The US Food and Drug Administration (FDA) has cleared Escient Pharmaceuticals’ investigational new drug (IND) application to commence a Phase I first-in-human trial of EP262 for mast cell mediated disorders.

The Phase I study has been designed for assessing the pharmacokinetics, tolerability, and safety of EP262 in healthy volunteers.

EP262 is a first-in-class, potent, oral, once-daily, highly selective small molecule antagonist of Mas-related G protein-coupled receptor X2 (MRGPRX2), a receptor mediating non-IgE driven mast cell degranulation.

It is being developed to treat several mast cell-mediated diseases, with an initial focus on atopic dermatitis and chronic urticarias, by blocking MRGPRX2 activation and mast cells degranulation.

Escient Pharmaceuticals stated that EP262 is a new, targeted method to treat these disorders by oral administration of the MRGPRX2 antagonist once a day, without any serious side effects.

Escient Pharmaceuticals president and chief medical officer Christian Weyer said: “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.

“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.”

The company intends to commence the Phase I study in the first half of this year.

After completion of the trial, Escient also plans to commence many clinical proof-of-concept studies to assess EP262 in chronic spontaneous urticaria, chronic inducible urticaria, and atopic dermatitis patients, in the second half of this year.