Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [C]Cobimetinib, a MEK Inhibitor, in Humans
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چکیده
328 words Introduction: 420 words Discussion: 1403 words Abbreviations: AUC, area under the curve; CL, clearance, Cmax, maximum concentration; F, bioavailability; Fa, fraction absorbed; Fg, fraction escaping gut wall elimination; Fh, fraction escaping hepatic elimination; HLM, human liver microsomes; PK, pharmacokinetics, SD, standard deviation; tmax, time to reach Cmax. This article has not been copyedited and formatted. The final version may differ from this version. DMD Fast Forward. Published on October 8, 2015 as DOI: 10.1124/dmd.115.066282 at A PE T Jornals on Sptem er 1, 2017 dm d.aspurnals.org D ow nladed from
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Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans.
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The pharmacokinetics, metabolism, and excretion of cobimetinib, a MEK inhibitor, were characterized in healthy male subjects (n = 6) following a single 20 mg (200 mCi) oral dose. Unchanged cobimetinib and M16 (glycine conjugate of hydrolyzed cobimetinib) were the major circulating species, accounting for 20.5% and 18.3% of the drug-related material in plasma up to 48 hours postdose, respectivel...
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