SB-649868
   HOME

TheInfoList



OR:

SB-649868 is a dual
orexin receptor The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene (, ). Both orexin receptors exhibit ...
antagonist that was being developed by GlaxoSmithKline as a treatment for
insomnia Insomnia, also known as sleeplessness, is a sleep disorder in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, ...
. A phase I
clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...
evaluated doses up to 80 mg, resulting in significant improvement in sleep latency without adverse effects. In randomized, double-blind, placebo-controlled crossover trials, the 10 and 30 mg doses increased sleep time and reduced sleep latency. The subsequent phase II study added a 60 mg dose and observed dose-dependent sleep promotion. The compound no longer appears to be under active development, with the last study posted to ClinicalTrials.gov completed in 2010.


See also

*
Almorexant Almorexant, also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treat ...
* Filorexant *
Lemborexant Lemborexant, sold under the brand name Dayvigo, is an orexin antagonist medication which is used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maint ...
* Suvorexant


References


Further reading

* * Hypnotics Sedatives Orexin antagonists Benzofurans Fluoroarenes {{sedative-stub