Fitch William L, Tran Thuy, Young May, Liu Liling, Chen Yuan
Department of Drug Metabolism and Pharmacokinetics, Roche Palo Alto, Palo Alto, CA 94304, USA.
Drug Metab Lett. 2009 Aug;3(3):191-8. doi: 10.2174/187231209789352085.
The microsomal metabolism of ketoconazole is revisited using accurate mass LC/MS(n) and deuterium labelling. Structures for sixteen metabolites are proposed from rat and human microsomal metabolism of commercial ketoconazole. Thirteen of the proposed structures are well determined and consistent with all data; five of the proposed structures are less certain. Ten of the metabolites are described for the first time. Reaction phenotyping shows that most of the metabolites arise from CYP3A4, the enzyme known to be well inhibited by ketoconazole.
