SLCO2B1

SLCO2B1 is the gene encoding the organic anion transporting polypeptide 2B1 (OATP2B1), a member of the solute carrier SLCO/OATP family. The protein functions as a membrane transporter that facilitates the cellular uptake of a diverse range of endogenous compounds and xenobiotics, contributing to the pharmacokinetics of many drugs and to normal physiology.

OATP2B1 is widely expressed in human tissues, with notable levels in the small intestine, liver, kidney, brain, and placenta. In these tissues, it participates in the absorption of orally administered compounds, hepatic uptake from the blood, and possibly transport at barriers such as the blood-brain barrier. The transporter exhibits broad substrate specificity, including steroid conjugates, bile acids, thyroid hormones, and various pharmaceutical agents. Its activity can influence drug absorption, distribution, and clearance, and it can be inhibited or modulated by other drugs and dietary substances.

Genetics and regulation of SLCO2B1 contribute to interindividual differences in drug response. Polymorphisms in SLCO2B1 can alter transporter activity and impact the pharmacokinetics of certain medications. Expression and function may be influenced by regulatory factors such as nuclear receptors and inflammatory states, reflecting broader physiological and pathophysiological contexts.

Clinical relevance of SLCO2B1 centers on pharmacokinetic variability and potential drug–drug or drug–diet interactions. Understanding SLCO2B1 can help explain differences in drug exposure and, in some cases, therapeutic efficacy or risk of toxicity. Further research continues to clarify substrate range, tissue-specific roles, and the clinical implications of genetic variation in this transporter.