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Setipiprant is an investigational oral small molecule drug that acts as a selective antagonist of the prostaglandin D2 receptor 2 (DP2), also known as CRTh2. It was originally developed by Actelion for allergic conditions such as asthma and seasonal allergic rhinitis, and later investigated for androgenetic alopecia (male pattern hair loss). Setipiprant blocks the action of prostaglandin D2 on DP2 receptors found on inflammatory cells (eosinophils, basophils, Th2 lymphocytes), thereby inhibiting downstream inflammatory responses in allergy and potentially counteracting PGD2-mediated inhibition of hair growth in androgenetic alopecia. Clinical trials showed it to be well tolerated but with efficacy similar to existing therapies for allergies; development was discontinued for these indications. Later studies focused on its potential to promote scalp hair growth by antagonizing PGD2 signaling in hair follicles[1][3][7][9].
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