Chemistry:Vornorexant

From HandWiki
Short description: Chemical compound
Vornorexant
Vornorexant skeletal.svg
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
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC23H22FN7O2
Molar mass447.474 g·mol−1
3D model (JSmol)

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 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. 1.0 1.1 1.2 1.3 "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. July 2022. doi:10.1007/s00213-022-06089-6. PMID 35296912. 
  2. 2.0 2.1 "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. April 2020. doi:10.1093/sleep/zsaa056.144. ISSN 0161-8105. 
  3. 3.0 3.1 3.2 "TS 142 - AdisInsight". https://adisinsight.springer.com/drugs/800049420. 
  4. "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. November 2020. doi:10.1080/17425255.2020.1817380. PMID 32901578. 
  5. 5.0 5.1 5.2 "Hypocretins (orexins): The ultimate translational neuropeptides". Journal of Internal Medicine 291 (5): 533–556. May 2022. doi:10.1111/joim.13406. PMID 35043499. 
  6. "Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia". Bioorganic & Medicinal Chemistry 28 (13): 115489. July 2020. doi:10.1016/j.bmc.2020.115489. PMID 32482533. 

External links