2017
DOI: 10.1021/acsmedchemlett.7b00353
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Correction to “Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma”

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“…Fevipiprant is a potent and selective DP2 antagonist that has shown therapeutic benefit in certain subsets of asthma patients in phase 2 clinical trials (1517). In a mechanistic phase 2 clinical trial study in patients with persistent eosinophilic asthma, fevipiprant not only reduced airway inflammation but also improved epithelial integrity and reduced airway smooth muscle (ASM) mass (16,17). In two recently published phase 3 studies, although neither trial showed a statistically significant reduction in asthma exacerbations, consistent and modest reductions in exacerbation rates were observed with a high dose of fevipiprant in both studies (18).…”
mentioning
confidence: 99%
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“…Fevipiprant is a potent and selective DP2 antagonist that has shown therapeutic benefit in certain subsets of asthma patients in phase 2 clinical trials (1517). In a mechanistic phase 2 clinical trial study in patients with persistent eosinophilic asthma, fevipiprant not only reduced airway inflammation but also improved epithelial integrity and reduced airway smooth muscle (ASM) mass (16,17). In two recently published phase 3 studies, although neither trial showed a statistically significant reduction in asthma exacerbations, consistent and modest reductions in exacerbation rates were observed with a high dose of fevipiprant in both studies (18).…”
mentioning
confidence: 99%
“…An x-ray crystallographic study illustrated how fevipiprant competitively occupies a semioccluded ligand-binding pocket in DP2 to block the function of the receptor (19). Previous in vitro studies demonstrated the anti-inflammatory effect of fevipiprant in DP2-mediated reactions in Th2 and ILC2 cells (17,20,21). The effects of DP2 antagonism in Tc2 cells are not fully understood.…”
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confidence: 99%