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

ACS Medicinal Chemistry Letters
David A SandhamJennifer Willis

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.

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Citations

Nov 1, 2018·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·Revital ShamriFrancesca Levi-Schaffer
Oct 23, 2019·Signal Transduction and Targeted Therapy·Seyyed Shamsadin Athari
Nov 27, 2019·Pharmacological Reviews·Stacy Gelhaus WendellCheng Zhang
Oct 1, 2018·Respiratory Research·Christian DomingoPablo Altman
Sep 21, 2019·Combinatorial Chemistry & High Throughput Screening·Abdul R IssahakuMahmoud E S Soliman
Nov 5, 2019·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Corrado PelaiaGirolamo Pelaia
Oct 18, 2020·Signal Transduction and Targeted Therapy·Seyyed Shamsadin Athari
Apr 8, 2021·Pulmonary Pharmacology & Therapeutics·Chris BrightlingPablo Altman
May 21, 2021·The Journal of Immunology : Official Journal of the American Association of Immunologists·Wentao ChenLuzheng Xue
Jul 15, 2021·Nature Reviews. Drug Discovery·Jian Payandeh, Matthew Volgraf
Aug 3, 2021·Frontiers in Physiology·Bohae Rachel LeeNeelam Sharma-Walia

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