Drug transport via the intestinal peptide transporter PepT1.

•The concept that PepT1 serves as a drug transporter has been further substantiated.•Significant progress has been made on drugs such as cefadroxil and valacyclovir.•Prodrugs of zanamivir, oseltamivir and didanosine have been developed.•High affinity does not necessarily translate into actual drug translocation.