Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data.

  title={Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data.},
  author={Haruka Nishimuta and Kimihiko Sato and Masashi Yabuki and Setsuko Komuro},
  journal={Drug metabolism and pharmacokinetics},
  volume={26 6},
This study aimed to establish a practical and simplified method of predicting intestinal availability in humans (F(g,human)) at the drug discovery stage using in vitro metabolic clearance values and permeability clearance values. A prediction model for F(g,human) of 19 CYP3A substrates and 5 UGT substrates was constructed based on the concept that the permeability clearance values mean the permeability across the basal membrane with a pH of 7.4 on both sides. Permeability clearance values were… 

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