The orexin receptor antagonist lemborexant (Dayvigo) has been approved by the US Food and Drug Administration for the treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance in adults, drug developer Eisai Co. announced.
Upon scheduling by the US Drug Enforcement Administration, the medication will be available in 5-mg and 10-mg tablets.
The approval followed two phase 3 studies that evaluated lemborexant and comparators for up to 1 month, and lemborexant and placebo for 6 months, in approximately 2000 adults with insomnia. In subjective and objective evaluations, lemborexant was significantly superior to placebo for sleep onset and sleep maintenance.
In the trials, lemborexant was not associated with rebound insomnia following discontinuation. Furthermore, there was no evidence of withdrawal effects following discontinuation at either dose.
Lemborexant’s mechanism of action is presumed to be through the antagonism of orexin receptors. The orexin neuropeptide signaling system is involved in wakefulness, and an individual’s wake drive is thought to be suppressed by blocking the binding of wake-promoting neuropeptides orexin A and orexin B to orexin receptors OX1R and OX2R. Lemborexant, the company explained, binds to orexin receptors OX1R and OX2R and acts as a competitive antagonist.
“Insomnia disorder is a chronic condition that has a variety of potential negative impacts and long-term consequences for health and well-being,” said Russell Rosenberg, PhD, a principal investigator in the lemborexant clinical studies and former chairman of the board of the National Sleep Foundation. “The clinical trials provide evidence that Dayvigo may improve patients’ ability to fall asleep and stay asleep.”