Seltorexant

Experimental anti-insomnia drug From Wikipedia, the free encyclopedia

Seltorexant, also known by its developmental code names MIN-202 and JNJ-42847922, is an orexin antagonist medication which is under development for the treatment of depression, insomnia, and Alzheimer's disease.[4][5][2] It is a selective antagonist of the orexin OX2 receptor (2‑SORA).[2][3][1] The medication is taken orally.[1]

Other namesMIN-202; MIN202; JNJ-42847922; JNJ42847922; JNJ-922; JNJ922
Routes of
administrationOral[1]
Drug classOrexin receptor antagonist; Hypnotic
ATC code
  • None
Quick facts Clinical data, Other names ...
Seltorexant
Clinical data
Other namesMIN-202; MIN202; JNJ-42847922; JNJ42847922; JNJ-922; JNJ922
Routes of
administration		Oral[1]
Drug classOrexin receptor antagonist; Hypnotic
ATC code
  • None
Legal status
Legal status
Pharmacokinetic data
MetabolismCYP3A4[2]
Onset of action0.3–1.5 hours (TmaxTooltip time to peak concentrations)[2][3]
Elimination half-life2–3 hours[2]
Identifiers
  • [5-(4,6-dimethylpyrimidin-2-yl)-hexahydropyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-ylphenyl)methanone
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC21H22FN7O
Molar mass407.453 g·mol−1
3D model (JSmol)
  • c4c(C)nc(nc4C)N5CC2CN(CC2C5)C(=O)c1c(cccc1F)-n3nccn3
  • InChI=1S/C21H22FN7O/c1-13-8-14(2)26-21(25-13)28-11-15-9-27(10-16(15)12-28)20(30)19-17(22)4-3-5-18(19)29-23-6-7-24-29/h3-8,15-16H,9-12H2,1-2H3/t15-,16+
  • Key:SQOCEMCKYDVLMM-IYBDPMFKSA-N
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Side effects

Seltorexant is reported to be safe and well-tolerated.[2][3] Side effects of seltorexant observed in clinical trials so far have included somnolence, fatigue, dizziness, headache, abdominal discomfort, and nightmares.[2]

Pharmacology

Pharmacodynamics

Seltorexant shows over 100-fold greater binding affinity for the OX2 receptor over the OX1 receptor.[3] This is in contrast to other orexin receptor antagonists like suvorexant, lemborexant, and daridorexant, which are all dual orexin receptor antagonists (DORAs).[3][2]

Pharmacokinetics

Seltorexant has fast absorption with a time to peak levels of 0.3 to 1.5 hours and has a relatively short duration with an elimination half-life of only 2 to 3 hours.[2][3] No residual effects of the medication were observed 4 hours after daytime administration.[2] The pharmacokinetics of seltorexant are considered to be ideal for sleep induction.[3] Seltorexant is metabolized by the cytochrome P450 enzyme CYP3A4.[2]

Chemistry

Seltorexant is a small-molecule compound and is structurally related to other clinically used orexin receptor antagonists.[6][2]

Research

As of October 2025, seltorexant is in phase 3 clinical trials for treatment of major depressive disorder (MDD) and phase 2 trials for treatment of insomnia and Alzheimer's disease.[4][5] It was also under investigation for the treatment of sleep apnea, but no recent development has been reported for this indication.[4] Seltorexant is under development by Minerva Neurosciences and Johnson & Johnson's Janssen Pharmaceuticals.[4][5]

Seltorexant is being explored at doses of 5 to 80 mg.[2] In the early clinical trials conducted so far, seltorexant has been found to improve depression scores on the Hamilton Depression Rating Scale in people with MDD and to improve sleep onset, total sleep time, time awake after sleep onset, and sleep efficiency in people with MDD and/or insomnia.[2][3]

See also

References

External links

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