Escient Pharma Announces Promising Results from phase 1 study of EP262 to Treat mast cell Mediated Disorders

Escient Pharmaceuticals, a clinical-stage drug development firm focused on developing innovative small molecule treatments for systemic neuro-inflammatory disorders, published encouraging results from a phase 1 first-in-human study of EP262, a strong, highly selective MRGPRX2 antagonist. EP262 has the potential to treat mast cell-mediated illnesses by inhibiting MRGPRX2 activation and degranulation, with an initial focus on chronic urticaria (hives) and atopic dermatitis (eczema).

EP262 is a novel, targeted method to treating these illnesses, with the possibility for once-daily oral dosing without the substantial side effects seen with prior techniques. EP262 was safe and well-tolerated at all doses tested in the phase 1 study, which enrolled 64 healthy volunteers, with no serious or severe adverse events, no adverse events leading to discontinuation, and no adverse changes in safety laboratory parameters, vital signs, or ECG parameters identified. EP262 treatment-emergent adverse events were all moderate, with a lower incidence than placebo (33.3% vs. 62.5%) that did not increase with dose.

"The lack of significant safety findings in this first-in-human EP262 study is consistent with findings from nonclinical toxicology studies," stated Christian Weyer, M.D., M.A.S, Escient's chief medical officer. "Having pioneered MRGPRX2 pharmacology research with our proprietary preclinical knock-in model and successfully completed phase 1, we now look forward to evaluating the therapeutic potential of this new target in patients with mast cell-mediated disorders, a first in the field."

The phase 1 study was a randomized, double-blind, placebo-controlled trial to evaluate the safety, tolerability, and pharmacokinetics of single and multiple ascending doses of EP262 in healthy subjects. It included five single ascending dose levels of EP262, ranging from 50 mg to 1200 mg, and three multiple ascending dose levels of EP262, administered orally once a day. The doses were evaluated in cohorts of eight volunteers, including two individuals receiving placebo in each cohort. Escient Pharmaceuticals is a clinical-stage company focused on developing novel therapeutics to address a broad range of neurosensory-inflammatory disorders.