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

Stem definition	Drug id	CAS RN
orexin receptor antagonists	5360	1369764-02-2

Description:

Molecule	Description
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: 3.99 LIPINSKI: 0 HAC: 6 HDO: 1 TPSA: 77 ALOGS: -4.57 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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: 3.99
LIPINSKI: 0
HAC: 6
HDO: 1
TPSA: 77
ALOGS: -4.57
ROTB: 6

Status: ONP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 20, 2019	FDA	EISAI INC
Jan. 23, 2020	PMDA	Eisai Co., Ltd

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sleep paralysis	279.06	41.21	36	530	624	63487832
Nightmare	57.00	41.21	16	550	19178	63469278

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sleep paralysis	108.79	34.75	14	406	170	34956341
Nightmare	70.89	34.75	19	401	14372	34942139
Abnormal dreams	51.79	34.75	13	407	7565	34948946

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sleep paralysis	154.77	28.88	22	880	616	79742870
Nightmare	56.62	28.88	18	884	25843	79717643
Pneumonia aspiration	33.69	28.88	16	886	66951	79676535
Altered state of consciousness	33.37	28.88	14	888	43808	79699678
Abnormal dreams	29.37	28.88	9	893	11403	79732083

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05CM21	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Other hypnotics and sedatives
FDA EPC	N0000191000	Orexin Receptor Antagonist
FDA MoA	N0000187064	Cytochrome P450 2B6 Inducers
FDA MoA	N0000190998	Orexin Receptor Antagonists
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

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Insomnia	indication	193462001
Narcolepsy	contraindication	60380001	DOID:8986

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.22	acidic
pKa2	4.56	Basic
pKa3	1.71	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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
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	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	10188652	Oct. 21, 2035	TREATMENT OF ADULT PATIENTS WITH INSOMNIA, CHARACTERIZED BY DIFFICULTIES WITH SLEEP ONSET AND/OR SLEEP MAINTENANCE

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG	DAYVIGO	EISAI INC	N212028	April 7, 2020	RX	TABLET	ORAL	April 7, 2025	NEW CHEMICAL ENTITY
10MG	DAYVIGO	EISAI INC	N212028	April 7, 2020	RX	TABLET	ORAL	April 20, 2026	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY E2006-A001-113
5MG	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 20, 2026	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY E2006-A001-113

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Orexin receptor type 1	GPCR	O43613	OX1R_HUMAN	ANTAGONIST	Ki	8.22	DRUG LABEL	DRUG LABEL
Orexin receptor type 2	GPCR	O43614	OX2R_HUMAN	ANTAGONIST	Ki	8.52	DRUG LABEL	DRUG LABEL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.21	CHEMBL

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External reference:

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ID	Source
018242	NDDF
0K5743G68X	UNII
2272403	RXNORM
334297	MMSL
38462	MMSL
4039370	VANDF
56944144	PUBCHEM_CID
838465007	SNOMEDCT_US
838492001	SNOMEDCT_US
9302	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-405	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-405	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-405	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-410	TABLET, FILM COATED	10 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-410	TABLET, FILM COATED	10 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-410	TABLET, FILM COATED	10 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-455	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-455	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections
DAYVIGO	HUMAN PRESCRIPTION DRUG LABEL	1	62856-455	TABLET, FILM COATED	5 mg	ORAL	NDA	36 sections

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