MRGPRX2 Program

Chronic Spontaneous Urticaria (CSU) and Other Mast Cell Diseases

Chronic spontaneous urticaria (CSU) is a systemic inflammatory skin disease characterized by the spontaneous and persistent recurrence of itchy, painful hives on the skin and angioedema, or swelling, that affects approximately 1.5 million patients in the United States. While there is no known trigger, the degranulation of mast cells and release of histamine and other inflammatory mediators lead to these debilitating symptoms.

Multiple other diseases are driven by activated mast cells including allergic asthma, atopic dermatitis, interstitial cystitis, migraine, and prurigo nodularis.

Oral Small Molecule MRGPRX2 NAM for CSU and Other Mast Cell Diseases

Mas-related G-protein coupled receptor member X2 (MRGPRX2) plays an important role in mast cell activation and degranulation. We believe an oral therapy that inhibits MRGPRX2 could provide a differentiated treatment option for patients with CSU given the selective inhibition of mast cells and potential for combination therapy.