Vornorexant

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Vornorexant
Vornorexant skeletal.svg
Clinical data
Other namesORN-0829; TS-142
Drug classOrexin antagonist
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 (developmental code names ORN-0829, TS-142) is an orexin receptor antagonist which is under development for the treatment of insomnia and sleep apnea syndrome.[1][2][3] It is a dual orexin OX1 and OX2 receptor antagonist (DORA).[1][3] Vornorexant is predicted to have a short elimination half-life in humans,[3] but few clinical data are available so far.[2] As of June 2021, vornorexant is in phase 2 clinical trials for insomnia and phase 1 trials for sleep apnea syndrome.[1]

See also[]

  • List of investigational sleep drugs § Orexin receptor antagonists

References[]

  1. ^ a b c "TS 142 - AdisInsight".
  2. ^ a b 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.
  3. ^ a b c 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.

External links[]



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