SLCO2B1 encodes OATP2B1, an organic anion transporting polypeptide that functions as a sodium-independent secondary active transporter localized to apical and basolateral plasma membranes 1. The protein mediates cellular uptake of diverse substrates including estrone 3-sulfate, prostaglandins, xenobiotics, and uremic toxins like indoxyl sulfate 2. SLCO2B1 exhibits tissue-specific expression in liver and small intestine, with Sp1 as a key transcriptional regulator 1. Clinically, SLCO2B1 genetic variants significantly impact multiple drug responses and disease outcomes. The rs12422149 A allele, which reduces testosterone precursor uptake, associates with lower prostate cancer progression rates (hazard ratio 0.80; 95% CI 0.69-0.93), suggesting potential for risk stratification in androgen deprivation therapy 3. The GG allele correlates with castration resistance and shorter time to progression 4. SLCO2B1 polymorphisms substantially affect abiraterone and fluvastatin pharmacokinetics, with variants influencing drug exposure and metabolite levels 56. In asthma, SLCO2B1 variants contribute to leukotriene modifier response variability 7. Additionally, SLCO2B1 mediates indoxyl sulfate-induced proinflammatory macrophage activation via Dll4-Notch signaling, linking the transporter to cardiovascular complications in chr11 kidney disease 2.