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SB-649868 is a dual orexin receptor antagonist that was being developed by GlaxoSmithKline as a treatment for insomnia.[1]
A phase I clinical trial 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 phase II study added a 60 mg dose and observed dose-dependent sleep promotion.[4]
The compound no longer appears to be under active development, with the last study posted to ClinicalTrials.gov completed in 2010.
See also
References
- ^ Renzulli C, Nash M, Wright M, Thomas S, Zamuner S, Pellegatti M, et al. (February 2011). "Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans". Drug Metabolism and Disposition. 39 (2): 215–27. doi:10.1124/dmd.110.035386. PMID 21045199. S2CID 1995624.
- ^ Bettica P, Nucci G, Pyke C, Squassante L, Zamuner S, Ratti E, et al. (August 2012). "Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist". Journal of Psychopharmacology. 26 (8): 1058–70. doi:10.1177/0269881111408954. PMID 21730017. S2CID 29578953.
- ^ Bettica P, Squassante L, Groeger JA, Gennery B, Winsky-Sommerer R, Dijk DJ (April 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 (5): 1224–33. doi:10.1038/npp.2011.310. PMC 3306884. PMID 22237311.
- ^ Bettica P, Squassante L, Zamuner S, Nucci G, Danker-Hopfe H, Ratti E (August 2012). "The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia". Sleep. 35 (8): 1097–104. doi:10.5665/sleep.1996. PMC 3397789. PMID 22851805.
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". Annual Review of Pharmacology and Toxicology. 51: 243–66. doi:10.1146/annurev-pharmtox-010510-100528. PMC 3058259. PMID 21034217.
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