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timapiprant

Development stage: Phase 2
Lead developer: Chiesi
Modality: Small Molecules
Administration: Oral

Overview

Timapiprant (AZD1981) is an orally bioavailable small molecule antagonist of the prostaglandin D2 receptor 2 (DP2), also known as chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). Developed by AstraZeneca, it was primarily investigated as a non-steroidal treatment for asthma. By blocking the DP2 receptor, timapiprant inhibits the activation and migration of Th2 cells, eosinophils, and basophils, which are key drivers of allergic inflammation. Despite reaching Phase II clinical trials, the drug failed to demonstrate significant efficacy in primary endpoints for asthma and development was subsequently discontinued.

Other names: 4-(acetylamino)-3-[(4-chlorophenyl)thio]-2-methyl-1H-indole-1-acetic acidAZD-1981AZD1981AZD 1981

Targets

PTGDR2 (Prostaglandin D2 receptor 2)

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