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A recent study investigating the pharmacokinetics of fentanyl in Sprague–Dawley rats suggested fentanyl to be a substrate of rat organic anion‐transporting polypeptide Oatp. In human beings, the most important OATP for the pharmacokinetics of many drugs is OATP1B1. Therefore, genetic variants of OATP1B1 (SLCO1B1) might modulate fentanyl pharmacokinetics and efficacy in human beings. Sixteen healthy...