Revisiting the Metabolism of Ketoconazole Using Accurate Mass

Title: Revisiting the Metabolism of Ketoconazole Using Accurate Mass

Volume: 3 Issue: 3

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

Affiliation:

Keywords: Ketoconazole, metabolism, mass spectrometry, deuterium labeling

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.

Cite this article as:

Fitch L. William, Tran Thuy, Young May, Liu Liling and Chen Yuan, Revisiting the Metabolism of Ketoconazole Using Accurate Mass, Drug Metabolism Letters 2009; 3 (3) . https://dx.doi.org/10.2174/187231209789352085