Oxidative metabolism of clarithromycin in the presence of human liver microsomes. Major role for the cytochrome P4503A (CYP3A) subfamily.

@article{Rodrigues1997OxidativeMO,
  title={Oxidative metabolism of clarithromycin in the presence of human liver microsomes. Major role for the cytochrome P4503A (CYP3A) subfamily.},
  author={A. David Rodrigues and Ellen M Roberts and Darcy J Mulford and Yao Yao and Daniele Ouellet},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={1997},
  volume={25 5},
  pages={623-30}
}
In vitro studies were conducted to identify the hepatic cytochrome P450 (CYP) protein(s) involved in the oxidative metabolism of [14C]clarithromycin (CLAR) in the presence of native human liver microsomes. The identity of the two major CLAR metabolites present in microsome incubates, 14-(R)-hydroxy-CLAR and N-desmethyl-CLAR, was confirmed by MS. Over the CLAR concentration range of 1.0-140 microM, the rate of CLAR 14-(R)-hydroxylation (KM = 48 +/- 17.7 microM; Vmax = 206 +/- 76 pmol/min/mg… CONTINUE READING

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