Substrate- and Dose-Dependent Drug Interactions with Grapefruit Juice Caused by Multiple Binding Sites on OATP2B1

@article{Shirasaka2014SubstrateAD,
  title={Substrate- and Dose-Dependent Drug Interactions with Grapefruit Juice Caused by Multiple Binding Sites on OATP2B1},
  author={Y. Shirasaka and Takanori Mori and Y. Murata and T. Nakanishi and I. Tamai},
  journal={Pharmaceutical Research},
  year={2014},
  volume={31},
  pages={2035-2043}
}
ABSTRACTPurposeOATP2B1-mediated grapefruit juice (GFJ)-drug interactions are substrate-dependent; for example, GFJ ingestion significantly reduces bioavailability of fexofenadine, but not pravastatin. In the present study, we aimed to establish whether this observation can be explained by the presence of multiple binding sites (MBS) on OATP2B1.MethodsOATP2B1-mediated drug uptake was evaluated using a Xenopus oocyte expression system. Drug concentration was quantified by LC/MS/MS analysis… Expand
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