Predicting P-Glycoprotein Effects on Oral Absorption: Correlation of Transport in Caco-2 with Drug Pharmacokinetics in Wild-Type and mdr1a(-/-) Mice in Vivo

@article{Collett2004PredictingPE,
  title={Predicting P-Glycoprotein Effects on Oral Absorption: Correlation of Transport in Caco-2 with Drug Pharmacokinetics in Wild-Type and mdr1a(-/-) Mice in Vivo},
  author={Andrew Collett and Jolanta Tanianis-Hughes and David Hallifax and Geoff Warhurst},
  journal={Pharmaceutical Research},
  year={2004},
  volume={21},
  pages={819-826}
}
Purpose. Cell-based permeability screens are widely used to identify drug-P-glycoprotein (PGP) interaction in vitro. However, their reliability in predicting the impact of PGP on human drug pharmacokinetics is poorly defined. The aim was to determine whether a quantitative relationship exists between PGP-mediated alterations in Caco-2 permeability and oral pharmacokinetics in mice. Methods. Two indicators of drug efflux were measured in Caco-2 for a group of 10 compounds, the ratio of A-B and B… CONTINUE READING

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