Fazamorexant

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][5][2][3] It is taken by mouth.^[1]

Fazamorexant

Clinical data
Other names	YZJ-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
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 N[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

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

• List of investigational insomnia drugs