In Vitro and In Vivo Efficacy on Retinal Neo-Vascularization of an Innovative Broad-Range Anti-Angiogenic Synthetic Peptide (Uparant)

Pathologic blood neovessels growth in the macular region of the retina is responsible for several serious illnesses that can quickly lead to vision loss. Nowadays, some anti-angiogenic drugs for intravitreal use are present on the market, targeting the main angiogenic factor, VEGF. However, not all patients respond to anti-VEGF therapy (some 30% are classified as non-responders), and chronic suppression of VEGF (which appears to be also a neurotrophic factor) could exert some negative effects in the long run. We present here a new drug, a modified tetrapeptide, that works as an antagonist of the urokinase plasminogen activator cell receptor, that is able to inhibit the angiogenic response of endothelial cells to several different angiogenic and pro-inflammatory factors, since it blocks their motility and invasion independently from the trigger. We show evidence of its efficacy in widely known experimental model systems both in vitro and in vivo.