Lemborexant

The mechanism of action of lemborexant in the treatment of insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system plays a role in wakefulness.

• DAYVIGO is indicated for the treatment of adult patients with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance [see Clinical Studies ( 14.1 )] . DAYVIGO is an orexin receptor antagonist indicated for the treatment of adult patients with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance.ICD-10: G47.00

• DAYVIGO is contraindicated in patients with narcolepsy. DAYVIGO is contraindicated in patients with narcolepsy.contraindicated

Recommended dose is 5 mg taken no more than once per night, immediately before going to bed, with at least 7 hours remaining before the planned time of awakening. Dosage may be increased to 10 mg based on clinical response and tolerability. ( 2.1 ) The maximum recommended dose is 10 mg once daily. ( 2.1 ) Time to sleep onset may be delayed if taken with or soon after a meal. ( 2.1 ) Hepatic Impairment: ( 2.3 ) ○ Moderate hepatic impairment: Initial and maximum recommended dosage is 5 mg no more than once per night. ○ Severe hepatic impairment: Not recommended. 2.1 Dosing Information The recommended dosage of DAYVIGO is 5 mg taken no more than once per night, immediately before going to bed, with at least 7 hours remaining before the planned time of awakening. The dose may be increased to the maximum recommended dose of 10 mg based on clinical response and tolerability. Time to sleep onset may be delayed if taken with or soon after a meal [see Clinical Pharmacology ( 12.3 )]. 2.2 Dosage Recommendations for Concomitant Use with CYP3A Inhibitors or CYP3A Inducers Co-administration with Strong or Moderate CYP3A Inhibitors Avoid concomitant use of DAYVIGO with strong or moderate CYP3A inhibitors [see Drug Interactions ( 7.1 ), Clinical Pharmacology ( 12.3 )]. Co-administration with Weak CYP3A Inhibitors The maximum recommended dosage of DAYVIGO is 5 mg no more than once per night when co-administered with weak CYP3A inhibitors [see Drug Interactions ( 7.1 ), Clinical Pharmacology ( 12.3 )].

CNS Depressant Effects and Daytime Impairment: Impairs alertness and motor coordination including morning impairment. Risk increases with dose and use with other central nervous system (CNS) depressants. For patients taking DAYVIGO 10 mg, caution against next-day driving and other activities requiring complete mental alertness. ( 5.1 ) Sleep Paralysis, Hypnagogic/Hypnopompic Hallucinations, and Cataplexy-like Symptoms: May occur with use of DAYVIGO. ( 5.2 ) Complex Sleep Behaviors: Behaviors including sleep-walking, sleep-driving, and engaging in other activities while not fully awake may occur. Discontinue immediately if a complex sleep behavior occurs. ( 5.3 ) Compromised Respiratory Function: Effect on respiratory function should be considered. ( 5.4 , 8.8 ) Worsening of Depression/Suicidal Ideation: Worsening of depression or suicidal thinking may occur. Prescribe the lowest number of tablets feasible to avoid intentional overdosage. ( 5.5 ) Need to Evaluate for Co-morbid Diagnoses: Reevaluate if insomnia persists after 7 to 10 days of treatment. ( 5.6 ) 5.1 CNS Depressant Effects and Daytime Impairment DAYVIGO is a central nervous system (CNS) depressant that can impair daytime wakefulness even when used as prescribed. CNS depressant effects may persist in some patients for up to several days after discontinuing DAYVIGO. Prescribers should advise patients about the potential for next-day somnolence. Driving ability was impaired in some subjects taking DAYVIGO 10 mg [see Clinical Studies ( 14.2 )].

The following clinically significant adverse reactions are discussed in detail in other sections of the labeling: CNS Depressant Effects and Daytime Impairment [see Warnings and Precautions ( 5.1 )] Sleep Paralysis, Hypnagogic/Hypnopompic Hallucinations, and Cataplexy-like Symptoms [see Warnings and Precautions ( 5.2 )] Complex Sleep Behaviors [see Warnings and Precautions ( 5.3 )] Patients with Compromised Respiratory Function [see Warnings and Precautions ( 5.4 )] Worsening of Depression/Suicidal Ideation [see Warnings and Precautions ( 5.5 )] The most common adverse reaction (reported in ≥5% of patients treated with DAYVIGO and at least twice the rate of placebo) was somnolence. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Eisai Inc. at 1-888-274-2378 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of DAYVIGO was evaluated in 1418 adult patients with insomnia disorder (age 18 to 88 years) from two controlled efficacy trials (Study 1 and Study 2). Study 1 was a 6-month placebo-controlled trial assessing DAYVIGO 5 or 10 mg once nightly, followed by a 6-month parallel-group extension period in which patients initially treated with DAYVIGO continued on the same dose, and patients who received placebo were re-randomized to receive DAYVIGO 5 or 10 mg once nightly.

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women who are exposed to psychiatric medications, including DAYVIGO, during pregnancy. Healthcare providers are encouraged to advise patients to register by calling the National Pregnancy Registry for Psychiatric Medications, at1-866-961-2388 or visiting online at https://womensmentalhealth.org/research/pregnancyregistry . Risk Summary There are no available data on DAYVIGO use in pregnant women to evaluate for drug-associated risks of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, oral administration of lemborexant to pregnant rats and rabbits during the period of organogenesis caused toxicities only at high multiples of the human exposure at the maximum recommended human dose (MRHD) based on AUC. The no observed adverse effect levels (NOAEL) are approximately >100 and 23 times the MRHD based on AUC in rats and rabbits, respectively. Similarly, oral administration of lemborexant to pregnant and lactating rats caused toxicities only at high multiples of the human exposure at the MRHD based on AUC. The NOAEL is 93 times the MRHD based on AUC ( see Data ) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.

