The FDA has cleared Escient Pharmaceuticals’ investigational new drug (IND) application for EP262. The clearance allows the Escient to initiate a Phase 1 first-in-human study for the company’s second drug candidate to be advanced into clinical development.

EP262 is a first-in-class, highly selective small molecule antagonist of MRGPRX2, a receptor mediating non-IgE driven mast cell degranulation. According to Escient, by blocking activation of MRGPRX2 and degranulation of mast cells, EP262 has the potential to effectively treat a broad range of mast cell mediated diseases with an initial focus on chronic urticarias (hives) and atopic dermatitis. EP262 represents a novel, targeted approach to the treatment of these disorders with the potential for once-daily oral administration without the side effects observed with other approaches.

“There is growing evidence that MRGPRX2 plays an important role in the pathogenesis of many diseases, as a key mediator of mast cell degranulation and neurogenic and eosinophilic inflammation,” Christian Weyer, MD, President and Chief Medical Officer of Escient Pharmaceuticals, said in a company news release. “Advancement of EP262 into the clinic marks an important milestone for Escient and for the field as it paves the way for clinical investigations aimed at elucidating and harnessing the therapeutic potential of this novel target.”

Escient plans to conduct a Phase 1 study in the first half of 2023 to evaluate the safety, tolerability and pharmacokinetics of EP262 in healthy volunteers. Following this study, in the second half of 2023, the company plans to initiate several clinical proof-of-concept studies evaluating EP262 in patients with chronic inducible urticaria, chronic spontaneous urticaria, and atopic dermatitis.