Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, and ATP-binding cassette sub-family G member 2 (OATP1B1/3 and BCRP)

OATP1B1, OATP1B3, and BCRP are critical membrane transporters that collectively govern the pharmacokinetics and disposition of numerous drugs and endogenous compounds. OATP1B1 and OATP1B3 are uptake transporters primarily located on the sinusoidal membrane of hepatocytes, where they facilitate the entry of substrates such as statins, bile acids, and bilirubin from the blood into the liver for metabolism and excretion. BCRP is an efflux transporter expressed in the liver, intestine, and blood-brain barrier, serving to limit the absorption or promote the biliary and renal clearance of drugs like rosuvastatin and various chemotherapeutic agents. These transporters are major sites of clinically significant drug-drug interactions; for example, the inhibition of OATP1B1 by drugs like cyclosporine can dramatically increase the plasma concentration of statins, significantly raising the risk of myopathy and rhabdomyolysis. Genetic variations in these transporters, particularly the SLCO1B1 c.521T>C polymorphism, are well-documented to influence drug efficacy and safety profiles. Due to their profound impact on drug safety, regulatory agencies like the FDA and EMA require the evaluation of these transporters during the drug development process to predict and manage potential interaction risks.

Other names

SLCO1B1SLCO1B3ABCG2Organic anion transporting polypeptide 1B1Organic anion transporting polypeptide 1B3Breast cancer resistance proteinOATP-COATP8LST-1LST-2MXRABCPCDw338

Inhibition of hepatic uptake (OATP1B1/3) or efflux (BCRP) activity, leading to increased systemic exposure and potential toxicity of substrate drugs.