Oral drug delivery using peptide carriers (360G-Wellcome-074116_Z_04_A)

University Translation Award Oral drug delivery using peptide carriers PepT1 is a protein located in the jejenum region of the small intestine, and (to lesser extents) in specific membranes of other organs (e.g. kidney, lung). PepT1 transports di- and tri-peptides across the wall of the small intestine, and it is the primary mechanism by which nitrogen enters the bloodstream. It is also able to transport certain drugs (e.g. ß-lactams, peptidic ACE inhibitors), but most drugs are not recognised or transported by PepT1. We aim to develop dipeptide analogues that will be recognised and transported by PepT1, and to which drug molecules that are not orally active might be attached. The resulting conjugates are intended to increase the bioavailability of the drug, by facilitating uptake via the PepT1 pathway in the small intestine, followed by release of the active drug by hydrolysis. The commercialisation objectives are: a) Identify the optimum patenting strategy and exemplify the UK priority patent filing through synthesis of relevant dipeptide analogues; b) Identify the best carrier(s) for drug delivery by an extensive structure-activity analysis, and develop the technical know-how to prepare specific drug-carrier conjugates; c) Conduct initial market research to identify the areas of commercial opportunity, and develop a more detailed commercialisation strategy based upon the results.