Abstract
Intestinal absorption is a pharmacokinetically important step to determine pharmacological efficacy of drugs because it affects bioavailability of drugs; however, it is not an easy task to create orally effective drug due to difficulty in providing with sufficient intestinal absorption. Current evidence shows that membrane transporters affect drug absorption and disposition, suggesting that they are potentially useful to adjust pharmacokinetic properties of drugs. This review will summarize the recent information regarding transporter-mediated intestinal absorption of drugs and introduce key membrane transporters with their contribution to drug absorption. In addition, this will also discuss about possible applications of transporters to enhance intestinal permeability of drugs which are highly soluble but poorly permeable to biological membrane, focusing on, in particular, H+-coupled oligopeptide transporter, PEPT1
