Solute carrier organic anion transporter family member 1B1 (OATP1B1)

Solute carrier organic anion transporter family member 1B1 (OATP1B1) is a liver-specific transporter protein encoded by the SLCO1B1 gene. Located on the surface of hepatocytes, OATP1B1 facilitates the sodium-independent uptake of a wide range of endogenous organic anions (such as bilirubin and hormones) and numerous drugs—including statins, certain antibiotics, rifampin, and chemotherapeutics—from the bloodstream into liver cells. This transport is essential for drug clearance, hormone regulation, and removal of metabolic waste. Genetic variants in SLCO1B1 significantly impact transporter function, altering the pharmacokinetics of its substrates and contributing to drug response variability and risk of adverse effects, especially statin-induced myopathy. Clinical genetic testing for SLCO1B1 polymorphisms is used to optimize statin therapy and minimize the risk of muscle toxicity

Other names

OATP1B1OATP-COATP-2OATP2OATPCSLC21A6SO1B1LST-1LST1liver-specific organic anion transporter 1solute carrier family 21 member 6sodium-independent organic anion-transporting polypeptide 2HBLRR

Facilitates hepatic uptake of drugs (including statins), affecting plasma concentrations and therapeutic/toxic response Genetic variation may diminish transporter function, raising plasma levels and risk of drug toxicity (myopathy) Enhanced transporter function can increase hepatic clearance, lowering drug efficacy