Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP 2 Receptor Antagonist for Treatment of Asthma

ACS Med Chem Lett. 2017 Apr 25;8(5):582-586. doi: 10.1021/acsmedchemlett.7b00157. eCollection 2017 May 11.

Abstract

Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compound 11, NVP-QAW039, fevipiprant), which exhibits improved potency on human eosinophils and Th2 cells, together with a longer receptor residence time, and is currently in clinical trials for severe asthma.

Keywords: DP2 receptor antagonist; clinical candidate; severe asthma.