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

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.

SUBMITTER: Sandham DA

PROVIDER: S-EPMC5430394 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature

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

Sandham David A DA Barker Lucy L Brown Lyndon L Brown Zarin Z Budd David D Charlton Steven J SJ Chatterjee Devnandan D Cox Brian B Dubois Gerald G Duggan Nicholas N Hall Edward E Hatto Julia J Maas Janet J Manini Jodie J Profit Rachael R Riddy Darren D Ritchie Catherine C Sohal Bindi B Shaw Duncan D Stringer Rowan R Sykes David A DA Thomas Matthew M Turner Katharine L KL Watson Simon J SJ West Ryan R Willard Elisabeth E Williams Gareth G Willis Jennifer J

ACS medicinal chemistry letters 20170425 5

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. ...[more]

PMID: 28523115

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