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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2025, Vol. 30 ›› Issue (11): 1491-1499.doi: 10.12092/j.issn.1009-2501.2025.11.005

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Daridorexant: from discovery to clinical application

WANG Zan, WANG Ruiqi, SUN Qingqing, ZHANG Yanan   

  1. Sleep Center, Department of Neurology, The First Hospital of Jilin University, Changchun 130021, Jilin, China
  • Online:2025-11-26 Published:2025-12-04

Abstract:

Insomnia is a common sleep-wake disorder characterized by difficulty in falling asleep or maintaining sleep, accompanied by daytime dysfunction, which severely affects patients' physical and mental health, quality of life, and social functioning. Traditional first-line medications for insomnia, such as benzodiazepines, have limited utility due to their side effects, including addiction, drug tolerance, and daytime functional impairment. Central nervous system hyperarousal is one of the core pathophysiological mechanisms of insomnia. The orexin system has garnered significant attention for its key role in regulating and maintaining wakefulness, and suppressing arousal has emerged as a novel therapeutic strategy for insomnia. Daridorexant, as a new dual orexin receptor antagonist, significantly improves nighttime sleep and daytime function without altering sleep architecture by simultaneously blocking orexin type 1 and type 2 receptors, and it exhibits a favorable safety profile. Currently, daridorexant has been approved for marketing in China. This article reviews the research journey of daridorexant, covering aspects from drug discovery, pharmacological properties, and clinical development to its safety, efficacy, and clinical application, thereby providing evidence for the use of this novel anti-insomnia agent.

Key words: insomnia, dual orexin receptor antagonist, daridorexant, safety, daytime function

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