vasotide

Description: Vasotide, D(Cys-Leu-Pro-Arg-Cys) abbreviated as D(CLPRC), is a novel and potent peptidomimetic compound that targets two retinal VEGF receptors (VEGFR-1 and VEGFR-2) and reduces pathological angiogenesis in murine and nonhuman primate models of retinal disease. Blood vessel growth from preexisting vessels (angiogenesis) underlies many severe diseases including major blinding retinal diseases such as retinopathy of prematurity (ROP) and aged macular degeneration (AMD). This observation has driven development of antibody inhibitors that block a central factor in AMD, named vascular endothelial growth factor (VEGF), from binding to its receptors VEGFR-1 and VEGFR-2. However, some patients are insensitive to current anti-VEGF drugs or develop resistance, and the required repeated intravitreal injection of these large molecules is costly and clinically problematic. Vasotide inhibits retinal angiogenesis by binding selectively to the VEGF receptors, VEGFR-1 and Neuropilin-1 (NRP-1). Delivery of Vasotide in eye drops or via intraperitoneal injection in a laser-induced monkey model of human wet AMD, a mouse genetic knockout model of the AMD subtype called retinal angiomatous proliferation (RAP), and a mouse oxygen-induced model of retinopathy of prematurity (ROP) markedly decreased retinal angiogenesis in all three animal models. This prototype drug candidate is a promising new dual receptor inhibitor of the VEGF ligand with potential for translation into safer, less invasive applications to combat pathological angiogenesis in retinal disorders.

References: Sci Transl Med. 2015 Oct 14; 7(309):309ra165; Ann Transl Med. 2016 Oct; 4(Suppl 1):S41.