Fazamorexant

Last updated

Fazamorexant
Fazamorexant.svg
Clinical data
Other namesYZJ-1139; YZJ1139
Routes of
administration 		Oral [1]
Drug class Orexin receptor antagonist [1] [2] [3]
Pharmacokinetic data
Elimination half-life 1.9–3.7 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
Formula C25H25FN4O2
Molar mass 432.499 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 (INN Tooltip International Nonproprietary Name; developmental code name YZJ-1139) is an orexin receptor antagonist which is under development for the treatment of insomnia. [1] [5] [2] [3] 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. [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 is under development by Jiangsu Yangtze River Pharmaceutical Group and/or Shanghai Haiyan Pharmaceutical Technology in China. [1] [5] [2] As of September 2022, it is in phase 3 clinical trials for insomnia. [1] [5] [3] 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]

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 4 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 . PMID   40552089.
  5. 1 2 3 "Delving into the Latest Updates on Fazamorexant with Synapse". Synapse. 31 October 2024. Retrieved 31 October 2024.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.