• Phase 2a placebo-controlled study to enroll approximately 30 patients with moderate to severe atopic dermatitis (AD)
  • Study supported by preclinical findings, showing that once-a-day oral treatment with EP262 potently reduced skin inflammation in a mouse model of AD

SAN DIEGO, CA, USA I November 28, 2023 I Escient Pharmaceuticals, a clinical-stage drug development company advancing novel small molecule therapeutics for systemic neuro-immune disorders, today announced that the first subject has been dosed in EASE, a Phase 2a clinical proof-of-concept study of EP262 in subjects with atopic dermatitis (AD).

By blocking activation of MRGPRX2 and degranulation of mast cells, EP262 has the potential to effectively treat multiple mast cell mediated diseases with an initial focus on chronic urticaria (hives) and atopic dermatitis (eczema). 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.

The Phase 2a study, EASE, is a randomized, double-blind, placebo-controlled study designed to evaluate the safety, tolerability and pharmacodynamics of EP262 in approximately 30 patients with moderate to severe AD. Patients will be randomized, in a 2:1 ratio, to treatment with EP262 150 mg, or placebo, administered orally, once daily for 6 weeks, followed by an off-treatment follow-up period. The study will evaluate clinical scores as well as histological and transcriptomic markers in lesional skin biopsies. More information about this study is available on www.clinicaltrials.gov (Identifier: NCT06144424).

In preclinical studies, in a well-established mouse model (HDM/SEB) that replicates several key features of human AD, oral treatment with EP262 improved AD-like skin lesions and markers of type 2 inflammation. Notably, the preclinical efficacy observed with EP262 treatment was comparable to that of anti IL4 treatment in this model. Some of this data was presented at the American Academy of Dermatology annual meeting in March 2023, as highlighted in our press release issued on March 16, 2023.

With the initiation of our EASE clinical proof-of-concept study, we look forward to evaluating whether the promising preclinical findings with EP262 translate to patients with atopic dermatitis,” said Christian Weyer, M.D., M.A.S, Chief Medical Officer at Escient. “If successful, EP262 could become a well-differentiated, once daily oral treatment option.”

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 Atopic Dermatitis

Atopic dermatitis is a chronic inflammatory skin disease characterized by abnormalities in immune regulation and skin barrier function. The disease typically manifests with itchy eczematous skin lesions. Thickening, crusting and cracking of the skin may also develop over time. Hypersensitivity to house dust mites and skin colonization by staphylococcus aureus are present in the majority of patients. And these are among the causative or exacerbating factors thought to contribute to the disease.

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