Organic anion transporting polypeptide 2B1 (OATP2B1)

Organic anion transporting polypeptide 2B1 (OATP2B1) is a membrane transporter belonging to the solute carrier organic anion (SLCO) family, encoded by the SLCO2B1 gene. It is widely expressed in human tissues including the small intestine, liver, kidney, brain, placenta, heart, and others, with significant roles at barriers such as the intestines (for oral absorption) and hepatic sinusoidal membrane (for hepatic drug uptake). OATP2B1 mediates the uptake of a diverse range of organic anions, including pharmaceutical drugs (such as fexofenadine and statins), endogenous steroids, and other small molecules. Its activity is pH-dependent and exhibits substrate specificity somewhat narrower than related hepatic OATP transporters. OATP2B1 is implicated in the absorption and distribution of drugs and endogenous compounds, in drug-drug and drug-food interactions, and is influenced by common genetic variants which may affect drug efficacy and toxicity. Due to these roles, OATP2B1 is considered an important therapeutic target and a key determinant in pharmacokinetics and drug safety.

Other names

Solute carrier organic anion transporter family member 2B1SLCO2B1OATP-BOATPBSLC21A9

Drugs interact with OATP2B1 mainly as substrates (undergoing uptake into cells) or inhibitors (blocking transport activity, leading to altered pharmacokinetics and possible drug-drug or drug-food interactions), and the transport of some substrates is pH-dependent.