Skip to main content
Log in

Lemborexant in insomnia disorder: a profile of its use

  • Adis Drug Q&A
  • Published:
Drugs & Therapy Perspectives Aims and scope Submit manuscript

A Correction to this article was published on 01 October 2020

This article has been updated

Abstract

Lemborexant (Dayvigo™), a dual orexin receptor antagonist, is an effective and well-tolerated treatment option for adults with insomnia characterized by difficulties with sleep onset and/or sleep maintenance. In phase 3 clinical trials, oral lemborexant 5 or 10 mg once nightly significantly reduced sleep onset latency (SOL) and wake-after-sleep onset (WASO), and improved sleep efficiency (SE). Lemborexant was also associated with reductions in patient-reported fatigue and insomnia severity, and was well tolerated through 12 months of treatment. In special safety studies, lemborexant did not increase the auditory awakening threshold or cause next-day postural instability, and was not associated with rebound insomnia, withdrawal symptoms, or clinically meaningful impairment of next-day memory or driving performance.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

Change history

  • 01 October 2020

    The author has alerted us to the following errors, and the following corrections should be noted.

References

  1. Liu MT. Current and emerging therapies for insomnia. Am J Manag Care. 2020;26(4 Suppl):S85–90.

    PubMed  Google Scholar 

  2. Morin CM, Drake CL, Harvey AG, et al. Insomnia disorder. Nat Rev. 2015;1(1):1–18.

    Google Scholar 

  3. Qaseem A, Kansagara D, Forciea MA, et al. Management of chronic insomnia disorder in adults: a clinical practice guideline from the American College of Physicians. Ann Intern Med. 2016;165(2):125–33.

    Article  PubMed  Google Scholar 

  4. Matheson E, Hainer BL. Insomnia: pharmacologic therapy. Am Fam Physician. 2017;96(1):29–35.

    PubMed  Google Scholar 

  5. Wang C, Wang Q, Ji B, et al. The orexin/receptor system: molecular mechanism and therapeutic potential for neurological diseases. Front Mol Neurosci. 2018;11:220.

    Article  PubMed  PubMed Central  Google Scholar 

  6. Han Y, Yuan K, Zheng Y, et al. Orexin receptor antagonists as emerging treatments for psychiatric disorders. Neurosci Bull. 2020;36(4):432–48.

    Article  CAS  PubMed  Google Scholar 

  7. Dayvigo™ (lemborexant): US prescribing information. Woodcliff Lake: Eisai Inc.; 2020.

  8. Dayvigo tablets 2.5 mg/Dayvigo tablets 5 mg/Dayvigo tablets 10 mg: Japanese prescribing information. Tokyo: Eisai Co Ltd; 2020.

  9. Yoshida Y, Naoe Y, Terauchi T, et al. Discovery of (1R,2S)-2-{[(2,4-dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluor opyridin-2-yl)cyclopropanecarboxamide (E2006): a potent and efficacious oral orexin receptor antagonist. J Med Chem. 2015;58(11):4648–64.

    Article  CAS  PubMed  Google Scholar 

  10. Beuckmann CT, Suzuki M, Ueno T, et al. In vitro and in silico characterization of lemborexant (E2006), a novel dual orexin receptor antagonist. J Pharmacol Exp Ther. 2017;362(2):287–95.

    Article  CAS  PubMed  Google Scholar 

  11. Karppa M, Yardley J, Pinner K, et al. 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. Sleep. 2020. https://doi.org/10.1093/sleep/zsaa123.

    Article  PubMed  PubMed Central  Google Scholar 

  12. Beuckmann CT, Ueno T, Nakagawa M, et al. Preclinical in vivo characterization of lemborexant (E2006), a novel dual orexin receptor antagonist for sleep/wake regulation. Sleep. 2019;42(6):zsz076.

    Article  PubMed  PubMed Central  Google Scholar 

  13. Mahoney CE, Mochizuki T, Scammell TE. Dual orexin receptor antagonists increase sleep and cataplexy in wild type mice. Sleep. 2019;43(6):zsz302.

    Article  PubMed Central  Google Scholar 

  14. Murphy P, Moline M, Mayleben D, et al. Lemborexant, a dual orexin receptor antagonist (DORA) for the treatment of insomnia disorder: results from a Bayesian, adaptive, randomized, double-blind, placebo-controlled study. J Clin Sleep Med. 2017;13(11):1289–99.

    Article  PubMed  PubMed Central  Google Scholar 

  15. Rosenberg R, Murphy P, Zammit G, et al. 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. JAMA Netw Open. 2019;2(12):e1918254.

    Article  PubMed  PubMed Central  Google Scholar 

  16. Moline M, Pinner K, Cheng J, et al. Effect of lemborexant compared with placebo and zolpidem extended release on sleep architecture in older adults with insomnia disorder [abstract]. Sleep Med. 2019;64(Suppl 1):s437.

    Article  Google Scholar 

  17. Yardley J, Karppa M, Inoue Y, et al. Long-term effectiveness and safety of lemborexant in adults with insomnia disorder: 12-month results from SUNRISE-2 [abstract]. Sleep Med. 2019;64(Suppl1):S263–4.

    Article  Google Scholar 

  18. Moline M, Murphy P, Yardley J, et al. Efficacy and tolerability of lemborexant in female and male subjects with insomnia [abstract no. 0368]. Sleep. 2019;42(Suppl 1):S150.

