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Orexin Receptor Antagonists and Insomnia
Xin Wu1,2, Tao Xue3, Zhouqing Chen1
1Department of Neurosurgery & Brain, Nerve Research Laboratory, The First Affiliated Hospital of Soochow University, Jiangsu Province, Suzhou, 215006, China.
Current Psychiatry Reports
|August 16, 2022
Summary
Orexin receptor antagonists effectively treat insomnia, with ongoing research focusing on specific drugs for primary and comorbid conditions. Further trials are needed to compare approved and non-approved options and understand orexin system roles.
Area of Science:
- Pharmacology
- Sleep Medicine
- Neuroscience
Background:
- Insomnia is a prevalent sleep disorder affecting millions worldwide.
- The orexin system plays a crucial role in regulating sleep-wake cycles.
- Orexin receptor antagonists (ORAs) represent a novel therapeutic approach for insomnia.
Purpose of the Study:
- To review recent evidence on the efficacy and application of orexin receptor antagonists (ORAs) in treating insomnia.
- To evaluate studies on five dual-acting ORAs and one selective ORA.
- To identify research gaps and future directions in ORA development and application.
Main Methods:
- Comprehensive literature search of recent studies on ORAs for insomnia.
- Evaluation of clinical trials and experimental research on specific ORAs (suvorexant, lemborexant, daridorexant, almorexant, filorexant, seltorexant).
- Analysis of drug efficacy, safety profiles, and target populations (primary vs. comorbid insomnia).
Main Results:
- Suvorexant research increasingly focuses on comorbid insomnia.
- Lemborexant and daridorexant are validated for primary insomnia.
- Almorexant is primarily used in animal studies due to safety concerns; filorexant shows some effects but lacks extensive recent research.
- Seltorexant (selective ORA) has not yet reached Phase 3 trials.
Conclusions:
- ORAs show promise in insomnia treatment, with varying applications for primary and comorbid conditions.
- Further high-quality clinical trials are essential for direct comparison of approved ORAs, investigation of non-approved agents, and understanding ORA use in comorbid insomnia.
- Elucidating the pathophysiology of the orexin signaling system in insomnia is critical for future therapeutic advancements.
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