Solute carrier organic anion transporter family member 2B1 (OATP2B1) (OATP2B1)

Solute carrier organic anion transporter family member 2B1 (OATP2B1), encoded by the SLCO2B1 gene, is a member of the solute carrier organic anion transporter family [1, 2, 8]. It is a ubiquitously expressed uptake transporter found in various tissues, most notably on the apical membrane of intestinal enterocytes and the sinusoidal membrane of hepatocytes [1, 4, 6]. Its primary biological function is the sodium-independent uptake of a broad range of endogenous compounds, such as steroid sulfates and thyroid hormones, as well as numerous xenobiotics, including statins and fexofenadine [1, 5, 8]. A unique characteristic of OATP2B1 is its pH-dependent activity, showing enhanced transport efficiency under the acidic conditions typically found in the upper small intestine [1, 6, 8]. In clinical practice, OATP2B1 is a critical determinant of the oral bioavailability and systemic disposition of many drugs [3, 4, 6]. It is a major site for drug-drug and food-drug interactions; for instance, components in fruit juices can inhibit OATP2B1, significantly reducing the absorption of substrate drugs like fexofenadine [3, 5, 7, 10]. Genetic polymorphisms in the SLCO2B1 gene also contribute to inter-individual variability in drug response and exposure [5, 7, 11]. Beyond its role in pharmacokinetics, OATP2B1 is often overexpressed in various cancers, where it may facilitate the uptake of hormones that drive tumor growth, making it a subject of interest in oncology and personalized medicine [10].

Other names

SLCO2B1OATP-BOATPBSLC21A9Organic anion transporter BOrganic anion transporter polypeptide-related protein 2OATP-RP2

Facilitated diffusion, sodium-independent uptake, pH-dependent transport, and transporter inhibition [1, 2, 6, 8, 10].