CRTH2 is a G protein coupled receptor. It is of interest as a target for drugs that treat allergic disease for the following reasons:
Significance of timapiprant for Patients
- It is selectively expressed by the key effector cell types mediating allergic responses – Th2 lymphocytes, type 2 innate lymphoid cells (ILCs), basophils and eosinophils
- CRTH2 is specifically activated by prostaglandin D2, an abundant lipid product of activated mast cells.
- Mast cell dependent activation of Th2 lymphocytes, type 2 ILCs and eosinophils is blocked by CRTH2 antagonists
- The prostaglandin D2/CRTH2 pathway is known to be upregulated in severe eosinophilic asthma, and implicated in the pathogenesis of atopic dermatitis