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Brexanolone

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Also known as AllopregnanoloneAllotetrahydroprogesteroneBrexanolonaSAGE-547SGE-102ZulressoSID50106899SID90341306SID26756639SID50106900SID144205595

Summary

Brexanolone (CHEMBL207538) is an approved small-molecule antidepressant (ATC N06AX29) targeting GABRA1, GABRA2, and GABRA3; indicated across 12 conditions including postpartum depression and depressive disorder.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: N06AX29
  • Targets: 6 (GABRA1, GABRA2, GABRA3…)
  • Indications: 12 conditions
  • Clinical trials: 24
  • Chemistry: 318.5 Da · C21H34O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL207538
NameBrexanolone
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID92786
ChEBICHEBI:50169
ATCN06AX29
Molecular formulaC21H34O2
Molecular weight318.5
InChIKeyAURFZBICLPNKBZ-SYBPFIFISA-N

SMILES: CC(=O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC[C@@H]4[C@@]3(CC[C@H](C4)O)C)C

IUPAC name: 1-[(3R,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone

ChEBI definition: A 3-hydroxy-5α-pregnan-20-one in which the hydroxy group at position 3 has α-configuration. It is a metabolite of the sex hormone progesterone and used for the treatment of postpartum depression in women.

Pharmacological roles (ChEBI): antidepressant, GABA modulator, intravenous anaesthetic, sedative.

Other ChEBI roles (chemical / environmental): human metabolite.

Also known as: Allopregnanolone, Allotetrahydroprogesterone, Brexanolona, Brexanolone, SAGE-547, SGE-102, Zulresso, allopregnanolone, SID50106899, SID90341306, SID26756639, SID50106900

Patent coverage: 573 distinct patent families (1,585 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
GABRA1GABAA receptor α1 subunitPotentiation0%P14867
GABRA2GABAA receptor α2 subunitPotentiation0%P47869
GABRA3GABAA receptor α3 subunitPotentiation0%P34903
GABRA4GABAA receptor α4 subunitPotentiation0%P48169
GABRA5GABAA receptor α5 subunitPotentiation0.9%P31644
GABRA6GABAA receptor α6 subunitPotentiation0.1%Q16445

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Prelamin-A/C, RecQ-like DNA helicase BLM, Geminin, Peripheral myelin protein 22, GABA-A receptor; anion channel, Menin/Histone-lysine N-methyltransferase MLL, GABA-A receptor; anion channel, GABA-A receptor; anion channel, GABA-A receptor; alpha-1/beta-2/gamma-2, GABA-A receptor; agonist GABA site.

Bioactivity

ChEMBL activities: 21 potent at pChembl ≥ 5 of 27 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
GABRP7.66IC5022nMCHEMBL_ACT_15244146
O090287.29IC5051nMCHEMBL_ACT_1171552
O090287.13IC5074nMCHEMBL_ACT_1505991
O090287.13IC5074nMCHEMBL_ACT_1741102
O090287.13IC5074nMCHEMBL_ACT_624392
O090287.13IC5074nMCHEMBL_ACT_962756
GABRA17.12EC5075.5nMCHEMBL_ACT_15244890
GABRD7.12EC5075.5nMCHEMBL_ACT_18187276
O090287.1IC5080nMCHEMBL_ACT_25107070
O090287.1IC5080nMCHEMBL_ACT_388961
O090287.07IC5086nMCHEMBL_ACT_25107066
O090287.04IC5091nMCHEMBL_ACT_693976
O090286.81IC50155nMCHEMBL_ACT_608104
GABRA16.8EC50160nMCHEMBL_ACT_1171554
GABRA16.62EC50237nMCHEMBL_ACT_15244128
GABRA16.62EC50237nMCHEMBL_ACT_18187234
P163056.06EC50871nMCHEMBL_ACT_1718849
O090285.58IC502610nMCHEMBL_ACT_388960
NPSR15.5Potency3162nMCHEMBL_ACT_4897194
MEN15.1Potency7943nMCHEMBL_ACT_4567726
GMNN5Potency10000nMCHEMBL_ACT_5065138

Target pathways

Aggregated over 6 target gene(s): GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6.

