Intestinal OATP1A2 inhibition as a potential mechanism for the effect of grapefruit juice on aliskiren pharmacokinetics in healthy subjects

@article{Rebello2011IntestinalOI,
  title={Intestinal OATP1A2 inhibition as a potential mechanism for the effect of grapefruit juice on aliskiren pharmacokinetics in healthy subjects},
  author={Sam Rebello and Sally Zhao and Sam Hariry and Marion Dahlke and Natalya Alexander and Arpine Vapurcuyan and Imad Hanna and Venkateswar Jarugula},
  journal={European Journal of Clinical Pharmacology},
  year={2011},
  volume={68},
  pages={697-708}
}
To conduct a mechanistic investigation of the interaction between aliskiren and grapefruit juice in healthy subjects. Twenty-eight subjects received an oral dose of aliskiren 300 mg (highest recommended clinical dose) with 300 mL of either water or grapefruit juice in a two-way crossover design. Safety and pharmacokinetic analyses were performed. In vitro studies were performed in HEK293 cells to investigate the role of organic anion transporting polypeptide (OATP) transporter-mediated uptake… CONTINUE READING
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