In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug–Drug Interactions

@inproceedings{Karlgren2011InVA,
  title={In Vitro and In Silico Strategies to Identify OATP1B1 Inhibitors and Predict Clinical Drug–Drug Interactions},
  author={Maria Karlgren and Gustav Ahlin and Christel A. S. Bergstr{\"o}m and Richard M Svensson and Johan Palm and Per Artursson},
  booktitle={Pharmaceutical Research},
  year={2011}
}
To establish in vitro and in silico models that predict clinical drug–drug interactions (DDIs) with the OATP1B1 (SLCO1B1) transporter. The inhibitory effect of 146 drugs and drug-like compounds on OATP1B1-mediated transport was studied in HEK293 cells. A computational model was developed to predict OATP1B1 inhibition. Concentration-dependent effects were investigated for six compounds; clinical DDIs were predicted by calculating change in exposure (i.e. R-values) in eight different ways. Sixty… CONTINUE READING
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