The mammalian proton-coupled oligopeptide transporter PepT1 is recognised as an important route of oral drug delivery. Peptidebased compounds offer great potential as drugs but their application is limited by poor membrane permeability, amongst other challenges. Using cyclosporin A as a proof-of-concept, we demonstrate for the first time that peptidic molecules over 1000 Da in size can be targeted towards and transported by PepT1.