OATP1B1 (OATP1B1)

Organic Anion-Transporting Polypeptide 1B1 (gene: SLCO1B1), a hepatic uptake transporter predominantly expressed on the sinusoidal (basolateral) membrane of hepatocytes. Mediates the sodium-independent uptake of statins, bilirubin, thyroid hormones, and other organic anions from portal blood into the liver. The SLCO1B1 c.521T>C polymorphism significantly increases simvastatin myopathy risk.

Exemples

• SLCO1B1*5 variant increasing simvastatin-induced myopathy 5-fold
• Cyclosporine inhibition of OATP1B1 raising statin plasma levels
• Rifampin single-dose inhibition of OATP1B1 (vs chronic induction of CYP3A4)