Actelion announces publication of ACT-078573 data

Actelion has announced that the results of clinical and pre-clinical trials of Orexin-OX1/OX2 receptor antagonist ACT-078573 have been published in the most recent issue of Nature Medicine.

According to the data, when healthy human volunteers were administered with the compound during the active part of the circadian cycle, they exhibited reduced alertness and other signs of sleep.

ACT-078573 is an oral orexin receptor antagonist that induces a temporary and reversible block on OX1 and OX2. Orexins play a role in the body in the maintaining of wakefulness.

“These data demonstrate that Actelion’s Orexin-OX1/OX2 receptor antagonist ACT-078573 induces characteristic signs of sleep in animal models as well as in man,” the company reports.

It adds that administration with the compound resulted in an increase in rapid eye movement (REM) sleep in animal models, while treatment with standard GABA-A receptor modulators is linked to a fall in REM sleep.

Actelion commented that it would engage in analysis of the role of REM sleep in humans and its association with memory function.

The company reports that its orexin receptor antagonist is currently undergoing phase II clinical trials, which it states could “completely shift the paradigm” regarding the treatment of sleep disorders.