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Abstract
The importance of uptake transporters in determining drug disposition is increasingly
appreciated. While the focus of regulatory agencies worldwide has been on the hepatic
organic anion transporting polypeptides (OATPs)-1B1 and-1B3, there is another isoform
of the OATP sub-family, OATP2B1, which should be considered equally relevant. Unlike
the other members of the OATP sub-family, OATP2B1 is expressed in multiple organs
in humans, including in the intestine and the liver. Similar to other OATPs, OATP2B1
mediates the hepatic and intestinal uptake of many drugs and endogenous compounds.
The importance of OATP2B1 in the disposition of many drugs is highlighted by the growing
recognition of its role in significant in vivo drug-drug or food-drug interactions.
The dramatic changes in drug exposure attributable to inhibition of OATP2B1 highlight
the importance of developing a better understanding of the clinical role of OATP2B1.
This review aims to provide a thorough summary of the current understanding of the
pharmacogenetics, regulation, expression and abundance of OATP2B1 in humans, as well
as its clinical relevance in drug-drug and food-drug interactions.