The purpose of the present study is to examine the long‐lasting inhibition of intestinal organic anion transporting polypeptides (Oatps) by cyclosporin A (CsA) in rats using fexofenadine (FEX) as a probe drug. We examined the pharmacokinetics of FEX after its intravenous or oral administration to rats at 3 or 24 h after the oral administration of CsA. When FEX was administered at 3 h after the administration of CsA, its plasma concentration increased regardless of whether it was administered intravenously or orally. When FEX was intravenously administered at 24 h after the oral administration of CsA, its plasma concentration was increased; however, that observed after its oral administration was not significantly different from the vehicle‐treated control. When FEX was administered at 3 h after the administration of CsA, the hepatic availability (Fh) and the fraction absorbed in the intestine as an unchanged form (Fa·Fg) of FEX were increased, resulting in increased bioavailability (=Fa·Fg·Fh). At 24 h after the administration of CsA, the Fh of FEX was increased, whereas its bioavailability was decreased, suggesting that its Fa·Fg was decreased because of the long‐lasting inhibition. In conclusion, CsA has long‐lasting inhibitory effects on Oatps in the rat intestine as well as in the liver. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:2606–2615, 2012

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