Lemborexant
FDA-approved dual orexin receptor antagonist (DORA) for insomnia, prescription only.
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Pharmacology
Contents
WHAT IS LEMBOREXANT?
Detailed overview
Lemborexant (Dayvigo) is a dual orexin receptor antagonist (DORA) approved by the FDA in 2019 for adults with insomnia characterized by problems with sleep onset and/or sleep maintenance. Unlike benzodiazepines and Z-drugs, it does not broadly sedate the brain through the GABA system; instead it selectively blocks the OX1 and OX2 receptors for the orexin-A and orexin-B neuropeptides, turning down the wakefulness (arousal) signal to allow more natural sleep. In the phase 3 SUNRISE-1 and SUNRISE-2 trials it improved sleep latency, sleep maintenance and sleep efficiency versus placebo and extended-release zolpidem. It is a prescription, Schedule IV controlled substance in the United States.
Mechanism
Dual orexin OX1/OX2 antagonist (DORA)
Half-life
~17-19 hours
Legal status
Prescription (FDA 2019, Schedule IV)
Receptor profile
- Orexin OX2 receptorStrong
- Orexin OX1 receptorStrong
- Wakefulness (arousal) driveStrong
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Next-day somnolence or daytime fatigue, especially at the 10 mg dose
- Headache
- Vivid or abnormal dreams, nightmares
- Sleep paralysis, hypnagogic or hypnopompic hallucinations (uncommon)
- Transient nighttime or morning muscle weakness, cataplexy-like episodes (rare)
- Complex sleep behaviors (sleepwalking, sleep-driving) without full recall
Contraindications · 6
- Narcolepsy: orexin blockade is contraindicated
- Severe hepatic impairment: avoid; limit to 5 mg in moderate impairment
- Avoid or reduce with strong or moderate CYP3A inhibitors
- Alcohol and other CNS depressants: additive sedation, avoid combining
- Pregnancy and breastfeeding: safety not established
- Severe depression or other conditions causing daytime sleepiness
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Comparison of Lemborexant With Placebo and Zolpidem Tartrate Extended Release for the Treatment of Older Adults With Insomnia Disorder: A Phase 3 Randomized Clinical Trial
Rosenberg R, Murphy P, Zammit G, Mayleben D, Kumar D, Dhadda S, Filippov G, LoPresti A, Moline M
Long-term efficacy and tolerability of lemborexant compared with placebo in adults with insomnia disorder: results from the phase 3 randomized clinical trial SUNRISE 2
Kärppä M, Yardley J, Pinner K, Filippov G, Zammit G, Moline M, Perdomo C, Inoue Y, Ishikawa K, Kubota N
Long-term effectiveness and safety of lemborexant in adults with insomnia disorder: results from a phase 3 randomized clinical trial
Yardley J, Kärppä M, Inoue Y, Pinner K, Perdomo C, Ishikawa K, Filippov G, Kubota N, Moline M
Comparison of the effect of lemborexant with placebo and zolpidem tartrate extended release on sleep architecture in older adults with insomnia disorder
Moline M, Zammit G, Yardley J, Pinner K, Kumar D, Perdomo C, Cheng JY
Improvement in fatigue and sleep measures with the dual orexin receptor antagonist lemborexant in adults with insomnia disorder
Chepke C, Jain R, Rosenberg R, Moline M, Yardley J, Pinner K, Malhotra M
FAQ
FAQ
FDA-approved dual orexin receptor antagonist (DORA) for insomnia, prescription only.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.