. Jurusik and Dana M. Knecht and Peter D. Gorycki and Lauren E. Richards-Peterson},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2013},
  volume={41 12},
  pages={
          2215-24
        }
}
A phase I study was conducted to assess the metabolism and excretion of [(14)C]dabrafenib (GSK2118436; N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzene sulfonamide, methanesulfonate salt), a BRAF inhibitor, in four patients with BRAF V600 mutation-positive tumors after a single oral dose of 95 mg (80 µCi). Assessments included the following: 1) plasma concentrations of dabrafenib and metabolites using validated ultra-high-performance… CONTINUE READING

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References

Publications referenced by this paper.
SHOWING 1-10 OF 10 REFERENCES

Benzene sulfonamide thiazole and oxazole compounds

JL Adams, SH Dickerson, +10 authors B. Wilson
  • U S Patent Publication
  • 2009
VIEW 3 EXCERPTS
HIGHLY INFLUENTIAL

tumours: a phase 1 dose-escalation trial

KT Flaherty, JR Infante, +24 authors J. Weber
  • 2012
VIEW 1 EXCERPT

Mice, Rats, Dogs and Humans

JC Rubinstein, M Sznol, +6 authors R. Halaban
  • Raf Kinase Inhibitor,
  • 2010
VIEW 1 EXCERPT

ezlopitant as probed with isotope effects using five deuterated analogs

C Prakash, W Wang, T O'Connell, KA. Johnson
  • Drug Metab Dispos
  • 2008
VIEW 1 EXCERPT

Mutations of the BRAF gene in human cancer

CJ Marshall, R Wooster, MR Stratton, PA. Futreal
  • 2002

Pharmacokinetics and biotransformation studies of terfenadine in man

RH Hook, BJ Walker, RA. Okerholm
  • Arzneimittelforschung 32:1185-1190. GlaxoSmithKline
  • 1982
VIEW 1 EXCERPT