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

Solute carrier organic anion transporter family member 1B1 (OATP1B1) and ATP-binding cassette sub-family G member 2 (BCRP) are two distinct but functionally linked membrane transporters that play a pivotal role in the hepatic disposition of various drugs and endogenous substances [2, 4]. OATP1B1 is an uptake transporter located on the basolateral (sinusoidal) membrane of hepatocytes, responsible for the entry of organic anions from the blood into the liver [4, 10]. BCRP is an efflux transporter located on the apical (canalicular) membrane of hepatocytes and in the intestinal epithelium, where it mediates the excretion of substrates into the bile or gut lumen [4, 9]. Together, they form a vectorial transport system that is a primary determinant of the pharmacokinetics of many clinically important drugs, most notably HMG-CoA reductase inhibitors (statins) like rosuvastatin and pitavastatin [2, 6, 8]. Genetic polymorphisms in the genes encoding these transporters, such as SLCO1B1 (OATP1B1) and ABCG2 (BCRP), as well as their inhibition by other drugs, can lead to significant increases in systemic drug exposure and an associated risk of toxicity, such as statin-induced myopathy [2, 9, 11]. Consequently, they are extensively studied in the context of drug-drug interactions and are recognized as key 'antitargets' by regulatory agencies during drug development [3, 8, 10].

Other names

SLCO1B1ABCG2OATP-COATP2LST-1MXRABCPBCRP1CD338

Drugs typically act as substrates or inhibitors of these transporters, affecting the systemic exposure and tissue distribution of co-administered medications.