ROLE OF ITRACONAZOLE METABOLITES IN CYP3A4 INHIBITION

@article{Isoherranen2004ROLEOI,
  title={ROLE OF ITRACONAZOLE METABOLITES IN CYP3A4 INHIBITION},
  author={N. Isoherranen and K. Kunze and Kyle E. Allen and W. L. Nelson and K. Thummel},
  journal={Drug Metabolism and Disposition},
  year={2004},
  volume={32},
  pages={1121 - 1131}
}
Itraconazole (ITZ) is a potent inhibitor of CYP3A in vivo. However, unbound plasma concentrations of ITZ are much lower than its reported in vitro Ki, and no clinically significant interactions would be expected based on a reversible mechanism of inhibition. The purpose of this study was to evaluate the reasons for the in vitro-in vivo discrepancy. The metabolism of ITZ by CYP3A4 was studied. Three metabolites were detected: hydroxy-itraconazole (OH-ITZ), a known in vivo metabolite of ITZ, and… Expand
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