Vornorexant

Vornorexant
Clinical data
Trade namesVorzzz
Other namesORN-0829; ORN0829; TS-142; TS142
Routes of
administration		Oral[1]
Drug classOrexin receptor antagonist; Orexin OX1 and OX2 receptor antagonist; Hypnotic
ATC code
  • None
Pharmacokinetic data
Protein binding94.5–96.3%[2]
MetabolismCYP3A4[2]
Elimination half-life1.3–3.3 hours[1][3][2]
Identifiers
  • [(2S)-2-[[3-(5-fluoropyridin-2-yl)pyrazol-1-yl]methyl]-1,3-oxazinan-3-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC23H22FN7O2
Molar mass447.474 g·mol−1
3D model (JSmol)
  • CC1=CC(=C(C=C1)N2N=CC=N2)C(=O)N3CCCO[C@H]3CN4C=CC(=N4)C5=NC=C(C=C5)F
  • InChI=1S/C23H22FN7O2/c1-16-3-6-21(31-26-8-9-27-31)18(13-16)23(32)30-10-2-12-33-22(30)15-29-11-7-20(28-29)19-5-4-17(24)14-25-19/h3-9,11,13-14,22H,2,10,12,15H2,1H3/t22-/m0/s1
  • Key:AEZZJXJIJFSUEM-QFIPXVFZSA-N

Vornorexant, sold under the brand name Vorzzz, is an orexin receptor antagonist which is used in the treatment of insomnia in Japan.[4][5][6][2][7][8] It is taken orally.[4][1] The drug is available for insomnia in the form of 2.5, 5, and 10 mg oral tablets.[6][2] It has been found to improve sleep onset, sleep maintenance, and daytime functioning with both short-term and long-term use.[6][2]

Side effects of vornorexant include somnolence among others.[6][2] It does not appear to impair next-day functioning or driving performance, which suggests that it causes minimal next-day or residual effects.[6][2] The drug also does not appear to cause dependence, withdrawal, rebound insomnia, or suicidality.[6][2] Vornorexant acts as a dual orexin OX1 and OX2 receptor antagonist (DORA).[8][9] It has a time to peak of 2.5 hours and a relatively short elimination half-life of 1.3 to 3.3 hours.[1][3] Vornorexant was designed to have a short half-life and duration in order to reduce next-day side effects like somnolence.[8][6]

Vornorexant was first described in the scientific literature by 2020.[9] It was developed by Taisho Pharmaceutical in Japan.[4] The drug was approved for the treatment of insomnia in Japan in August 2025.[4][6][2] It was also under development for the treatment of sleep apnea syndrome, but no recent development for this indication has been reported.[4] Vornorexant is not a controlled substance in Japan.[2]

Vornorexant (Vorzzz) blister pack sold in Japan.

See also

References

  1. 1 2 3 4 Uchiyama M, Kambe D, Imadera Y, Kajiyama Y, Ogo H, Uchimura N (July 2022). "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. 239 (7): 2143–2154. doi:10.1007/s00213-022-06089-6. PMC 9205809. PMID 35296912.
  2. 1 2 3 4 5 6 7 8 9 10 11 "医療用医薬品 : ボルズィ (ボルズィ錠2.5mg 他)". KEGG (in Japanese). 17 June 2026. Retrieved 25 June 2026.
  3. 1 2 Uchiyama M, Kambe D, Imadera Y, Sunaga H, Hasegawa S, Nogi T, Kajiyama Y, Yoshida S, Ogo H, Uchimura N (April 2020). "0146 Efficacy and Safety of Single Dose of TS-142, a Novel and Potent Dual Orexin Receptor Antagonist, in Insomnia Patients". Sleep. 43 (Supplement 1): A58. doi:10.1093/sleep/zsaa056.144. eISSN 1550-9109. ISSN 0161-8105.
  4. 1 2 3 4 5 "TS 142 - AdisInsight".
  5. ↑ Chino Y, Sugiyama H, Chaki S, Sato Y (December 2025). "Current and novel dual orexin receptor antagonists for the treatment of insomnia: the emergence of vornorexant". Int J Neuropsychopharmacol. 28 (12). doi:10.1093/ijnp/pyaf077. PMC 13223731. PMID 41273062.
  6. 1 2 3 4 5 6 7 8 Yokota H, Chino Y, Shibayama K, Chaki S, Imadera Y (2026). "[The preclinical profiles and the clinical efficacy and safety of vornorexant (Vorzzz® tablets), a new orexin receptor antagonist]". Nihon Yakurigaku Zasshi (in Japanese). 161 (3): 192–197. doi:10.1254/fpj.25096. PMID 42091480.
  7. ↑ 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. S2CID 221572078.
  8. 1 2 3 Jacobson LH, Hoyer D, de Lecea L (May 2022). "Hypocretins (orexins): The ultimate translational neuropeptides". Journal of Internal Medicine. 291 (5): 533–556. doi:10.1111/joim.13406. PMID 35043499. S2CID 248119793.
  9. 1 2 Futamura A, Suzuki R, Tamura Y, Kawamoto H, Ohmichi M, Hino N, et al. (July 2020). "Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia". Bioorganic & Medicinal Chemistry. 28 (13) 115489. doi:10.1016/j.bmc.2020.115489. PMID 32482533. S2CID 216517776.
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