Lemborexant

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Lemborexant
Clinical data
Trade namesDayvigo
Other namesE-2006
License data
Pregnancy
category
Routes of
administration		By mouth[3]
Drug classOrexin receptor antagonist; Hypnotic; Sedative
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityGood (≥87%)[5][6]
Protein binding94%[3]
MetabolismLiver (major: CYP3A4, minor: CYP3A5)[3]
MetabolitesM10[3]
Elimination half-life17–19 hours or 55 hours[3][7]
ExcretionFeces: 57.4%[3]
Urine: 29.1%[3]
Identifiers
  • (1R,2S)-2-[(2,4-Dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide
JSmol)
  • CC1=NC(=NC=C1OC[C@]2(C[C@H]2C(=O)NC3=NC=C(C=C3)F)C4=CC(=CC=C4)F)C
  • InChI=1S/C22H20F2N4O2/c1-13-19(11-25-14(2)27-13)30-12-22(15-4-3-5-16(23)8-15)9-18(22)21(29)28-20-7-6-17(24)10-26-20/h3-8,10-11,18H,9,12H2,1-2H3,(H,26,28,29)/t18-,22+/m0/s1
  • Key:MUGXRYIUWFITCP-PGRDOPGGSA-N

Lemborexant, sold under the brand name Dayvigo, is an

maintenance in adults.[3][8] The medication is taken by mouth.[3][8]

Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.[3][8]

Lemborexant was approved for medical use in the United States in December 2019.

potential for misuse.[3][8] Besides lemborexant, other orexin receptor antagonists including suvorexant and daridorexant have also been introduced.[12][13]

Medical uses

Lemborexant is used in the treatment of insomnia in adults.[3]

A major

Z-drugs generally showed larger effect sizes (e.g., SMDs of 0.45 to 0.83) than lemborexant and the other orexin receptor antagonists.[14] However, the review concluded that lemborexant and eszopiclone among all of the insomnia medications assessed had the best profiles overall in terms of efficacy, tolerability, and acceptability.[14]

Compared to

dependence.[15] Memory and attention are not affected the next morning when taking lemborexant.[16]

Available forms

Lemborexant is available in the form of 5 and 10 mg

film-coated tablets.[3]

Side effects

hypnagogic hallucinations (0.1% at 5 mg and 0.7% at 10 mg vs. 0% for placebo).[3]

Lemborexant at doses of 10, 20, and 30 mg produces

misuse potential.[3][17]

Pharmacology

Pharmacodynamics

Lemborexant is a dual

duration of action.[12]

Pharmacokinetics

The

terminal elimination half-life is 55 hours.[3][7][8] The medication is excreted in feces (57%) and to a lesser extent urine (29%).[3]

steady state in humans.[21]

Although lemborexant has a longer

terminal elimination half-life than suvorexant, it appears to be more rapidly cleared than suvorexant in the earlier phases of elimination.[21][7] In addition, lemborexant dissociates from the orexin receptors more rapidly than does suvorexant.[21] These differences may allow for comparatively reduced next-day effects such as daytime somnolence with lemborexant.[21][7]

History

In June 2016, Eisai initiated Phase III clinical trials in the United States, France, Germany, Italy, Japan, Poland, Spain and the UK.[22]

In December 2019, lemborexant was approved for use in the United States based on results from the SUNRISE 1 and SUNRISE 2 Phase III clinical trials.[11][23]

Society and culture

Names

Lemborexant is the

INNTooltip International Nonproprietary Name while E-2006 was its developmental code name. Lemborexant is sold under the brand name Dayvigo.[3]

Availability

Lemborexant is marketed in the United States, Canada, Australia, and Japan.[24][25][26][27] It is not approved by the European Medicines Agency (EMA) for use in the European Union or by the Medicines and Healthcare products Regulatory Agency (MHRA) in the United Kingdom.[28][29]

Research

Lemborexant is under development for the treatment of

sleep apnea, and chronic obstructive pulmonary disease.[30] As of February 2022, it is in phase 2 clinical trials for circadian rhythm sleep disorders and phase 1 trials for sleep apnea and chronic obstructive pulmonary disease.[30]

References

  1. ^ a b "Dayvigo". Therapeutic Goods Administration (TGA). 23 July 2021. Retrieved 5 September 2021.
  2. ^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 12 May 2022. Retrieved 13 May 2022.
  3. ^ a b c d e f g h i j k l m n o p q r s t u v w x y z aa ab ac ad "Dayvigo- lemborexant tablet, film coated". DailyMed. Retrieved 17 June 2021.
  4. ^ "Summary Basis of Decision (SBD) for Dayvigo". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  5. ^
    ISSN 0377-8282
    .
  6. ^
    PMID 32666570
    .
  7. ^
    S2CID 221572078
    .
  8. ^
    S2CID 235321467
    .
  9. ^ "Novel Drug Approvals for 2019". U.S. Food and Drug Administration (FDA). 2 January 2020. Retrieved 10 January 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  10. ^ "FDA-Approved Drugs: Lemborexant". U.S. Food and Drug Administration (FDA). Retrieved 10 January 2020.
  11. ^ a b "FDA Approves Dayvigo (lemborexant) for the Treatment of Insomnia in Adult Patients". Drugs.com. 23 December 2019. Retrieved 10 January 2020.
  12. ^
    S2CID 248119793
    .
  13. PMID 35298826
    .
  14. ^
    S2CID 250536370
    .
  15. PMID 34422270
    .
  16. PMID 32022664
    .
  17. S2CID 238476630
    .
  18. PMID 25489915
    .
  19. PMID 26045032
    .
  20. S2CID 21106711
    .
  21. ^
    PMID 34553844
    .
  22. ^ "Lemborexant". Specialist Pharmacy Service. Archived from the original on 7 November 2017. Retrieved 5 November 2017.
  23. ^ "Drug Trials Snapshot: Dayvigo". U.S. Food and Drug Administration (FDA). 20 December 2019. Retrieved 24 January 2020. Public Domain This article incorporates text from this source, which is in the public domain.
  24. ^ "Micromedex Products: Please Login".
  25. ^ "Drug Product Database: Access the database". 18 March 2010.
  26. ^ "Dayvigo". 23 July 2021.
  27. ^ "EISAI TO LAUNCH IN-HOUSE DEVELOPED NEW ANTI-INSOMNIA DRUG DAYVIGO® (LEMBOREXANT) WITH INDICATION FOR INSOMNIA IN JAPAN | News Release：2020 | Eisai Co., Ltd".
  28. ^ "Medicines". European Medicines Agency.
  29. ^ "Products". Medicines and Healthcare products Regulatory Agency (MHRA).
  30. ^ a b "Lemborexant - Eisai - AdisInsight".
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