Fazamorexant

Fazamorexant
Clinical data
Other names	YZJ-1139; YZJ1139
Routes of; administration	Oral
Drug class	Orexin receptor antagonist
Identifiers
	IUPAC name [(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	1808918-69-5 [GSRS];
PubChem CID	156889652;
ChemSpider	128922072;
UNII	MDH4D7M594;
ChEMBL	ChEMBL5314459;
Chemical and physical data
Formula	C25H25FN4O2
Molar mass	432.499 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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; developmental code name YZJ-1139) is an orexin receptor antagonist which is under development for the treatment of insomnia.^[1]^[4]^[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]

Fazamorexant is under development by Jiangsu Yangtze River Pharmaceutical Group and/or Shanghai Haiyan Pharmaceutical Technology in China.^[1]^[4]^[2] As of September 2022, it is in phase 3 clinical trials for insomnia.^[1]^[4]^[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]

References

^ ^a ^b ^c ^d ^e ^f "YZJ 1139". AdisInsight. 14 September 2022. Retrieved 31 October 2024.
^ ^a ^b ^c ^d ^e ^f 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.
^ ^a ^b ^c ^d 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.
^ ^a ^b ^c "Delving into the Latest Updates on Fazamorexant with Synapse". Synapse. 31 October 2024. Retrieved 31 October 2024.

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[AdisInsight-1] ^ ^a ^b ^c ^d ^e ^f "YZJ 1139". AdisInsight. 14 September 2022. Retrieved 31 October 2024.

[MuehlanVaillantZenklusen2020-2] ^ ^a ^b ^c ^d ^e ^f 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.

[BeckenstromColomaDawson2023-3] 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.

[Synapse-4] "Delving into the Latest Updates on Fazamorexant with Synapse". Synapse. 31 October 2024. Retrieved 31 October 2024.

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