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 Stringer & 8 others David 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

6 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
JournalA C S Medicinal Chemistry Letters
Volume8
Issue number5
DOIs
Publication statusPublished - 11 May 2017
Externally publishedYes

Keywords

  • clinical candidate
  • DP receptor antagonist
  • severe asthma

Cite this

Sandham, David A. ; Barker, Lucy ; Brown, Lyndon ; Brown, Zarin ; Budd, David ; Charlton, Steven J ; Chatterjee, Devnandan ; Cox, Brian J ; 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 B ; Turner, Katharine 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. In: A C S Medicinal Chemistry Letters. 2017 ; Vol. 8, No. 5. pp. 582-586.
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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 = "clinical candidate, DP receptor antagonist, severe asthma",
author = "Sandham, {David A.} and Lucy Barker and Lyndon Brown and Zarin Brown and David Budd and Charlton, {Steven J} and Devnandan Chatterjee and Cox, {Brian J} and Gerald Dubois and Nicholas Duggan and Edward Hall and Julia Hatto and Janet Maas and Jodie Manini and Rachael Profit and Darren Riddy and Catherine Ritchie and Bindi Sohal and Duncan Shaw and Rowan Stringer and Sykes, {David A.} and Thomas, {Matthew B} and Turner, {Katharine L.} and Watson, {Simon J.} and Ryan West and Elisabeth Willard and Gareth Williams and Jennifer Willis",
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Sandham, DA, Barker, L, Brown, L, Brown, Z, Budd, D, Charlton, SJ, Chatterjee, D, Cox, BJ, Dubois, G, Duggan, N, Hall, E, Hatto, J, Maas, J, Manini, J, Profit, R, Riddy, D, Ritchie, C, Sohal, B, Shaw, D, Stringer, R, Sykes, DA, Thomas, MB, Turner, KL, Watson, SJ, West, R, Willard, E, Williams, G & Willis, J 2017, 'Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma', A C S Medicinal Chemistry Letters, vol. 8, no. 5, pp. 582-586. https://doi.org/10.1021/acsmedchemlett.7b00157

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, Devnandan; Cox, Brian J; 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 B; Turner, Katharine L.; Watson, Simon J.; West, Ryan; Willard, Elisabeth; Williams, Gareth; Willis, Jennifer.

In: A C S Medicinal Chemistry Letters, Vol. 8, No. 5, 11.05.2017, p. 582-586.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Sandham, David A.

AU - Barker, Lucy

AU - Brown, Lyndon

AU - Brown, Zarin

AU - Budd, David

AU - Charlton, Steven J

AU - Chatterjee, Devnandan

AU - Cox, Brian J

AU - Dubois, Gerald

AU - Duggan, Nicholas

AU - Hall, Edward

AU - Hatto, Julia

AU - Maas, Janet

AU - Manini, Jodie

AU - Profit, Rachael

AU - Riddy, Darren

AU - Ritchie, Catherine

AU - Sohal, Bindi

AU - Shaw, Duncan

AU - Stringer, Rowan

AU - Sykes, David A.

AU - Thomas, Matthew B

AU - Turner, Katharine L.

AU - Watson, Simon J.

AU - West, Ryan

AU - Willard, Elisabeth

AU - Williams, Gareth

AU - Willis, Jennifer

PY - 2017/5/11

Y1 - 2017/5/11

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KW - clinical candidate

KW - DP receptor antagonist

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U2 - 10.1021/acsmedchemlett.7b00157

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JO - A C S Medicinal Chemistry Letters

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