Identification of enzymes responsible for rifalazil metabolism in human liver microsomes |
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| Authors: | T. Mae T. Inaba E. Konishi K. Hosoe |
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| Affiliation: | 1. Takasago Research Laboratories, Kaneka Corporation, 1-8, Miyamae-machi, Takasago-cho, Takasago-shi, Hyogo, 676-8688, Japan;2. Department of Pharmacology, Faculty of Medicine, University of Toronto, Toronto M5S1A8, Canada |
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| Abstract: | ![]()
1. The major metabolites of rifalazil in human are 25-deacetyl-rifalazil and 32- hydroxy-rifalazil. Biotransformation to these metabolites in pooled human liver microsomes, cytosol and supernatant 9000g (S9) fractions was studied, and the enzymes responsible for rifalazil metabolism were identified using inhibitors of esterases and cytochromes P450 (CYP). 2. The 25-deacetylation and 32-hydroxylation of rifalazil occurred in incubations with microsomes or S9 but not with cytosol, indicating that both the enzymes responsible for rifalazil metabolism were microsomal. Km and Vmax |
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