Enanta MRGPRX2 inhibitor

Enanta Pharmaceuticals is developing an oral small molecule inhibitor of the Mas-related G protein-coupled receptor X2 (MRGPRX2) for the treatment of mast cell-mediated inflammatory diseases, specifically chronic spontaneous urticaria (CSU) and atopic dermatitis (AD). MRGPRX2 is a non-canonical GPCR expressed primarily on mast cells that mediates IgE-independent activation and degranulation, a pathway distinct from the traditional IgE-mediated allergic response. Enanta's prototype inhibitors demonstrate nanomolar potency (EC50 of 1-2nM) and high selectivity for MRGPRX2 over other GPCRs. Preclinical studies in humanized mouse models have shown that these compounds prevent skin mast cell activation. The program is designed for once-daily oral administration, with a development candidate selection expected in the second half of 2026.

Other names

Undisclosed MRGPRX2 inhibitor