Seltorexant

Overview

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. It is a selective antagonist of the orexin OX₂ receptor (2‑SORA). The medication is taken orally.[1–5] WP

Drug class

Orexin receptor antagonist Hypnotic WP

From the Wikipedia article's infobox.

Risks and side effects

Side effects

Seltorexant is reported to be safe and well-tolerated. Side effects of seltorexant observed in clinical trials so far have included somnolence, fatigue, dizziness, headache, abdominal discomfort, and nightmares.[3][4] WP

Pharmacology

Pharmacodynamics

Seltorexant shows over 100-fold greater binding affinity for the OX₂ receptor over the OX₁ receptor. This is in contrast to other orexin receptor antagonists like suvorexant, lemborexant, and daridorexant, which are all dual orexin receptor antagonists (DORAs).[3][4] WP

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. No residual effects of the medication were observed 4 hours after daytime administration. The pharmacokinetics of seltorexant are considered to be ideal for sleep induction. Seltorexant is metabolized by the cytochrome P450 enzyme CYP3A4.[3][4] WP

Research

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. It was also under investigation for the treatment of sleep apnea, but no recent development has been reported for this indication. Seltorexant is under development by Minerva Neurosciences and Johnson & Johnson's Janssen Pharmaceuticals.[1][2] WP

Seltorexant is being explored at doses of 5 to 80 mg. 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.[3][4] WP

Chemistry

Formula

C21H22FN7O PC

CAS number

1293281-49-8 PC

Molar mass (g/mol)

407.4 PC

IUPAC name (computed by PubChem)

[2-(4,6-dimethylpyrimidin-2-yl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-[2-fluoro-6-(triazol-2-yl)phenyl]methanone PC

SMILES

CC1=CC(=NC(=N1)N2CC3CN(CC3C2)C(=O)C4=C(C=CC=C4F)N5N=CC=N5)C PC

InChIKey

SQOCEMCKYDVLMM-UHFFFAOYSA-N PC

PubChem CID

67116280

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Seltorexant - Janssen Research & Development/Minerva Neurosciences. 2022-02-28
2. Other Delving into the Latest Updates on Seltorexant with Synapse. 6 September 2025
3. Journal / agency Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J. Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders. Expert Opin Drug Metab Toxicol. November 2020. doi:10.1080/17425255.2020.1817380 · PMID 32901578
4. Journal / agency Jacobson LH, Hoyer D, de Lecea L. Hypocretins (orexins): The ultimate translational neuropeptides. J Intern Med. January 2022. doi:10.1111/joim.13406 · PMID 35043499
5. Journal / agency Sun Y, Tisdale RK, Kilduff TS. Hypocretin/Orexin Receptor Pharmacology and Sleep Phases. Front Neurol Neurosci. 2021. doi:10.1159/000514963 · PMID 34052813 · PMC8171809

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.