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

Stem definitionDrug idCAS RN
steroids not used as glucocorticosteroids 5324 516-54-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • brexanolone
  • zurlesso
  • SAGE-547
  • SGE-102
  • SGE-00122
Brexanolone is a neuroactive steroid gamma-aminobutyric acid (GABA) A receptor positive modulator indicated for the treatment of postpartum depression (PPD) in adults.
  • Molecular weight: 318.50
  • Formula: C21H34O2
  • CLOGP: 4.51
  • LIPINSKI: 1
  • HAC: 2
  • HDO: 1
  • TPSA: 37.30
  • ALOGS: -5.37
  • ROTB: 1

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
March 19, 2019 FDA SAGE THERAPEUTICS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N06AX29 NERVOUS SYSTEM
PSYCHOANALEPTICS
ANTIDEPRESSANTS
Other antidepressants
MeSH PA D018682 GABA Agents
MeSH PA D018757 GABA Modulators
MeSH PA D000081227 Neurosteroids
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:35469 antidepressants
CHEBI has role CHEBI:35717 hypnotics
CHEBI has role CHEBI:38877 intravenous anesthetics
CHEBI has role CHEBI:50268 GABA modulators
CHEBI has role CHEBI:77746 Homo sapiens metabolite
FDA MoA N0000193997 GABA A Receptor Positive Modulators
FDA EPC N0000194006 Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator

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

DiseaseRelationSNOMED_IDDOID
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG/20ML (5MG/ML) ZULRESSO SAGE THERAP N211371 June 17, 2019 RX SOLUTION INTRAVENOUS 10251894 Nov. 27, 2033 METHOD OF TREATING POSTPARTUM DEPRESSION
100MG/20ML (5MG/ML) ZULRESSO SAGE THERAP N211371 June 17, 2019 RX SOLUTION INTRAVENOUS 10940156 March 8, 2037 METHOD OF TREATING POSTPARTUM DEPRESSION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG/20ML (5MG/ML) ZULRESSO SAGE THERAP N211371 June 17, 2019 RX SOLUTION INTRAVENOUS June 17, 2024 NEW CHEMICAL ENTITY
100MG/20ML (5MG/ML) ZULRESSO SAGE THERAP N211371 June 17, 2019 RX SOLUTION INTRAVENOUS June 16, 2025 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
S39XZ5QV8Y UNII
C4548848 UMLSCUI
CHEBI:50169 CHEBI
CHEMBL207538 ChEMBL_ID
92786 PUBCHEM_CID
DB11859 DRUGBANK_ID
D11149 KEGG_DRUG
10446 INN_ID
C584548 MESH_SUPPLEMENTAL_RECORD_UI
017976 NDDF
787054008 SNOMEDCT_US
787064004 SNOMEDCT_US
4038491 VANDF
2121777 RXNORM
36584 MMSL
d09319 MMSL
C000625635 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Zulresso HUMAN PRESCRIPTION DRUG LABEL 1 72152-547 INJECTION, SOLUTION 5 mg INTRAVENOUS NDA 32 sections
Zulresso HUMAN PRESCRIPTION DRUG LABEL 1 72152-547 INJECTION, SOLUTION 5 mg INTRAVENOUS NDA 32 sections