Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: human UDP-glucuronosyltransferase enzymes involved in lactonization.

@article{Fujino2003MetabolicFO,
  title={Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: human UDP-glucuronosyltransferase enzymes involved in lactonization.},
  author={Hideki Fujino and Iwao Yamada and Syunsuke Shimada and Masaru Yoneda and Junji Kojima},
  journal={Xenobiotica; the fate of foreign compounds in biological systems},
  year={2003},
  volume={33 1},
  pages={27-41}
}
1. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes. Pitavastatin lactone, which can be converted back to the unchanged form, is the major metabolite of pitavastatin in humans. To clarify the mechanism of the lactonization of pitavastatin and the metabolic properties of the lactone, we performed experiments in vitro. 2. On addition of UDP-glucuronic acid, human hepatic microsomes produced pitavastatin lactone and an unknown metabolite… CONTINUE READING

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