    Google Scholar 

  19. Drake C, Yardley J, Kumar D, et al. Impact of lemborexant treatment on the patient global impression-insomnia scale [abstract no. 118]. Sleep Med. 2019;64(Suppl 1):S96–7.

    Article  Google Scholar 

  20. Drake C, Yardley J, Pinner K, et al. Subject-reported perception of long-term effectiveness of lemborexant versus placebo in nonelderly and elderly subgroups [abstract no. NR-17]. Am J Geriatr Psychiatry. 2020;28(4 Suppl):S133–4.

    Article  Google Scholar 

  21. Yardley J, Moline M, Pinner K, et al. Long-term effect of lemborexant on fatigue in subjects with insomnia disorder: patient-reported outcome from the 6-month placebo-controlled treatment period of the phase 3 study SUNRISE-2 [abstract]. Sleep Med. 2019;64(Suppl 1):s264.

    Article  Google Scholar 

  22. Yardley J, Pinner K, Moline M, et al. Impact of lemborexant on insomnia disease severity and fatigue in elderly subjects with insomnia from SUNRISE-2 [abstract no. NR-18]. Am J Geriatr Psychiatry. 2020;28(4 Suppl):S134–5.

    Article  Google Scholar 

  23. Zee PC, Murphy P, Yardley J, et al. Patient-reported sleep onset and sleep maintenance: pooled analyses of lemborexant phase 3 studies [abstract no. 0370]. Sleep. 2019;42(Suppl 1):A150–1.

    Article  Google Scholar 

  24. Roth T, Rosenberg R, Murphy P, et al. Lemborexant treatment for insomnia in phase 3: impact on disease severity [abstract no. 0371]. Sleep. 2019;42(Suppl 1):A151.

    Article  Google Scholar 

  25. Cheng JY, Filipov G, Moline M, et al. Respiratory safety of lemborexant in healthy adult and elderly subjects with mild obstructive sleep apnea: a randomized, double-blind, placebo-controlled, crossover study. J Sleep Res. 2020. https://doi.org/10.1111/jsr.13021.

    Article  PubMed  PubMed Central  Google Scholar 

  26. Murphy PJ, Yasuda S, Nakai K, et al. Concentration-response modeling of ECG data from early-phase clinical studies as an alternative clinical and regulatory approach to assessing QT risk: experience from the development program of lemborexant. J Clin Pharmacol. 2017;57(1):96–104.

    Article  CAS  PubMed  Google Scholar 

  27. Murphy P, Kumar D, Zammit G, et al. Safety of lemborexant versus placebo and zolpidem: effects on auditory awakening threshold, postural stability, and cognitive performance in healthy older subjects in the middle of the night and upon morning awakening. J Clin Sleep Med. 2020. https://doi.org/10.5664/jcsm.8294.

    Article  PubMed  PubMed Central  Google Scholar 

  28. Zammit G, Rosenberg R, Mayleben D, et al. Lemborexant versus zolpidem extended release on morning postural stability in older adults [abstract no. G57]. J Manag Care Spec Pharm. 2019;25(3-A Suppl):S67.

    Google Scholar 

  29. Vermeeren A, Jongen S, Murphy P, et al. On-the-road driving performance the morning after bedtime administration of lemborexant in healthy adult and elderly volunteers. Sleep. 2019;42(4):zsy260.

    Article  PubMed  Google Scholar 

  30. Farkouh A, Riedl T, Gottardi R, et al. Sex-related differences in pharmacokinetics and pharmacodynamics of frequently prescribed drugs: a review of the literature. Adv Ther. 2020;37(2):644–55.

    Article  CAS  PubMed  Google Scholar 

  31. Kishi T, Nomura I, Matsuda Y, et al. Lemborexant vs suvorexant for insomnia: a systematic review and network meta-analysis. J Psychiatr Res. 2020;128:68–74.

    Article  PubMed  Google Scholar 

  32. Scott LJ. Lemborexant: first approval. Drugs. 2020;80(4):425–32.

    Article  CAS  PubMed  Google Scholar 

Download references

Acknowledgements

The manuscript was updated from Drugs 2020;80(4):425–32 [32], and was reviewed by: S. de Biase, Neurology Unit, Ospedale Dell’Angelo, Venice-Mestre, Italy; D. N. Neubauer, Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, MD, USA. During the peer review process, Eisai, the marketing-authorization holder of lemborexant, was also offered an opportunity to provide a scientific accuracy review of their data. Changes resulting from comments received were made on the basis of scientific and editorial merit.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Hannah A. Blair.

Ethics declarations

Funding

The preparation of this review was not supported by any external funding.

Authorship and Conflict of interest

H. A. Blair is a salaried employee of Adis International Ltd/Springer Nature, and declares no relevant conflicts of interest. All authors contributed to the review and are responsible for the article content.

Ethics approval, Consent to participate, Consent to publish, Availability of data and material, Code availability

Not applicable.

Additional information

The original version of this article was revised: Due to textual changes.

Enhanced material for this Adis Drug Q&A can be found at https://doi.org/10.6084/m9.figshare.12824534.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Blair, H.A. Lemborexant in insomnia disorder: a profile of its use. Drugs Ther Perspect 36, 427–434 (2020). https://doi.org/10.1007/s40267-020-00771-5

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40267-020-00771-5

Navigation