Solute carrier organic anion transporter family member 1B1 (SLCO1B1) (SLCO1B1)

Solute carrier organic anion transporter family member 1B1 (SLCO1B1), also known as OATP1B1, is a critical membrane-bound transporter protein primarily expressed on the basolateral membrane of hepatocytes [1, 5]. It facilitates the sodium-independent hepatic uptake of a wide range of endogenous compounds, such as bilirubin and bile acids, as well as numerous clinically important drugs, most notably statins [1, 4, 9]. Genetic variations in the SLCO1B1 gene, particularly the rs4149056 (T521C) polymorphism, significantly impact the transporter's functional activity, leading to altered drug pharmacokinetics [1, 11, 12]. Reduced function of OATP1B1 results in elevated systemic concentrations of substrate drugs, which is a major risk factor for statin-associated muscle symptoms (SAMS) and life-threatening rhabdomyolysis [3, 11, 14]. Beyond statins, SLCO1B1 is involved in the disposition of other therapeutic agents like methotrexate and repaglinide, making it a key focus in pharmacogenomics and drug-drug interaction studies [1, 13]. Consequently, SLCO1B1 genotyping is increasingly used in clinical practice to personalize medication dosing and minimize adverse drug reactions [6, 7, 14].

Other names

OATP1B1OATP-CLST-1SLC21A6OATP2OATPCLiver-specific organic anion transporter 1Sodium-independent organic anion-transporting polypeptide 2

Drugs interact with SLCO1B1 primarily as substrates for hepatic uptake or as inhibitors that block the transport of other substrates [1, 2, 6].