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Clinical data
ATC code
  • None
Legal status
Legal status
  • Investigational
PubChem CID
CompTox Dashboard (EPA)
Chemical and physical data
Molar mass477.549 g/mol (free base) g·mol−1
3D model (JSmol)

SB-649868 is a dual orexin receptor antagonist in development by GlaxoSmithKline.[1] The drug is currently[when?] 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


  1. ^ 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. doi:10.1124/dmd.110.035386. PMID 21045199.
  2. ^ 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. doi:10.1177/0269881111408954. PMID 21730017.
  3. ^ 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. doi:10.1038/npp.2011.310. PMC 3306884. PMID 22237311.
  4. ^ 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. doi:10.5665/sleep.1996. PMC 3397789. PMID 22851805.

Further reading