The phase III trial using almorexant for the treatment of sleep disorders has been discontinued due to results in regard to its clinical profile and tolerability profiles.
Almorexant is a dual orexin receptor antagonist being co-developed by both GlaxoSmithKline (GSK) and Actelion under the Orexin Alliance formed in July 2008 (See below for more information).
Informatin about Orexin and almorexant:
- Orexin is a neural peptide modulators often seen in the brain. They are produced in the hypothalamic neurons. Its functions include regulating the sleep and wake states in human body. Orexin receptor is G-protein coupling receptor. Once orexin binds to its receptor, its effects have been demonstrated to increase wakefullness. When a deficiency of orexin signals occurred, narcolepsy has been observed.
- Almorexant works to stop the orexin receptor from interaction with orexin which will lead to alertness and wakefullness. As a result, by stopping this interaction, less orexin neuron will be activated and