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The cytochrome P-450 metabolite complex derived from troleandomycin: Properties in vitro and stability in vivo

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Cited by (29)

  • Drug Metabolism: Cytochrome P450

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  • Roles of cytochrome P450 enzymes in pharmacology and toxicology: Past, present, and future

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    A relevant example is troleandomycin (Pessayre et al., 1983). The rates of breakdown of the complex is slow and takes more than a day in vivo (Delaforge, Jaouen, & Mansuy, 1984). Generation of reactive metabolites that bind to P450 covalently to inhibit.

  • In vitro hepatic conversion of the anticancer agent nemorubicin to its active metabolite PNU-159682 in mice, rats and dogs: A comparison with human liver microsomes

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    By contrast, no statistically significant correlations (P > 0.05) were found between PNU-159682 formation rate and dextromethorphan-O-demethylase activity (Figs. 4–6). In order to confirm the above results, we examined the effects of the CYP3A inhibitors ketoconazole [15–17] and TAO [18–20] on the rate of PNU-159682 formation by microsomes obtained from males of the various animal species. For the purpose of comparison, the same experiments were also performed using pooled, mixed-gender HLMs.

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