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2017 ; 8
(5
): 582-586
Nephropedia Template TP
gab.com Text
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English Wikipedia
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP(2) Receptor
Antagonist for Treatment of Asthma
#MMPMID28523115
Sandham DA
; Barker L
; Brown L
; Brown Z
; Budd D
; Charlton SJ
; Chatterjee D
; Cox B
; 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 M
; Turner KL
; Watson SJ
; West R
; Willard E
; Williams G
; Willis J
ACS Med Chem Lett
2017[May]; 8
(5
): 582-586
PMID28523115
show ga
Further optimization of an initial DP(2) 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.