In vitro characterization of sarizotan metabolism: hepatic clearance, identification and characterization of metabolites, drug-metabolizing enzyme identification, and evaluation of cytochrome p450 inhibition.

@article{Gallemann2010InVC,
  title={In vitro characterization of sarizotan metabolism: hepatic clearance, identification and characterization of metabolites, drug-metabolizing enzyme identification, and evaluation of cytochrome p450 inhibition.},
  author={Dieter Gallemann and Elmar Wimmer and Constance C. H{\"o}fer and Achim Freisleben and Markus Fluck and Bernhard J. Ladstetter and Hugues Dolgos},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2010},
  volume={38 6},
  pages={
          905-16
        }
}
In vitro biotransformation studies of sarizotan using human liver microsomes (HLM) showed aromatic and aliphatic monohydroxylation and dealkylation. Recombinant cytochromes P450 (P450) together with P450-selective inhibitors in HLM/hepatocyte cultures were used to evaluate the relative contribution of different P450s and revealed major involvement of CYP3A4, CYP2C9, CYP2C8, and CYP1A2 in sarizotan metabolism. The apparent K(m, u) and V(max) of sarizotan clearance, as investigated in HLM, were 9… CONTINUE READING

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