• Data shows that EP262 attenuates mast cell degranulation in multiple species including human MRGPRX2 knock-in mice, Beagle dogs and human ex vivo skin explants
  • Results support the initiation of clinical proof-of-concept studies in chronic urticaria, planned for the second half of 2023

SAN DIEGO, CA, USA I June 08, 2023 I Escient Pharmaceuticals, a clinical-stage company advancing novel small molecule therapeutics for the potential treatment of a broad range of neurosensory-inflammatory disorders, today announced the presentation of preclinical data in multiple models of mast cell degranulation related to the company’s EP262 development program at the European Academy of Allergy and Clinical Immunology annual meeting being held in Hamburg, Germany, June 9-11, 2023.

EP262 is a potent, highly selective antagonist of MRGPRX2 which inhibits agonist-induced mast cell degranulation and activation of the downstream inflammatory cascade, thus representing a novel therapeutic approach to a broad range of mast cell-mediated disorders.

The presentation highlights preclinical data demonstrating that treatment with EP262 potently attenuates mast cell degranulation and vascular permeability in vivo in a proprietary human MRGPRX2 transgenic mouse model. In addition, EP262 was shown to block canine MRGPRX2-induced mast cell degranulation responses in Beagle dogs and to attenuate mast cell degranulation-induced histamine release in ex vivo human skin explants.

Details of the presentation are shown below:

Presentation Title: MRGPRX2 Small Molecule Antagonists Potently Inhibit Agonist-Induced Skin Mast Cell Degranulation
Presenter: Veena Viswanath PhD, Sr Vice-President Translational Biology and Drug Discovery, Escient Pharmaceuticals
Presentation Date: Friday, June 09, 2023
Conference website: https://eaaci.org/events_congress/eaaci-congress-2023/

The abstract will be available on Escient’s website (under Scientific Presentations) here: https://www.escientpharma.com/science/publications/

About EP262

EP262 is a potent, highly selective once-daily small molecule antagonist of MRGPRX2, a receptor expressed on mast cells that is activated by numerous ligands, including many peptides released from sensory neurons as well as other cell types. In response to MRGPRX2 activation, mast cells release histamine, tryptase, chymase, chemokines and cytokines, which can cause itchy hives, angioedema, type 2 inflammation (through engagement of the adaptive immune system) and chronic pruritus and pain. Escient’s preclinical data demonstrates that, by blocking activation of MRGPRX2, EP262 has the potential to effectively treat a broad range of mast-cell-mediated diseases, with an initial focus on chronic urticarias and atopic dermatitis.

About Chronic Urticaria

Chronic urticaria, defined as urticaria persisting for more than 6 weeks, manifests with very itchy hives that may vary in size and can significantly impact a patient’s quality of life by interfering with sleep and daily activities. Some patients with chronic urticaria may also develop swelling deeper under the skin or in other tissues (angioedema). There are two main forms of chronic urticaria. In chronic spontaneous urticaria (CSU), hives occur spontaneously, without known triggers. In chronic inducible urticaria (CIndU), hives are induced by specific triggers such as cold exposure (cold urticaria) or touch (symptomatic dermographism), among others.

About Escient Pharmaceuticals

Escient Pharmaceuticals is a clinical-stage company focused on developing novel therapeutics to address a broad range of neurosensory-inflammatory disorders. The company’s pipeline includes two first-in-class small molecule antagonists targeting MRGPRX2 for the treatment of various mast cell mediated disorders and MRGPRX4 for cholestatic pruritus. Based in San Diego, California, Escient is led by an experienced management and scientific team and funded by top-tier life science investors.

Visit www.escientpharma.com to learn more.

SOURCE: Escient Pharmaceuticals