Actelion reports strong early data on sleep drug

Swiss drugmaker Actelion says that preclinical and placebo-controlled clinical trial data were published in the February edition of Nature Medicine which demonstrate that its orexin-OX1/OX2 receptor blocker, ACT-078573, induces characteristic signs of sleep in animal models, as well as in man. In healthy human volunteers, signs of sleep such as reduced alertness were observed when ACT-078573 was administered during daytime, the active part of the circadian cycle in man.

Orexins are neuropeptides produced in the brain that play an important role in maintaining wakefulness and therefore regulate the sleep-wake cycle. ACT-078573 is the first oral orexin receptor blocker that penetrates the blood-brain barrier. In animal models, the agent caused an increase in rapid-eye-movement sleep, a distinct phase of normal sleep which is thought to play a key role in the consolidation of different types of memory function.

In addition, within one hour after taking a single dose of 200mg of ACT-078573, healthy volunteers displayed signs of sleep. Treatment was well-tolerated up to 1,000mg with no severe or serious adverse events reported. Signs of sleep disappeared after six hours with a dose of 400mg.