Novel Small Molecule MRGPRX2 Antagonists for the Treatment of Allergic Reactions

Clinically, patients with allergic reactions, such as atopic dermatitis, psoriasis and rosacea remain a limited response to available drugs. Upregulation of MRGPRX2 expression in these allergic reactions strongly suggested the pathophysiological role of MRGPRX2. However, there is no MRGPRX2 targeting drug available in the market.

• The underlying mechanism of the invention are small molecules designed by the computational approach which can bind to MRGPRX2 and inhibit its activity
• In vivo evaluation of the effect of the potent novel small molecules on compound 48/80 induced allergy and local anaphylaxis activity showed that the compound candidate can significantly reduce epidermal thickness and mast cell degranulation compared to the non-treatment group
• The compound candidates can significantly reverse the body temperature change and reduce anaphylaxis symptoms induced by allergy inducers compared with non-treatment group

• Specifically target MRGPRX2 involved non-IgE non-IgE mediated allergic reactions 
• Suitable for oral and topical applications due to small molecules involved

• Drugs for anti-allergic reactions, especially for chronic allergic reactions, e.g. atopic dermatitis, psoriasis and rosacea 

• US Application No: 17/334,872
• PRC Application No: 202210608467.9