SB-649868: Difference between revisions

SB-649868
Clinical data
ATC code	None;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name N-([(2S)-1-([5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl)-2-piperidinyl]methyl)-4-benzofurancarboxamide;
PubChem CID	25195495;
ChemSpider	25069706;
ChEMBL	ChEMBL1272307;
CompTox Dashboard (EPA)	DTXSID90191491 ;
Chemical and physical data
Formula	C26H24FN3O3S
Molar mass	477.549 g/mol (free base) g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NC(=C(S1)C2=CC=C(C=C2)F)C(=O)N3CCCC[C@H]3CNC(=O)C4=C5C=COC5=CC=C4;
	InChI InChI=1S/C26H24FN3O3S/c1-16-29-23(24(34-16)17-8-10-18(27)11-9-17)26(32)30-13-3-2-5-19(30)15-28-25(31)21-6-4-7-22-20(21)12-14-33-22/h4,6-12,14,19H,2-3,5,13,15H2,1H3,(H,28,31)/t19-/m0/s1; Key:ZJXIUGNEAIHSBI-IBGZPJMESA-N;

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Revision as of 08:36, 26 October 2014

SB-649,868 is an dual orexin receptor antagonist in development by GlaxoSmithKline.^[1] Currently in Phase 2 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]

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. doi:10.1124/dmd.110.035386. PMID 21045199.{{cite journal}}: CS1 maint: multiple names: authors list (link)
^ "Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist". Aug 2012. PMID 21730017. {{cite journal}}: Cite journal requires |journal= (help)
^ "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.
^ "The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia". Sleep. Aug 2012. PMID 22851805.

Revision as of 07:43, 26 October 2014 edit BG19bot (talk \| contribs) 1,005,055 edits m WP:CHECKWIKI error fix for #61. Punctuation goes before References. Do general fixes if a problem exists. - using AWB (10480) ← Previous edit		Revision as of 08:36, 26 October 2014 edit undo 84.106.113.160 (talk) No edit summary Next edit →
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	'''SB-649,868''' is an dual [[orexin]] receptor antagonist in development by [[GlaxoSmithKline]].<ref name="pmid21045199">{{cite journal \| author = Renzulli C, Nash M, Wright M, Thomas S, Zamuner S, Pellegatti M, Bettica P, Boyle G \| title = Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans \| journal = Drug Metab. Dispos. \| volume = 39 \| issue = 2 \| pages = 215–27 \|date=February 2011 \| pmid = 21045199 \| doi = 10.1124/dmd.110.035386 \| url = http://dmd.aspetjournals.org/content/39/2/215.full.pdf }}</ref> Currently in Phase 2 development for insomnia~~, its one of two such compounds currently in development, the other being Merck & Co's [[suvorexant]]~~.		'''SB-649,868''' is an dual [[orexin]] receptor antagonist in development by [[GlaxoSmithKline]].<ref name="pmid21045199">{{cite journal \| author = Renzulli C, Nash M, Wright M, Thomas S, Zamuner S, Pellegatti M, Bettica P, Boyle G \| title = Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans \| journal = Drug Metab. Dispos. \| volume = 39 \| issue = 2 \| pages = 215–27 \|date=February 2011 \| pmid = 21045199 \| doi = 10.1124/dmd.110.035386 \| url = http://dmd.aspetjournals.org/content/39/2/215.full.pdf }}</ref> Currently in Phase 2 development for insomnia.

	A Phase I study evaluated doses up to 80 mg, resulting in significant improvement in sleep latency without adverse effects.<ref>{{Cite journal\|url = \|title = Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.\|last = \|first = \|date = Aug 2012\|journal = \|accessdate = \|doi = \|pmid = 21730017}}</ref>{{drugbox		A Phase I study evaluated doses up to 80 mg, resulting in significant improvement in sleep latency without adverse effects.<ref>{{Cite journal\|url = \|title = Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist.\|last = \|first = \|date = Aug 2012\|journal = \|accessdate = \|doi = \|pmid = 21730017}}</ref>{{drugbox

Revision as of 08:36, 26 October 2014

References

Further reading