Fruit Juices as Perpetrators of Drug Interactions: The Role of Organic Anion–Transporting Polypeptides

2012/10/03 by M J Dolton, Michael Dolton, B D Roufogalis +3 · 74 citations
Chemistry · Medicine · #Antibiotics Pharmacokinetics and Efficacy #Bioavailability #Biochemistry #CYP3A4 #Chemistry #Clinical pharmacology #Cytochrome P450 #Drug #Drug Transport and Resistance Mechanisms #Food science #Fruit juice #Gastroesophageal reflux and treatments #Gene #Grapefruit juice #Medicine #Metabolism #Organic anion-transporting polypeptide #Organic cation transport proteins #Pharmacokinetics #Pharmacology #Transporter

paper · doi:10.1038/clpt.2012.159

published in Clinical Pharmacology & Therapeutics 92(5), 622-630 (Wiley)

openalex publication_date 2012/10/03 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/29

Abstract

Grapefruit juice is widely recognized to cause important drug interactions via inhibition of CYP3A4, and a wider variety of fruit juices have been shown to inhibit influx transporters in enterocytes known as organic anion-transporting polypeptides (OATPs). Fruit juice coadministration significantly reduces the oral bioavailability of numerous important medicines relying on this anion transporter pathway for absorption. This article reviews the current literature on interactions between clinically used OATP substrates and fruit juice consumption.

Citations

• Fruit juices inhibit organic anion transporting polypeptide–mediated drug uptake to decrease the oral availability of fexofenadine
• Intestinal Drug Transporter Expression and the Impact of Grapefruit Juice in Humans
• Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice

Cited by

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• Prioritizing pharmacokinetic drug interaction precipitants in natural products: application to OATP inhibitors in grapefruit juice. [europepmc]
• Phytotherapeutics: The Emerging Role of Intestinal and Hepatocellular Transporters in Drug Interactions with Botanical Supplements. [europepmc]
• Food-drug interactions precipitated by fruit juices other than grapefruit juice: An update review. [europepmc]
• Synergistic Effects of Plant Derivatives and Conventional Chemotherapeutic Agents: An Update on the Cancer Perspective. [europepmc]
• Identification of the amino acid residue responsible for the myricetin sensitivity of human proton-coupled folate transporter. [europepmc]
• Potential Risk of Food-Drug Interactions: Citrus Polymethoxyflavones and Flavanones as Inhibitors of the Organic Anion Transporting Polypeptides (OATP) 1B1, 1B3, and 2B1. [europepmc]
• The involvement of human organic anion transporting polypeptides (OATPs) in drug-herb/food interactions. [europepmc]
• The successful combination of grapefruit juice and venetoclax in an unfit acute myeloid leukemia patient with adverse risk: A case report. [europepmc]
• Interactions between natural products and cancer treatments: underlying mechanisms and clinical importance. [europepmc]
• Editorial: Case reports in hematological malignancies: 2022. [europepmc]
• Organic anion transporting polypeptides: Pharmacology, toxicology, structure, and transport mechanisms. [europepmc]

Related

• Fruit juices inhibit organic anion transporting polypeptide–mediated drug uptake to decrease the oral availability of fexofenadine
• Naringin is a Major and Selective Clinical Inhibitor of Organic Anion-Transporting Polypeptide 1A2 (OATP1A2) in Grapefruit Juice
• Intestinal Drug Transporter Expression and the Impact of Grapefruit Juice in Humans
• Medicinal importance of grapefruit juice and its interaction with various drugs
• Grapefruit–medication interactions: Forbidden fruit or avoidable consequences?