Drug Metabolism Letters

Zhiyang Zhao
Amgen
Cambridge, MA
USA

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Revisiting the Metabolism of Ketoconazole Using Accurate Mass

Author(s): William L. Fitch, Thuy Tran, May Young, Liling Liu, Yuan Chen.

Abstract:

The microsomal metabolism of ketoconazole is revisited using accurate mass LC/MSn 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.

Keywords: Ketoconazole, metabolism, mass spectrometry, deuterium labeling

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Article Details

VOLUME: 3
ISSUE: 3
Year: 2009
Page: [191 - 198]
Pages: 8
DOI: 10.2174/187231209789352085
Price: $58