The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein-quantitative analysis based on information from the literature.

@article{Kato2003TheIF,
  title={The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein-quantitative analysis based on information from the literature.},
  author={Motohiro Kato and Koji Chiba and Akihiro Hisaka and Michi Ishigami and Makoto Kayama and Naomi Mizuno and Yoshinori Nagata and Susumu Takakuwa and Yuko Tsukamoto and Kaoru Ueda and Hiroyuki Kusuhara and Kiyomi Ito and Yuichi Sugiyama},
  journal={Drug metabolism and pharmacokinetics},
  year={2003},
  volume={18 6},
  pages={365-72}
}
It is suggested that the bioavailability of CYP3A4 substrates might be low due to first-pass metabolism in the small intestine, and it is possible that P-glycoprotein (P-gp) may influence first-pass metabolism in a co-operative manner. We have collected information of the pharmacokinetics of CYP3A4 substrates to evaluate the fraction absorbed (Fa), intestinal availability (Fg) and hepatic availability (Fh) and have investigated the intestinal first-pass metabolism and the effect of P-gp on this… CONTINUE READING

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