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Description: Setipiprant (ACT-129968 and KYTH-105) is a novel, potent, orally bioavailable and selective CRTH2 antagonist. It has been shown to have greater specificity for DP2 (prostaglandin D2 receptor 2-CRTH2) than for DP1. CRTH2 is a G protein-coupled receptor for PGD2. Setipiprant at multiple oral doses was well tolerated and reduced both the allergen-induced LAR and the associated AHR in allergic asthmatics. CRTH2 may be a promising target for the treatment of allergic disorders.
References: Allergy Asthma Clin Immunol. 2017; 13: 18.
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