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Fevipiprant is a DP2/CRTH2 antagonist (Ki = 1.05 nM).1 It reduces shape change of eosinophils induced by prostaglandin D2 (PGD2; Item No. 12010) with IC50 values of 0.4 and 0.44 nM for isolated human eosinophils and human whole blood, respectively. Fevipiprant inhibits PGD2-induced release of IL-5 and IL-13 in isolated human CD4+ Th2 cells (IC50s = 2.56 and 1.4 nM, respectively). It reduces the number of eosinophils in bronchoalveolar lavage fluid (BALF) in a mouse model of asthma (ED50 = ~1 mg/kg).2
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1. Fevipiprant (QAW039), a slowly dissociating CRTh2 antagonist with the potential for improved clinical efficacy. Mol. Pharmacol. 89(5), 593-605 (2016).
2. Fevipiprant, a potent selective prostaglandin D2 receptor 2 (DP2) antagonist, dose-