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Fazamorexant

Topic: Chemistry

 From HandWiki - Reading time: 6 min

Fazamorexant (INN; developmental code name YZJ-1139) is an orexin receptor antagonist which is under development for the treatment of insomnia.[1][2][3][4] It is taken by mouth.[1]

The drug acts as a dual orexin receptor antagonist (DORA), or as an antagonist of both the orexin OX1 and OX2 receptors.[3][4] Its time to peak levels is 0.6 to 1.3 hours and its elimination half-life is 1.9 to 3.7 hours.[5]

Fazamorexant is under development by Jiangsu Yangtze River Pharmaceutical Group and/or Shanghai Haiyan Pharmaceutical Technology in China.[1][2][3] As of September 2022, it is in phase 3 clinical trials for insomnia.[1][2][4] Relatively little public information is available on fazamorexant.[3] This was such that it had to be excluded from a 2020 literature review of orexin receptor antagonists for insomnia.[3]

See also

  • List of investigational insomnia drugs

References

  1. ↑ 1.0 1.1 1.2 1.3 "YZJ 1139". 14 September 2022. https://adisinsight.springer.com/drugs/800070010. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on Fazamorexant with Synapse". 31 October 2024. https://synapse.patsnap.com/drug/c7fe97b9b5a74ad29ac29df5588f38be. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders". Expert Opinion on Drug Metabolism & Toxicology 16 (11): 1063–1078. November 2020. doi:10.1080/17425255.2020.1817380. PMID 32901578. 
  4. ↑ 4.0 4.1 4.2 "Use of experimental medicine approaches for the development of novel psychiatric treatments based on orexin receptor modulation". Neuroscience and Biobehavioral Reviews 147. April 2023. doi:10.1016/j.neubiorev.2023.105107. PMID 36828161. 
  5. ↑ "Pharmacokinetics, Pharmacodynamic, Safety and Tolerability of Fazamorexant, a Novel Dual Orexin Receptor Antagonist: Report of the First-in-Human Study". Drug Design, Development and Therapy 19: 5271–5282. 19 June 2025. doi:10.2147/DDDT.S501111. PMID 40552089. 



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