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Fruit juices inhibit organic anion transporting polypeptide–mediated drug uptake to decrease the oral availability of fexofenadine

Clinical Pharmacology & Therapeutics · 2002 · Vol. 71(1) · pp. 11–20
George K. DresserDavid G. BaileyBrenda F. LeakeUte I. SchwarzPaul A. DawsonDavid J. FreemanRichard B. Kim

Abstract

Fruit juices and constituents are more potent inhibitors of OATPs than P-glycoprotein activities, which can reduce oral drug bioavailability. Results support a new model of intestinal drug absorption and mechanism of food-drug interaction.

Drug Transport and Resistance MechanismsGastroesophageal reflux and treatmentsAntibiotics Pharmacokinetics and EfficacyGrapefruit juiceFexofenadineChemistryPharmacokineticsOrganic anion-transporting polypeptidePharmacologyOrganic anion transporter 1AspartameFood scienceCrossover study

MeSH terms

Administration, OralAdultBeveragesBiological AvailabilityCarrier ProteinsCitrusDouble-Blind MethodFemaleFlavonoidsFruitHeLa CellsHistamine H1 AntagonistsHumansIntestinal AbsorptionMale
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