Systematic (IUPAC) name
Clinical data
Legal status
  • Investigational
ATC code None
PubChem CID:
Chemical data
Formula C26H24FN3O3S
Molecular mass 477.549 g/mol (free base)

SB-649,868 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


  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.  
  2. ^ "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. Aug 2012.  
  3. ^ "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. Apr 2012.  
  4. ^ "The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia.". Sleep 35: 1097–104. Aug 2012.  

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.