The Pharmaceutical Journal
Vol 278 No 7439 p184
17 February 2007

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Orexin antagonist shows promise as insomnia treatment

An antagonist of the orexin OX₁/OX₂ receptor — ACT-078573 — being developed by Actelion may prove useful for people suffering from sleep disorders.

The company reports that a study involving 39 patients with primary insomnia indicates that the compound improves sleep efficiency as measured by polysomnography. The study follows research published in Nature Medicine this month that shows an increase in sleep in animals and healthy volunteers (2007;13:150).

Actelion says that ACT-078573 is the first oral orexin receptor antagonist that penetrates the blood-brain barrier and is capable of inducing transcient and reversible blockade of the OX₁ and OX₂ receptors.