Vornorexant
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| Clinical data | |
|---|---|
| Other names | ORN-0829; TS-142 |
| Routes of administration | By mouth[1] |
| Drug class | Orexin antagonist |
| Pharmacokinetic data | |
| Elimination half-life | 1.3–3.3 hours[1][2] |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
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| Chemical and physical data | |
| Formula | C23H22FN7O2 |
| Molar mass | 447.474 g·mol−1 |
| 3D model (JSmol) | |
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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
[edit]- Seltorexant – another investigational short-acting orexin receptor antagonist
- List of investigational sleep drugs § Orexin receptor antagonists
References
[edit]- ^ a b c d 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.
- ^ a b 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.
- ^ a b c "TS 142 - AdisInsight".
- ^ 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.
- ^ a b c 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.
- ^ 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.
External links
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