In the last decade, many organic anion transporters have been isolated, characterized their distribution and substrates. The recently identified organic anion transporter family OATP (organic anion transporting polypeptide)/LST (liver-specific transporter) family, transport bile acids, hormones as well as eicosanoids, various compounds (BSP, HMG-CoA reductase inhibitor, angiotensin converting enzyme inhibitor, etc.). The isolation of the family revealed that not only hydrophilic compounds, drugs and hormones of lipophilic nature need a membrane transport system to penetrate cell membrane. In this family, the nomenclature becomes very complicated and the physiological role of this family is still unclear except about few organs such as the brain, liver and kidney. Even in such organs, the co-existence of the OATP/LST family and similar substrate specificity hamper the progress and clear characterization identifying the real role of the transporter family. Here, recent progress and an insight of this field are reviewed.