The involvement of human organic anion transporting polypeptides (OATPs) in drug-herb/food interactions

Organic anion transporting polypeptides (OATPs) are important transporter proteins that are expressed at the plasma membrane of cells, where they mediate the influx of endogenous and exogenous substances including hormones, natural compounds and many clinically important drugs. OATP1A2, OATP2B1, OATP1B1 and OATP1B3 are the most important OATP isoforms and influence the pharmacokinetic performance of drugs. These OATPs are highly expressed in the kidney, intestine and liver, where they determine the distribution of drugs to these tissues. Herbal medicines are increasingly popular for their potential health benefits. Humans are also exposed to many natural compounds in fruits, vegetables and other food sources. In consequence, the consumption of herbal medicines or food sources together with a range of important drugs can result in drug-herb/food interactions via competing specific OATPs. Such interactions may lead to adverse clinical outcomes and unexpected toxicities of drug therapies. This review summarises the drug-herb/food interactions of drugs and chemicals that are present in herbal medicines and/or food in relation to human OATPs. This information can contribute to improving clinical outcomes and avoiding unexpected toxicities of drug therapies in patients.