lemborexant Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
orexin receptor antagonists 5360 1369764-02-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lemborexant
  • dayvigo
  • E2006
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. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors OX1R and OX2R is thought to suppress wake drive.
  • Molecular weight: 410.43
  • Formula: C22H20F2N4O2
  • CLOGP: -4.57
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 77
  • ALOGS: 3.99
  • ROTB: 6

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 2019 FDA EISAI INC
Jan. 23, 2020 PMDA Eisai Co., Ltd

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sleep paralysis 271.88 64.79 30 101 560 53348375

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Sleep paralysis 109.41 74.96 12 77 178 32513259
Nightmare 76.84 74.96 15 74 13151 32500286

Pharmacologic Action:

SourceCodeDescription
ATC N05CM21 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Other hypnotics and sedatives
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D000068796 Orexin Receptor Antagonists
MeSH PA D000068776 Sleep Aids, Pharmaceutical

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Insomnia indication 193462001
Narcolepsy contraindication 60380001 DOID:8986

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.22 acidic
pKa2 4.56 Basic
pKa3 1.71 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG DAYVIGO EISAI INC N212028 April 7, 2020 RX TABLET ORAL 8268848 Sept. 20, 2031 TREATMENT OF ADULT PATIENTS WITH INSOMNIA, CHARACTERIZED BY DIFFICULTIES WITH SLEEP ONSET AND/OR SLEEP MAINTENANCE
5MG DAYVIGO EISAI INC N212028 April 7, 2020 RX TABLET ORAL 8268848 Sept. 20, 2031 TREATMENT OF ADULT PATIENTS WITH INSOMNIA, CHARACTERIZED BY DIFFICULTIES WITH SLEEP ONSET AND/OR SLEEP MAINTENANCE
10MG DAYVIGO EISAI INC N212028 April 7, 2020 RX TABLET ORAL 10188652 Oct. 21, 2035 TREATMENT OF ADULT PATIENTS WITH INSOMNIA, CHARACTERIZED BY DIFFICULTIES WITH SLEEP ONSET AND/OR SLEEP MAINTENANCE
5MG DAYVIGO EISAI INC N212028 April 7, 2020 RX TABLET ORAL 10188652 Oct. 21, 2035 TREATMENT OF ADULT PATIENTS WITH INSOMNIA, CHARACTERIZED BY DIFFICULTIES WITH SLEEP ONSET AND/OR SLEEP MAINTENANCE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG DAYVIGO EISAI INC N212028 April 7, 2020 RX TABLET ORAL April 7, 2025 NEW CHEMICAL ENTITY
5MG DAYVIGO EISAI INC N212028 April 7, 2020 RX TABLET ORAL April 7, 2025 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Orexin receptor type 1 GPCR ANTAGONIST Ki 8.22 DRUG LABEL DRUG LABEL
Orexin receptor type 2 GPCR ANTAGONIST Ki 8.52 DRUG LABEL DRUG LABEL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.21 CHEMBL

External reference:

IDSource
4039370 VANDF
NRK PDB_CHEM_ID
CHEMBL3545367 ChEMBL_ID
D11022 KEGG_DRUG
C000634104 MESH_SUPPLEMENTAL_RECORD_UI
9302 IUPHAR_LIGAND_ID
9988 INN_ID
DB11951 DRUGBANK_ID
0K5743G68X UNII
56944144 PUBCHEM_CID
2272403 RXNORM
838465007 SNOMEDCT_US
838492001 SNOMEDCT_US
334297 MMSL
38462 MMSL
d09561 MMSL
018242 NDDF
C4519269 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DAYVIGO HUMAN PRESCRIPTION DRUG LABEL 1 62856-405 TABLET, FILM COATED 5 mg ORAL NDA 33 sections
DAYVIGO HUMAN PRESCRIPTION DRUG LABEL 1 62856-410 TABLET, FILM COATED 10 mg ORAL NDA 33 sections
DAYVIGO HUMAN PRESCRIPTION DRUG LABEL 1 62856-455 TABLET, FILM COATED 5 mg ORAL NDA 33 sections