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Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia

Anthony J Roecker1, Christopher D Cox1, Paul J Coleman1

  • 1Department of Medicinal Chemistry, Merck Research Laboratories , P.O. Box 4, 770 Sumneytown Pike, WP14-2, West Point, Pennsylvania 19486, United States.

Journal of Medicinal Chemistry
|August 29, 2015
PubMed

Insights

The orexin system regulates sleep and wakefulness. Orexin antagonists were developed to treat insomnia, leading to the FDA approval of suvorexant for sleep disorders.

Area of Science:

  • Neuroscience
  • Pharmacology

Background:

  • The orexin system, comprising orexin receptors 1 and 2 and neuropeptides A and B, was discovered in 1998.
  • Genetic studies linked orexin system dysfunction to narcolepsy, a sleep disorder.

Purpose of the Study:

  • To explore the discovery and development of orexin antagonists.
  • To identify potential therapeutic agents for sleep/wake disorders, anxiety, and obesity.

Main Methods:

  • Focus on the discovery and development of structurally diverse orexin antagonists.
  • Preclinical pharmacology studies and human clinical trials were conducted.

Main Results:

  • Development of dual orexin receptor antagonists.
  • Successful preclinical and clinical evaluation of orexin antagonists.

Conclusions:

  • The development of orexin antagonists offers a therapeutic strategy for insomnia.
  • Suvorexant, a dual orexin receptor antagonist, was approved by the FDA in 2014 for insomnia treatment.

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