At the ongoing AAAAI meeting in San Antonio, researchers from Escient Pharmaceuticals Inc. presented preclinical data for the Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist EP-262, being evaluated as a novel therapeutic approach for mast cell-mediated diseases. In vitro, EP-262 acted as a potent and highly selective antagonist of MRGPRX2, which inhibited MRGPRX2 activation induced by a wide variety of agonists.
Escient Pharmaceuticals Inc. has obtained FDA clearance of its IND application for EP-262, a first-in-class, potent, highly selective small-molecule antagonist of Mas-related G-protein coupled receptor member X2 (MRGPRX2) for mast cell-mediated disorders.
Mas-related G-protein coupled receptor X2 (MRGPRX2) is expressed particularly on mast cells and its activation leads to the mast cell degranulation with release of inflammatory mediators.
