SB-649868
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| Formula | C26H24FN3O3S |
| Molar mass | 477.549 g/mol (free base) |
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SB-649868 is a dual orexin receptor antagonist in development by GlaxoSmithKline.[1] The drug is currently in phase II development for insomnia.
A phase I study evaluated doses up to 80 mg, resulting in significant improvement in sleep latency without adverse effects.[2]
In randomized, double-blind, placebo-controlled crossover trials, the 10 and 30 mg doses increased sleep time and reduced sleep latency.[3] The subsequent study added a 60 mg dose and observed dose-dependent sleep promotion.[4]
See also
References
- ↑ Renzulli C; Nash M; Wright M; Thomas S; Zamuner S; Pellegatti M; Bettica P; Boyle G (February 2011). "Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans" (PDF). Drug Metab. Dispos. 39 (2): 215–27. PMID 21045199. doi:10.1124/dmd.110.035386.
- ↑ Bettica, P; Nucci, G; Pyke, C; et al. (Aug 2012). "Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.". Journal of Psychopharmacology. 26: 1058–1070. PMID 21730017. doi:10.1177/0269881111408954.
- ↑ Bettica, P; Squassante, L; Groeger, JA; Gennery, B; Winsky-Sommerer, R; Dijk, DJ (Apr 2012). "Differential effects of a dual orexin receptor antagonist (SB-649868) and zolpidem on sleep initiation and consolidation, SWS, REM sleep, and EEG power spectra in a model of situational insomnia.". Neuropsychopharmacology. 37: 1224–33. PMC 3306884
. PMID 22237311. doi:10.1038/npp.2011.310. - ↑ Bettica, P; Squassante, L; Zamuner, S; Nucci, G; Danker-Hopfe, H; Ratti, E (Aug 2012). "The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia.". Sleep. 35: 1097–104. PMC 3397789 . PMID 22851805. doi:10.5665/sleep.1996.
Further reading
- Ratti E (December 13, 2007). "Psychiatry: An Innovative Drug Discovery Pipeline" (PDF) (GSK Neurosciences seminar). Archived from the original on December 5, 2008.
- Scammell TE; Winrow CJ (February 2011). "Orexin receptors: pharmacology and therapeutic opportunities". Annu. Rev. Pharmacol. Toxicol. 51: 243–66. PMC 3058259 . PMID 21034217. doi:10.1146/annurev-pharmtox-010510-100528.
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