Metabolism

Following single doses of lemborexant 2.5 to 75 mg, geometric mean C max and AUC 0-24h increased slightly less than in proportion to dose. The extent of accumulation of lemborexant at steady-state is 1.5- to 3-fold across this dose range.

There is limited clinical experience with DAYVIGO overdose. In clinical pharmacology studies, healthy patients who were administered multiple doses of up to 75 mg (7.5 times the maximum recommended dose) of DAYVIGO showed dose-dependent increases in the frequency of somnolence. There is no available specific antidote to an overdose of DAYVIGO. In the event of overdose, standard medical practice for the management of any overdose should be used. In managing overdose, provide supportive care, including close medical supervision and monitoring and consider the possibility of multiple drug involvement. Consult a Certified Poison Control Center for the most up to date information on the management of overdosage (1-800-222-1222 or www.poison.org). The value of dialysis in the treatment of overdosage has not been determined with lemborexant. As lemborexant is highly protein-bound, hemodialysis is not expected to contribute to elimination of lemborexant.

• Dec 20, 2019NDANDA212028Eisai Inc

1. 1Drug Ineffective29812%
2. 2Off Label Use1766.8%
3. 3Suicide Attempt1385.4%
4. 4Somnolence1355.2%
5. 5Condition Aggravated1224.7%
6. 6Suicidal Ideation1224.7%
7. 7Fall983.8%
8. 8Headache873.4%
9. 9Nausea863.3%
10. 10Dizziness843.3%
11. 11Sleep Paralysis833.2%
12. 12Insomnia793.1%
13. 13Nightmare763.0%
14. 14Pyrexia732.8%
15. 15Malaise712.8%

The 10 most recently updated of 47 ClinicalTrials.gov registrations naming Lemborexant as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Effects of Lemborexant on Motor-sleep Comorbidity in Parkinson's Disease
  Not yet recruiting · Phase 4 · Interventional · 44 enrolled · YangPan
  NCT07384429updated 2026-06-11
• Lemborexant in Delayed Sleep Phase Syndrome
  Recruiting · Phase 4 · Interventional · 15 enrolled · University of California, San Francisco
  NCT06874855updated 2026-06-05
• The Effects of Lemborexant on the Ability to Sleep During Daytime
  Terminated · Phase 2 · Interventional · 5 enrolled · Centre Integre Universitaire de Sante et Services Sociaux du Nord de l'ile de Montreal
  NCT06231641updated 2026-05-28
• Lemborexant for the Treatment of Residual Insomnia in Major Depressive Disorder (MDD)
  Recruiting · Phase 2 · Interventional · 30 enrolled · Unity Health Toronto
  NCT06843187updated 2026-05-08
• DORA and LP in Alzheimer's Disease Biomarkers
  Recruiting · Phase 2 · Interventional · 201 enrolled · Washington University School of Medicine
  NCT06274528updated 2026-05-05
• Lemborexant Augmentation of Naltrexone for Alcohol Craving and Sleep
  Completed · Phase 3 · Interventional · 8 enrolled · Baylor College of Medicine
  NCT05458609updated 2026-03-24
• Efficacy and Safety of Lemborexant for Patients With Cirrhosis and Sleep Problems
  Completed · Phase 2 · Interventional · 82 enrolled · Indonesia University
  NCT07480096updated 2026-03-18
• Lemborexant in Delayed Sleep Phase Syndrome
  Completed · Phase 4 · Interventional · 71 enrolled · Stanford University
  NCT05463861updated 2026-03-02
• A Multicenter Observational Study of Lemborexant on Insomnia Patients With Psychiatric Disorders
  Recruiting · Observational · 121 enrolled · Shanghai Mental Health Center
  NCT07417813updated 2026-02-18
• Lemborexant for Sleep and Delirium Prevention in Elderly ICU Patients
  Not yet recruiting · Phase 4 · Interventional · 100 enrolled · Mahidol University
  NCT07407400updated 2026-02-12

Frequently asked questions

How does Lemborexant work?

The mechanism of action of lemborexant in the treatment of insomnia is presumed to be through antagonism of orexin receptors. The orexin neuropeptide signaling system plays a role in wakefulness.

What is Lemborexant used for?

According to FDA labeling, Lemborexant carries indications including: DAYVIGO is indicated for the treatment of adult patients with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance [see Clinical Studies ( 14.1 )] . DAYVIGO is an orexin receptor antagonist indicated for the treatment of adult patients with insomnia, characterized by difficulties with sleep onset and/or sleep maintenance.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Lemborexant?

Lemborexant is classified as Orexin receptor antagonists, Orexin Receptor Antagonist, Cytochrome P450 2B6 Inducers, Orexin Receptor Antagonists, Decreased Organized Electrical Activity.

What are the brand names for Lemborexant?

Lemborexant is marketed under brand names including Dayvigo.

What are the contraindications for Lemborexant?

Lemborexant labeling lists contraindications including: DAYVIGO is contraindicated in patients with narcolepsy. DAYVIGO is contraindicated in patients with narcolepsy.. Always consult the full prescribing information and a clinician.