Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma

David A. Sandham, Lucy Barker, Lyndon Brown, Zarin Brown, David Budd, Steven J Charlton, Devnandan Chatterjee, Brian J Cox, Gerald Dubois, Nicholas Duggan, Edward Hall, Julia Hatto, Janet Maas, Jodie Manini, Rachael Profit, Darren Riddy, Catherine Ritchie, Bindi Sohal, Duncan Shaw, Rowan StringerDavid A. Sykes, Matthew B Thomas, Katharine L. Turner, Simon J. Watson, Ryan West, Elisabeth Willard, Gareth Williams, Jennifer Willis

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)582-586
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume8
Issue number5
DOIs
Publication statusPublished - 25 Apr 2017
Externally publishedYes

Keywords

  • clinical candidate
  • DP receptor antagonist
  • severe asthma

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