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 |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.03 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 20, 2019 | FDA | EISAI INC | |
| Jan. 23, 2020 | PMDA | Eisai Co., Ltd |
FDA Adverse Event Reporting System (Female)
| 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 |
FDA Adverse Event Reporting System (Male)
| 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 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 |
| FDA MoA | N0000187064 | Cytochrome P450 2B6 Inducers |
| FDA MoA | N0000190998 | Orexin Receptor Antagonists |
| FDA EPC | N0000191000 | Orexin Receptor Antagonist |
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)
| 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 |
| 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 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 |
| 5MG | 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 20, 2026 | REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY E2006-A001-113 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| NRK | PDB_CHEM_ID |
| CHEMBL3545367 | ChEMBL_ID |
| D11022 | KEGG_DRUG |
| C000634104 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9302 | IUPHAR_LIGAND_ID |
| DB11951 | DRUGBANK_ID |
| 018242 | NDDF |
| 838465007 | SNOMEDCT_US |
| 838492001 | SNOMEDCT_US |
| 4039370 | VANDF |
| C4519269 | UMLSCUI |
| 9988 | INN_ID |
| 56944144 | PUBCHEM_CID |
| 2272403 | RXNORM |
| 334297 | MMSL |
| 38462 | MMSL |
| d09561 | MMSL |
| 0K5743G68X | UNII |
Pharmaceutical products:
| 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 |