SB-649,868

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SB-649,868
SB649868 structure.png
Systematic (IUPAC) name
N-([(2S)-1-([5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl)-2-piperidinyl]methyl)-4-benzofurancarboxamide
Clinical data
Legal status
  • Investigational
Identifiers
ATC code None
PubChem CID 25195495
ChemSpider 25069706
ChEMBL CHEMBL1272307
Chemical data
Formula C26H24FN3O3S 
Mol. 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[edit]

References[edit]

  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". Drug Metab. Dispos. 39 (2): 215–27. doi:10.1124/dmd.110.035386. PMID 21045199. 
  2. ^ "Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.". Aug 2012. PMID 21730017. 
  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. Apr 2012. PMID 22237311. 
  4. ^ "The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia.". Sleep. Aug 2012. PMID 22851805. 

Further reading[edit]