ROLE OF ORGANIC CATION TRANSPORTERS IN DRUG ABSORPTION AND ELIMINATION

Organic cation transporters are critical in drug absorption, targeting , and disposition. It has become increasingly clear that multiple mech anisms are involved in organic cation transport in the key tissues res ponsible for drug absorption and disposition: the kidney, liver, and i ntestine. In this review, we discuss current models of transepithelial flux of organic cations in these three tissues. Particular emphasis i s placed on the more recent molecular studies that have paved the way for a more complete understanding of the physiological and pharmacolog ical roles of the organic cation transporters. Such information is ess ential in predicting pharmacokinetics and pharmacodynamics and in the design and development of cationic drugs.