Abstract: During the recent years, drug transporters have been known to play an increasingly important role in drug absorption and metabolism. Organic anion transporting polypeptides(OATPs), particularly OATP1B1, OATP1B3 and OATP2B1, are being increasingly recognized as important factors in governing the pharmacokinetics of clinical medicine because of their expression in critical tissues such as the liver, intestine and kidneys. Meanwhile, a variety of clinically used drugs have been identified as substrates of OATP transporters(e. g. many statins are substrates of OATP1B1). Some drugs may inhibit OATP transporters(e. g. cyclosporine A), causing pharmacokinetic drug-drug interactions. Moreover, genetic variability in genes encoding OATP transporters can result in marked inter-individual differences in pharmacokinetics. The aim of our work was to review the expression of OATP transporters in human and their substrates, drug-drug interactions and genetic polymorphisms, as well as their roles in drug pharmacokinetics and pharmacological efficacy.