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

Autor:	Catherine Ritchie, Lucy Barker, Matthew Bm Thomas, Jodie Manini, Elisabeth Willard, Jennifer Willis, Zarin Brown, Edward Charles Hall, Gareth Williams, Ryan West, Steven J. Charlton, David Andrew Sandham, Lyndon Nigel Brown, Simon J. Watson, Janet Maas, Devnandan Chatterjee, David A. Sykes, Nicholas Duggan, Katharine L. Turner, Gerald Dubois, David C. Budd, Bindi Sohal, Rowan Stringer, Rachael Profit, Darren Riddy, Duncan Shaw, Julia Hatto, Brian Cox
Jazyk:	angličtina
Rok vydání:	2017
Předmět:	0301 basic medicine Trifluoromethyl medicine.drug_class Severe asthma Organic Chemistry Fevipiprant Pharmacology Receptor antagonist medicine.disease Biochemistry 03 medical and health sciences Acetic acid chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine 030228 respiratory system chemistry immune system diseases Drug Discovery medicine Potency Receptor Asthma
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e65a3f67567222f76078480d2373e99e https://europepmc.org/articles/PMC5430394/ Zobrazit plný text záznamu