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Updated: May 27, 2026

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
Published on: October 17, 2013
Functions of OATP1A and 1B transporters in vivo: insights from mouse models
Dilek Iusuf1, Evita van de Steeg, Alfred H Schinkel
1Division of Molecular Biology, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands.
Abstract:
Organic anion-transporting polypeptides (OATPs) are a superfamily of uptake transporters that mediate the cellular uptake of a broad range of endogenous and exogenous compounds. Of these OATP transporters, members of the 1A and 1B subfamilies have broad substrate specificities. Because they are mainly expressed in liver, kidney and small intestine, OATP1A and 1B transporters can have a major impact on the pharmacokinetics of many drugs. To study their role in physiology and drug disposition, several mouse models lacking functional expression of one or more OATPs have been generated. This review discusses recent findings for these models that have led to new insights into the impact of OATP1A and 1B transporters on pharmacokinetics and toxicokinetics, and on bilirubin detoxification and bile acid handling in normal liver physiology.
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