Vornorexant

Vornorexant, also known by its developmental code names ORN-0829 and TS-142, is an orexin antagonist medication which is under development for the treatment of insomnia and sleep apnea.[3][4][5] It is a dual orexin OX1 and OX2 receptor antagonist (DORA).[5][6] The medication is taken by mouth.[1] As of June 2021, vornorexant is in phase 2 clinical trials for insomnia and phase 1 trials for sleep apnea.[3] It is under development by Taisho Pharmaceutical.[3]

Vornorexant
Clinical data
Other namesORN-0829; TS-142
Routes of
administration		By mouth[1]
Drug classOrexin antagonist
Pharmacokinetic data
Elimination half-life1.3–3.3 hours[1][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
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 has a time to peak of 2.5 hours and a relatively short elimination half-life of 1.3 to 3.3 hours.[1][2] It was designed to have a short half-life and duration in order to reduce next-day side effects like somnolence.[5]

See also

References
  1. Uchiyama M, Kambe D, Imadera Y, Kajiyama Y, Ogo H, Uchimura N (March 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 (Berl). doi:10.1007/s00213-022-06089-6. PMID 35296912.
  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–A58. doi:10.1093/sleep/zsaa056.144. eISSN 1550-9109. ISSN 0161-8105.
  3. "TS 142 - AdisInsight".
  4. 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 Opin Drug Metab Toxicol. 16 (11): 1063–1078. doi:10.1080/17425255.2020.1817380. PMID 32901578. S2CID 221572078.
  5. Jacobson LH, Hoyer D, de Lecea L (January 2022). "Hypocretins (orexins): The ultimate translational neuropeptides". J Intern Med. doi:10.1111/joim.13406. PMID 35043499.
  6. Futamura A, Suzuki R, Tamura Y, Kawamoto H, Ohmichi M, Hino N, Tokumaru Y, Kirinuki S, Hiyoshi T, Aoki T, Kambe D, Nozawa D (July 2020). "Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia". Bioorg Med Chem. 28 (13): 115489. doi:10.1016/j.bmc.2020.115489. PMID 32482533. S2CID 216517776.



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