Drug Transporters

Abstract

Membrane transporters perform a central function in many essential body functions, including traffic and compartmentalization of physiologic compounds, absorption of physiologic compounds (and, occasionally, structurally related xenobiotics, including drugs), and protection from potentially toxic exogenous compounds, which includes limiting their absorption and/or distribution and promoting their elimination (with no chemical modifications or as metabolites). The impact of drug biotransformation enzymes on pharmacokinetics and clinical outcome is much better understood than that of drug transporters, possibly due to the earlier discovery of metabolizing enzymes. The science of drug transporters can still be described as an emerging field, with knowledge on their structure, function, and regulation being continuously expanded.