As liver is the main organ governing systemic clearance of raloxifene, the aim of the present study was to identify the role of OATP1B1 and OATP1B3 transporters in hepatic uptake of raloxifene species and to investigate the influence of SLCO1B1 and SLCO1B3 genetic polymorphisms on pharmacokinetics and pharmacodynamics of raloxifene in women with postmenopausal osteoporosis. The gene discussed is SLCO1B1; the disease is postmenopausal osteoporosis.