Fazamorexant

Fazamorexant
Clinical data
Trade namesMengping
Other namesHY-901139; HY901139; YZJ-1139; YZJ1139
Routes of
administration		Oral[1]
Drug classOrexin receptor antagonist[1][2][3]
Legal status
Legal status
  • Rx in China, investigational in general
Pharmacokinetic data
Elimination half-life1.9–3.7 hours[4]
Identifiers
  • [(1S,2R,5S)-2-[(5-fluoropyridin-2-yl)oxymethyl]-8-azabicyclo[3.2.1]octan-8-yl]-(5-methyl-2-pyrimidin-2-ylphenyl)methanone
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC25H25FN4O2
Molar mass432.499 g·mol−1
3D model (JSmol)
  • CC1=CC(=C(C=C1)C2=NC=CC=N2)C(=O)N3[C@H]4CC[C@H]([C@@H]3CC4)COC5=NC=C(C=C5)F
  • InChI=1S/C25H25FN4O2/c1-16-3-8-20(24-27-11-2-12-28-24)21(13-16)25(31)30-19-6-4-17(22(30)9-7-19)15-32-23-10-5-18(26)14-29-23/h2-3,5,8,10-14,17,19,22H,4,6-7,9,15H2,1H3/t17-,19-,22-/m0/s1
  • Key:PMJPLAGTPPVSRL-JLMWRMLUSA-N

Fazamorexant (INNTooltip International Nonproprietary Name), sold under the brand name Mengping, is an orexin receptor antagonist which is used in the treatment of insomnia in China.[1][5][2][3] It is taken orally.[1]

The drug acts as a dual orexin receptor antagonist (DORA), or as an antagonist of both the orexin OX1 and OX2 receptors.[2][3] Its time to peak levels is 0.6 to 1.3 hours and its elimination half-life is 1.9 to 3.7 hours.[4]

Fazamorexant was developed by Jiangsu Yangtze River Pharmaceutical Group and/or Shanghai Haiyan Pharmaceutical Technology in China.[1][5][2] Relatively little public information is available on fazamorexant.[2] This was such that it had to be excluded from a 2020 literature review of orexin receptor antagonists for insomnia.[2] The drug was approved in China in May 2026.[1][6]

See also

References

  1. 1 2 3 4 5 6 "YZJ 1139". AdisInsight. 14 September 2022. Retrieved 31 October 2024.
  2. 1 2 3 4 5 6 Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J (November 2020). "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. doi:10.1080/17425255.2020.1817380. PMID 32901578.
  3. 1 2 3 Beckenstrom AC, Coloma PM, Dawson GR, Finlayson AK, Malik A, Post A, et al. (April 2023). "Use of experimental medicine approaches for the development of novel psychiatric treatments based on orexin receptor modulation". Neuroscience and Biobehavioral Reviews. 147 105107. doi:10.1016/j.neubiorev.2023.105107. PMC 10165155. PMID 36828161.
  4. 1 2 Ni J, Jin L, Zhao D, Zhang W, Li B, Huang X, et al. (19 June 2025). "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. doi:10.2147/DDDT.S501111. PMC 12184692. PMID 40552089.
  5. 1 2 "Delving into the Latest Updates on Fazamorexant with Synapse". Synapse. 31 October 2024. Retrieved 31 October 2024.
  6. ↑ "国家药监局批准法赞雷生片上市". nmpa.gov.cn (in Chinese). 21 May 2026. Retrieved 3 June 2026.
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