Lemborexant – Mechanism of Action | Psychopharmacology | Clinical Application

Posted on:May 30, 2022
Last Updated: November 24, 2023
Time to read: 7 minutes

Lemborexant (DAYVIGO) is a dual orexin receptor antagonist (DORA) that was approved in 2019 for the treatment of sleep-onset and/or sleep maintenance insomnia in adults. [Kärppä et al. 2020]

More recently, it has been suggested to be safe and effective in patients with mild obstructive sleep apnoea. [Cheng et al. 2020]

  • Lemborexant is an organic n-arylamide compound which contains a carboxamide group that is N-linked to an aryl group.

Recent advances in sleep research suggest that insomnia is driven by an inability to switch-off wake-promoting circuits. [Beuckmann et al 2017]; [Beuckmann et al 2019]

Unlike other pharmacologic treatments that focus on enhancing sleep onset, orexin antagonists such as lemborexant act to counteract inappropriate wakefulness.

The novel mechanism of action of orexin antagonists offers advantages over classic hypnotic agents, such as a more favourable safety profile; however, it must be noted that lemborexant may still carry some risk of abuse. [FDA DAYVIGO Prescribing Information].  , [TGA PI]