The intestine as an important contributor to prasugrel active metabolite formation in vivo.

@article{Hagihara2011TheIA,
  title={The intestine as an important contributor to prasugrel active metabolite formation in vivo.},
  author={Katsunobu Hagihara and M. Kazui and Hidenori Ikenaga and Toshihiko Nanba and Kiichi Fusegawa and Takashi Izumi and Toshihiko Ikeda and Atsushi Kurihara},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2011},
  volume={39 4},
  pages={565-70}
}
Prasugrel [2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine], a thienopyridine antiplatelet agent, undergoes rapid hydrolysis in vivo to a thiolactone intermediate, 2-[2-oxo-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)ethanone (R-95913), which is further converted to a pharmacologically active metabolite, 2-[1-2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4-mercapto-3-piperidinylidene acetic acid (R-138727), by oxidation via… CONTINUE READING