Organic anion transporting polypeptide 1B1 and 1B3 (OATP1B1 and OATP1B3)

Organic anion transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) are critical membrane transporters located on the basolateral (sinusoidal) membrane of human hepatocytes. Belonging to the solute carrier organic anion (SLCO) family, they facilitate the hepatic uptake of a wide range of endogenous substances, such as bilirubin and bile acids, as well as numerous clinically important drugs. These transporters are major determinants of the pharmacokinetics and systemic exposure of medications like HMG-CoA reductase inhibitors (statins). Genetic polymorphisms in the genes encoding these transporters, particularly SLCO1B1, are associated with significant interindividual variability in drug response and an increased risk of adverse effects, such as statin-induced myopathy. Furthermore, OATP1B1 and OATP1B3 are frequently involved in drug-drug interactions when co-administered with inhibitors like cyclosporine or rifampin, leading to elevated plasma concentrations of substrate drugs. In addition to their role in drug disposition, these transporters are often overexpressed in various cancers, making them potential targets for tumor-targeted drug delivery or therapy.

Other names

SLCO1B1SLCO1B3OATP-COATP-8LST-1LST-2OATP2SLC21A6SLC21A8

Substrate transport and Inhibition