Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma

Sandham, David A. and Barker, Lucy and Brown, Lyndon and Brown, Zarin and Budd, David and Charlton, Steven J. and Chatterjee, Devnanden and Cox, Brian and Dubois, Gerald and Duggan, Nicholas and Hall, Edward and Hatto, Julia and Maas, Janet and Manini, Jodie and Profit, Rachael and Riddy, Darren and Ritchie, Catherine and Sohal, Bindi and Shaw, Duncan and Stringer, Rowan and Sykes, David A. and Thomas, Matthew and Turner, Katherine L. and Watson, Simon J. and West, Ryan and Willard, Elisabeth and Williams, Gareth and Willis, Jennifer (2017) Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma. ACS Medicinal Chemistry Letters, 8 . pp. 582-586. ISSN 1948-5875

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Abstract

Further optimization of an initial DP2 receptor antagonist clinical candidate NVPQAV680 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.

Item Type: Article
Keywords: DP2 receptor antagonist, severe asthma, clinical candidate
Schools/Departments: University of Nottingham, UK > Faculty of Medicine and Health Sciences > School of Life Sciences > School of Biomedical Sciences
Identification Number: 10.1021/acsmedchemlett.7b00157
Depositing User: Charlton, Steven
Date Deposited: 12 Jul 2017 10:36
Last Modified: 12 Oct 2017 23:41
URI: http://eprints.nottingham.ac.uk/id/eprint/44096

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