A possible mechanism for the differences in efficiency and variability of active metabolite formation from thienopyridine antiplatelet agents, prasugrel and clopidogrel.

@article{Hagihara2009APM,
  title={A possible mechanism for the differences in efficiency and variability of active metabolite formation from thienopyridine antiplatelet agents, prasugrel and clopidogrel.},
  author={Katsunobu Hagihara and M. Kazui and Atsushi Kurihara and Michiharu Yoshiike and Kokichi Honda and Osamu Tatsuma Okazaki and Nagy A. Farid and Toshihiko Ikeda},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2009},
  volume={37 11},
  pages={
          2145-52
        }
}
The efficiency and interindividual variability in bioactivation of prasugrel and clopidogrel were quantitatively compared and the mechanisms involved were elucidated using 20 individual human liver microsomes. Prasugrel and clopidogrel are converted to their thiol-containing active metabolites through corresponding thiolactone metabolites. The formation rate of clopidogrel active metabolite was much lower and more variable [0.164 + or - 0.196 microl/min/mg protein, coefficient of variation (CV… CONTINUE READING
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In vitro metabolism of antiplatelet agent clopidogrel: cytochrome P450 isoforms responsible for two oxidation steps involved in the active metabolite formation

  • A Kurihara, K Hagihara, M Kazui, T Ozeki, NA Farid, T Ikeda
  • Drug Metab Rev 37:99
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13 Excerpts

Prasugrel (CS-747, LY640315), a novel thienopyridine antiplatelet agent, more efficiently generates active metabolite compared to clopidogrel

  • M Kazui, A Kurihara, K Hagihara, NA Farid, T Ikeda
  • Drug Metab Rev 37:98
  • 2005
Highly Influential
4 Excerpts