Sequential Metabolism of AMG 487, a Novel CXCR3 Antagonist, Results in Formation of Quinone Reactive Metabolites That Covalently Modify CYP3A4 Cys239 and Cause Time-Dependent Inhibition of the Enzyme

Kirk R. Henne(Denali Therapeutics (United States)), Bradley K. Wong(United States Military Academy), Thuy Tran, Brooke M. VandenBrink, Dan A. Rock(Amgen (United States)), Andrew K. Mason, David M. Stresser(AbbVie (United States)), George Tonn, Divesh Aidasani(Amgen (United States)), Yohannes Teffera(Amgen (United States)), Xiaoqi Chen, Michael G. Johnson(University of California, Berkeley), Simon Wong, Raju Subramanian(Gilead Sciences (United States))
Drug Metabolism and Disposition
April 21, 2012
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