Lemborexant

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
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H20F2N4O2
Molar mass410.425 g·mol−1
3D model (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 orexin antagonist medication which is used in the treatment of insomnia.[3][8] It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults.[3][8] The medication is taken by mouth.[3][8]

Side effects of lemborexant include somnolence, fatigue, headache, and abnormal dreams.[3][8] The medication is a dual orexin receptor antagonist (DORA).[3][8] It acts as a selective dual antagonist of the orexin receptors OX1 and OX2.[3][8] Lemborexant has a long elimination half-life of 17 to 55 hours and a time to peak of about 1 to 3 hours.[3][8] It is not a benzodiazepine or 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.[9][10][11] It is a schedule IV controlled substance in the United States and may have a low potential for misuse.[3][8] Besides lemborexant, other orexin receptor antagonists including suvorexant and daridorexant have also been introduced.[12][13]

  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 "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. ^ Cite error: The named reference HoyerJacobson2018 was invoked but never defined (see the help page).
  6. ^ Cite error: The named reference pmid32666570 was invoked but never defined (see the help page).
  7. ^ Cite error: The named reference pmid32901578 was invoked but never defined (see the help page).
  8. ^ a b c d e f g h i Waters K (February 2022). "Review of the Efficacy and Safety of Lemborexant, a Dual Receptor Orexin Antagonist (DORA), in the Treatment of Adults With Insomnia Disorder". The Annals of Pharmacotherapy. 56 (2): 213–221. doi:10.1177/10600280211008492. PMID 34078141. 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. ^ Cite error: The named reference Approval was invoked but never defined (see the help page).
  12. ^ Cite error: The named reference pmid35043499 was invoked but never defined (see the help page).
  13. ^ Markham A (April 2022). "Daridorexant: First Approval". Drugs. 82 (5): 601–607. doi:10.1007/s40265-022-01699-y. PMC 9042981. PMID 35298826.