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

By G. Dresser, D. Bailey, B. Leake, U. Schwarz, P. Dawson, D. Freeman, R. Kim. Clinical pharmacology and therapy, 2002

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Xenobiotic, Bile Acid, and Cholesterol Transporters: Function and Regulation (2010, background): “The grapefruit flavonoid naringin inhibits OATP1A2 uptake of fexofenadine in vitro, and thus grapefruit juice alters clinical fexofenadine pharmacokinetics (Dresser et al., 2002; Bailey et al., 2007; Glaeser et al., 2007).”
Impact of OATP transporters on pharmacokinetics (2009, background): “…in studies in healthy subjects, the AUC of fexofenadine has been decreased by 25% by ingestion of naringin, and by 40–70% due to ingestion of grapefruit or orange juice (Dresser et al., 2002, 2005; Bailey et al., 2007), consistent with inhibition of OATP1A2 at the apical membrane of enterocytes.”
OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies (2012, background): “Fruit juices decrease the oral bioavailability of fexofenadine in humans (Dresser et al., 2002; 2005; Glaeser et al., 2007).”
Predicting Drug Disposition via Application of BCS: Transport/Absorption/ Elimination Interplay and Development of a Biopharmaceutics Drug Disposition Classification System (2004, background): “Recent evidence suggests that intestinal drug uptake can be decreased by inhibiting organic anion transporting polypetides, as shown by the effect of fruit juices on fexofenadine (35).”