Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma
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...
| Main Authors: | , , , , , , , , , , , , , , , , , , , , , , , , , , , |
|---|---|
| Format: | Article |
| Published: |
American Chemical Society
2017
|
| Subjects: | |
| Online Access: | https://eprints.nottingham.ac.uk/44096/ |
| _version_ | 1848796837191876608 |
|---|---|
| author | Sandham, David A. Barker, Lucy Brown, Lyndon Brown, Zarin Budd, David Charlton, Steven J. Chatterjee, Devnanden Cox, Brian Dubois, Gerald Duggan, Nicholas Hall, Edward Hatto, Julia Maas, Janet Manini, Jodie Profit, Rachael Riddy, Darren Ritchie, Catherine Sohal, Bindi Shaw, Duncan Stringer, Rowan Sykes, David A. Thomas, Matthew Turner, Katherine L. Watson, Simon J. West, Ryan Willard, Elisabeth Williams, Gareth Willis, Jennifer |
| author_facet | Sandham, David A. Barker, Lucy Brown, Lyndon Brown, Zarin Budd, David Charlton, Steven J. Chatterjee, Devnanden Cox, Brian Dubois, Gerald Duggan, Nicholas Hall, Edward Hatto, Julia Maas, Janet Manini, Jodie Profit, Rachael Riddy, Darren Ritchie, Catherine Sohal, Bindi Shaw, Duncan Stringer, Rowan Sykes, David A. Thomas, Matthew Turner, Katherine L. Watson, Simon J. West, Ryan Willard, Elisabeth Williams, Gareth Willis, Jennifer |
| author_sort | Sandham, David A. |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T19:54:19Z |
| format | Article |
| id | nottingham-44096 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| last_indexed | 2025-11-14T19:54:19Z |
| publishDate | 2017 |
| publisher | American Chemical Society |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-440962020-05-04T18:43:12Z https://eprints.nottingham.ac.uk/44096/ Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma Sandham, David A. Barker, Lucy Brown, Lyndon Brown, Zarin Budd, David Charlton, Steven J. Chatterjee, Devnanden Cox, Brian Dubois, Gerald Duggan, Nicholas Hall, Edward Hatto, Julia Maas, Janet Manini, Jodie Profit, Rachael Riddy, Darren Ritchie, Catherine Sohal, Bindi Shaw, Duncan Stringer, Rowan Sykes, David A. Thomas, Matthew Turner, Katherine L. Watson, Simon J. West, Ryan Willard, Elisabeth Williams, Gareth Willis, Jennifer 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. American Chemical Society 2017-04-25 Article PeerReviewed Sandham, David A., Barker, Lucy, Brown, Lyndon, Brown, Zarin, Budd, David, Charlton, Steven J., Chatterjee, Devnanden, Cox, Brian, Dubois, Gerald, Duggan, Nicholas, Hall, Edward, Hatto, Julia, Maas, Janet, Manini, Jodie, Profit, Rachael, Riddy, Darren, Ritchie, Catherine, Sohal, Bindi, Shaw, Duncan, Stringer, Rowan, Sykes, David A., Thomas, Matthew, Turner, Katherine L., Watson, Simon J., West, Ryan, Willard, Elisabeth, 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 DP2 receptor antagonist severe asthma clinical candidate http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.7b00157 doi:10.1021/acsmedchemlett.7b00157 doi:10.1021/acsmedchemlett.7b00157 |
| spellingShingle | DP2 receptor antagonist severe asthma clinical candidate Sandham, David A. Barker, Lucy Brown, Lyndon Brown, Zarin Budd, David Charlton, Steven J. Chatterjee, Devnanden Cox, Brian Dubois, Gerald Duggan, Nicholas Hall, Edward Hatto, Julia Maas, Janet Manini, Jodie Profit, Rachael Riddy, Darren Ritchie, Catherine Sohal, Bindi Shaw, Duncan Stringer, Rowan Sykes, David A. Thomas, Matthew Turner, Katherine L. Watson, Simon J. West, Ryan Willard, Elisabeth Williams, Gareth Willis, Jennifer Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma |
| title | Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma |
| title_full | Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma |
| title_fullStr | Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma |
| title_full_unstemmed | Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma |
| title_short | Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma |
| title_sort | discovery of fevipiprant (nvp-qaw039), a potent and selective dp2 receptor antagonist for treatment of asthma |
| topic | DP2 receptor antagonist severe asthma clinical candidate |
| url | https://eprints.nottingham.ac.uk/44096/ https://eprints.nottingham.ac.uk/44096/ https://eprints.nottingham.ac.uk/44096/ |