OATP transporter-mediated drug absorption and interaction

Although oral administration of drugs is the most favorable route, the precise mechanism of intestinal epithelial permeation is not well understood. Recently, compelling evidence has emerged to show that absorptive transporters such as OATPs contribute to intestinal drug absorption. Since changes in intestinal transporter activity may alter systemic exposure, a thorough understanding of the overall intestinal absorption mechanism is essential to predict possible toxicity and to achieve optimal therapeutic efficacy. The intestinal lumen is exposed continuously to ingested food and beverages, and interaction of their components with drugs during intestinal permeation might also be significant. OATP2B1 is expressed in human intestine and transports various drugs. In this review, we describe the importance of OATP2B1 in drug absorption and the possible influence beverage components have on OATP2B1 function and expression.