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brexanolone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids not used as glucocorticosteroids | 5324 | 516-54-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Brexanolone is a neuroactive steroid gamma-aminobutyric acid (GABA) A receptor positive modulator indicated for the treatment of postpartum depression (PPD) in adults.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1 | 17 | |||
| kinase-selectivity-class | EIF2AK3 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 19, 2019 | FDA | SAGE THERAPEUTICS |
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 |
|---|---|---|---|---|---|---|
| Drug monitoring procedure incorrectly performed | 118.09 | 68.37 | 13 | 137 | 330 | 90627967 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Drug monitoring procedure incorrectly performed | 112.77 | 65.00 | 13 | 109 | 770 | 110588407 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AX29 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants |
| MeSH PA | D000081227 | Neurosteroids |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D018757 | GABA Modulators |
| FDA MoA | N0000193997 | GABA A Receptor Positive Modulators |
| FDA EPC | N0000194006 | Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator |
| CHEBI has role | CHEBI:35469 | antidepressant |
| CHEBI has role | CHEBI:35717 | sedative |
| CHEBI has role | CHEBI:38877 | intravenous anaesthetic |
| CHEBI has role | CHEBI:50268 | GABA modulator |
| CHEBI has role | CHEBI:77746 | human metabolite |
Related Drugs by ATC class:
N06AX Other antidepressants 28 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Postpartum depression | indication | 58703003 | DOID:9478 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG/20ML (5MG/ML) | ZULRESSO | SAGE THERAP SUPERNUS | N211371 | June 17, 2019 | DISCN | SOLUTION | INTRAVENOUS | 10251894 | Nov. 27, 2033 | METHOD OF TREATING POSTPARTUM DEPRESSION |
| 100MG/20ML (5MG/ML) | ZULRESSO | SAGE THERAP SUPERNUS | N211371 | June 17, 2019 | DISCN | SOLUTION | INTRAVENOUS | 10940156 | March 8, 2037 | METHOD OF TREATING POSTPARTUM DEPRESSION |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Glucose-6-phosphate 1-dehydrogenase | Enzyme | IC50 | 4.18 | CHEMBL | |||||
| GABA-A receptor alpha-1/beta-2/gamma-2 | Ion channel | POSITIVE ALLOSTERIC MODULATOR | EC50 | 7.22 | DRUG LABEL | ||||
| GABA A receptor alpha-4/beta-3/delta | Ion channel | POSITIVE ALLOSTERIC MODULATOR | EC50 | 7.10 | DRUG LABEL | ||||
| GABA-A receptor alpha-6/beta-3/delta | Ion channel | POSITIVE ALLOSTERIC MODULATOR | EC50 | 6.81 | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| S39XZ5QV8Y | UNII |
| 4038491 | VANDF |
| C4548848 | UMLSCUI |
| CHEBI:50169 | CHEBI |
| Y4B | PDB_CHEM_ID |
| CHEMBL207538 | ChEMBL_ID |
| 92786 | PUBCHEM_CID |
| DB11859 | DRUGBANK_ID |
| D11149 | KEGG_DRUG |
| 10446 | INN_ID |
| C000625635 | MESH_SUPPLEMENTAL_RECORD_UI |
| C584548 | MESH_SUPPLEMENTAL_RECORD_UI |
| 787054008 | SNOMEDCT_US |
| 787064004 | SNOMEDCT_US |
| 36584 | MMSL |
| d09319 | MMSL |
| 017976 | NDDF |
| 2121777 | RXNORM |
Pharmaceutical products:
None