Vornorexant

Overview

Vornorexant, sold under the brand name Vorzzz, is an orexin receptor antagonist which is used in the treatment of insomnia in Japan. It is taken orally. The drug is available for insomnia in the form of 2.5, 5, and 10 mg oral tablets. It has been found to improve sleep onset, sleep maintenance, and daytime functioning with both short-term and long-term use.[1–7] WP

Side effects of vornorexant include somnolence among others. It does not appear to impair next-day functioning or driving performance, which suggests that it causes minimal next-day or residual effects. The drug also does not appear to cause dependence, withdrawal, rebound insomnia, or suicidality. Vornorexant acts as a dual orexin OX₁ and OX₂ receptor antagonist (DORA). It has a time to peak of 2.5 hours and a relatively short elimination half-life of 1.3 to 3.3 hours. Vornorexant was designed to have a short half-life and duration in order to reduce next-day side effects like somnolence.[3][4][6–9] WP

Vornorexant was first described in the scientific literature by 2020. It was developed by Taisho Pharmaceutical in Japan. The drug was approved for the treatment of insomnia in Japan in August 2025. It was also under development for the treatment of sleep apnea syndrome, but no recent development for this indication has been reported. Vornorexant is not a controlled substance in Japan.[1][3][4][8] WP

Drug class

Orexin receptor antagonist Orexin OX1 and OX2 receptor antagonist Hypnotic WP

From the Wikipedia article's infobox.

Chemistry

Formula

C23H22FN7O2 PC

CAS number

2265899-49-6 PC

Molar mass (g/mol)

447.5 PC

IUPAC name (computed by PubChem)

[(2S)-2-[[3-(5-fluoro-2-pyridinyl)pyrazol-1-yl]methyl]-1,3-oxazinan-3-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone PC

SMILES

CC1=CC(=C(C=C1)N2N=CC=N2)C(=O)N3CCCO[C@H]3CN4C=CC(=N4)C5=NC=C(C=C5)F PC

InChIKey

AEZZJXJIJFSUEM-QFIPXVFZSA-N PC

PubChem CID

137419776

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 TS 142 - AdisInsight
2. Journal / agency Chino Y, Sugiyama H, Chaki S, Sato Y. Current and novel dual orexin receptor antagonists for the treatment of insomnia: the emergence of vornorexant. Int J Neuropsychopharmacol. December 2025. doi:10.1093/ijnp/pyaf077 · PMID 41273062 · PMC13223731
3. Journal / agency Yokota H, Chino Y, Shibayama K, Chaki S, Imadera Y. The preclinical profiles and the clinical efficacy and safety of vornorexant (Vorzzz® tablets), a new orexin receptor antagonist. Nihon Yakurigaku Zasshi. 2026. doi:10.1254/fpj.25096 · PMID 42091480
4. Other 医療用医薬品: ボルズィ (ボルズィ錠2.5mg 他). 17 June 2026
5. 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 Opinion on Drug Metabolism & Toxicology. November 2020. doi:10.1080/17425255.2020.1817380 · PMID 32901578
6. Journal / agency Jacobson LH, Hoyer D, de Lecea L. Hypocretins (orexins): The ultimate translational neuropeptides. Journal of Internal Medicine. May 2022. doi:10.1111/joim.13406 · PMID 35043499
7. Journal / agency Uchiyama M, Kambe D, Imadera Y, Kajiyama Y, Ogo H, Uchimura N. Effects of TS-142, a novel dual orexin receptor antagonist, on sleep in patients with insomnia: a randomized, double-blind, placebo-controlled phase 2 study. Psychopharmacology. July 2022. doi:10.1007/s00213-022-06089-6 · PMID 35296912 · PMC9205809
8. Journal / agency Futamura A, Suzuki R, Tamura Y, Kawamoto H, Ohmichi M, Hino N, Tokumaru Y, Kirinuki S, Hiyoshi T, Aoki T, Kambe D, Nozawa D. Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia. Bioorganic & Medicinal Chemistry. July 2020. doi:10.1016/j.bmc.2020.115489 · PMID 32482533
9. Journal / agency Uchiyama M, Kambe D, Imadera Y, Sunaga H, Hasegawa S, Nogi T, Kajiyama Y, Yoshida S, Ogo H, Uchimura N. 0146 Efficacy and Safety of Single Dose of TS-142, a Novel and Potent Dual Orexin Receptor Antagonist, in Insomnia Patients. Sleep. April 2020. doi:10.1093/sleep/zsaa056.144

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