US EPA

9641809 

Journal Article 

Review 

Organic anion-transporting polypeptide (OATP) transporter family and drug disposition 

Kim, RB 

2003 

Yes 

European Journal of Clinical Investigation
ISSN: 0014-2972
EISSN: 1365-2362 

33 Suppl 2 

1-5 

English 

14641549 

10.1046/j.1365-2362.33.s2.5.x 

Drug transporters are increasingly recognized as a key determinant of drug disposition. Recent studies have revealed that targeted expression of drug uptake and efflux transporters to specific cell membrane domains allows for the efficient directional movement of many drugs in clinical use. While the role of certain efflux transporters such as MDR1 (P-glycoprotein) in drug disposition has been extensively studied, emerging evidence suggests that uptake transporters may also be important to the intestinal absorption and renal or hepatic elimination of drugs. Members of the organic anion-transporting polypeptide (OATP) family of drug uptake transporters have been found capable of transporting a large array of structurally divergent drugs. Moreover, expression of OATP isoforms in the gastrointestinal tract, liver and kidney, as well as at the level of the blood-brain barrier, has important implications for our understanding of the factors governing drug absorption, elimination and tissue penetration.