KBP-2506 is a highly selective small-molecule MRGPRX2 antagonist that demonstrates breakthrough therapeutic potential for immune-inflammatory diseases such as Chronic Urticaria (CU) and Atopic Dermatitis (AD), which are caused by abnormal activation of mast cells. As a novel targeted therapeutic agent, KBP-2506 can effectively inhibits calcium influx and degranulation of LAD2 mast cells by specifically blocking the MRGPRX2 receptor signaling pathway on the surface of mast cells . significantly reduce the release of key inflammatory mediators ,such as histamine, trypsin, and cytokines,and thereby , regulate the abnormal immune response from the source of the disease.
In MRGPRX2 humanized genetically modified animal models, KBP-2506 demonstrated excellent in vivo activity. With outstanding oral bioavailability, favorable pharmacokinetic profile, and a broad therapeutic window, it holds promise as a best-in-class therapy in the field of dermatology.