Lemborexant

Dual orexin receptor antagonist (DORA)

Lemborexant

Dayvigo

Lemborexant (brand name Dayvigo) is a dual orexin receptor antagonist (DORA) FDA-approved in December 2019 for insomnia in adults. Among DORAs, lemborexant has faster receptor association/dissociation kinetics than suvorexant, which is hypothesized to facilitate sleep onset while still maintaining adequate duration of antagonism for sleep maintenance. The 17-19 hour half-life can produce some next-day residual sedation in sensitive individuals. DORAs broadly produce sleep that more closely resembles physiologic sleep architecture than GABAergic hypnotics, with reduced REM suppression. Side effect profile favorable compared to benzodiazepines, but sleep paralysis, sleep-related hallucinations, and complex sleep behaviors have been reported.

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Titration strategies

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Effects

Somnolence (next-day), headache, nightmares, abnormal dreams, sleep paralysis, hallucinations near sleep onset. Complex sleep behaviors class warning.

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Pharmacodynamics

Competitive antagonism at OX1R (Ki ~6 nM) and OX2R (Ki ~3 nM). No clinically significant activity at other receptors.

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Summary

Classes

Dual orexin receptor antagonist (DORA)

Common uses

Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019)

Pharmacy

Starting dose

5 mg PO at bedtime; may increase to 10 mg if inadequate

Preparations

5 mg, 10 mg tablets

US FDA Max

10 mg/d

Pharmacology

Routes

Oral

Onset

~30 min

Duration

~7-8 hours

Half-life

~17-19 hours (longer than daridorexant)

Bioavailability

~44%

Pregnancy

Limited data; avoid

Legal status

Rx, Schedule IV (US)

Purported mechanism

Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance.