Holding Hands: Using Peptide-Drug Conjugates (PDCs) for the Precise Treatment of Pulmonary Fibrosis

Targeted therapy represents an emerging paradigm for the current biomedical research, since selective and precise delivery of drugs to diseased tissues may be a good strategy to improve the therapeutic efficiency of the drug/probe, to overcome drug resistance, to reduce the off-target effects and to early detect several diseased states. Among the different strategies, Peptide-Drug Conjugates (PDCs) – that is constructs composed by i) a peptidic/peptidomimetic targeting unit; ii) a linker that connects the targeting unit with the drug; iii) the active payload (drug) – which has emerged as new tools for targeted therapy.

In this context, Dr. Kelly and her colleagues synthesized a panel of PDCs aiming at the precise treatment of pulmonary fibrosis, where nintedanib – a potent kinase inhibitor approved for the treatment of idiopathic pulmonary fibrosis – and a peptidomimetic targeting αVβ6 integrin – which is a receptor overexpressed in fibrotic tissues – are connected by different linkers. Given the promising in vitro results of one synthesized PDC, the in vivo antifibrotic activity is currently under evaluation in mice models of pulmonary fibrosis.