EP262

EP262 is a potent, highly selective, once-daily oral small molecule antagonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2), a receptor expressed on mast cells and activated by various neuropeptides and other agonists. By blocking MRGPRX2 activation and subsequent mast cell degranulation, EP262 aims to treat multiple mast cell-mediated diseases. Its initial clinical focus is on chronic urticaria (including chronic spontaneous urticaria and chronic inducible urticaria) and atopic dermatitis (eczema). The drug has demonstrated safety and tolerability in Phase 1 studies, with ongoing Phase 2 proof-of-concept trials. Originally developed by Escient Pharmaceuticals, the program was acquired by Incyte in April 2024[3][5][6][7][8].