Top Reactome pathways

2 total, by targets touching each:

PathwayTargetsGenes
GABA receptor activation6GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
Signaling by ERBB41GABRA1

Dominant GO biological processes

GO termTargets
gamma-aminobutyric acid signaling pathway6
synaptic transmission, GABAergic6
chloride transmembrane transport6
inhibitory synapse assembly6
monoatomic ion transport6
chloride transport6
monoatomic ion transmembrane transport6
regulation of postsynaptic membrane potential6
regulation of presynaptic membrane potential2
signal transduction2
central nervous system development1
behavioral fear response1
associative learning1
inner ear receptor cell development1
innervation1

Indications & clinical

Indications

12 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
postpartum depression4MONDO:0005929EFO:0007453
depressive disorder4MONDO:0002050MONDO:0002050
essential tremor2MONDO:0003233EFO:0003108
brain injury2MONDO:0043510MONDO:0043510
post-traumatic stress disorder2MONDO:0005146EFO:0001358
Alzheimer disease2MONDO:0004975MONDO:0004975
alcohol abuse1MONDO:0002046MONDO:0007079
Parkinson disease1MONDO:0005180MONDO:0005180
psychotic disorder0MONDO:0005485EFO:0005407

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 24.

Phase distribution

PhaseTrials
PHASE29
PHASE35
PHASE14
PHASE42
Not specified2
PHASE1/PHASE21
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04273191PHASE4WITHDRAWNA Study to Evaluate Multimodal Neuroimaging Parameters in Women With Postpartum Depression Who Are Receiving ZULRESSO™ (Brexanolone)
NCT05329779PHASE4TERMINATEDStudy on Allopregnanolone and Depression in Perimenopausal Women
NCT02477618PHASE3COMPLETEDA Study With SAGE-547 for Super-Refractory Status Epilepticus
NCT02942004PHASE3COMPLETEDA Study to Evaluate Efficacy and Safety of SAGE-547 in Participants With Severe Postpartum Depression (547-PPD-202B)
NCT02942017PHASE3COMPLETEDA Study to Evaluate Safety and Efficacy of SAGE-547 in Participants With Moderate Postpartum Depression (547-PPD-202C)
NCT03665038PHASE3COMPLETEDA Study to Assess the Safety of Brexanolone in the Treatment of Adolescent Female Participants With Postpartum Depression (PPD)
NCT04537806PHASE3TERMINATEDA Study of Brexanolone for Acute Respiratory Distress Syndrome (ARDS) Due to Coronavirus Disease 2019 (COVID-19)
NCT04003285PHASE2NOT_YET_RECRUITINGAllopregnanolone in Chronic Complex Traumatic Brain Injury
NCT04838301PHASE2RECRUITINGAllopregnanolone Regenerative Therapeutic for Mild Alzheimer’s Disease
NCT06580444PHASE2NOT_YET_RECRUITINGBrexanolone to Target Concurrent PTSD and Stress Induced Alcohol Use in Veterans: A Dose Finding Study
NCT01673828PHASE2COMPLETEDAllopregnanolone for the Treatment of Traumatic Brain Injury
NCT02052739PHASE1/PHASE2COMPLETEDStudy to Evaluate SAGE-547 Injection as Adjunctive Therapy for the Treatment of Super-Refractory Status Epilepticus
NCT02277106PHASE2COMPLETEDEvaluate SAGE-547 in Participants With Essential Tremor
NCT02285504PHASE2COMPLETEDEvaluate SAGE-547 in Female Participants With Severe Postpartum Depression
NCT02603926PHASE2COMPLETEDTreatment of Fragile-X Associated Tremor/Ataxia Syndrome (FXTAS) With Allopregnanolone
NCT02614547PHASE2COMPLETEDA Study to Evaluate SAGE-547 in Participants With Severe Postpartum Depression
NCT05645432PHASE2COMPLETEDAn Open-Label Study Evaluating Brexanolone in Adults With Tinnitus
NCT05223829PHASE1ACTIVE_NOT_RECRUITINGUtility of Brexanolone to Target Stress-induced Alcohol Use Among Men and Women With Posttraumatic Stress Disorder
NCT03748303PHASE1TERMINATEDAllopregnanolone Regenerative Therapeutic for Early Alzheimer’s Disease: Intramuscular Study
NCT04015869PHASE1COMPLETEDEffect of Allopregnanolone on Stress-induced Craving
NCT06263010PHASE1COMPLETEDAllopregnanolone as a Regenerative Treatment for Parkinson’s Disease
NCT05314153EARLY_PHASE1COMPLETEDEffects Zulresso on Postpartum Psychosis
NCT02433314Not specifiedNO_LONGER_AVAILABLEAn Open Label, Expanded Access Protocol With SAGE-547 for Super-Refractory Status Epilepticus
NCT05543746Not specifiedCOMPLETEDDynamic Neural Mechanisms of Brexanolone-induced Antidepressant Effects in Postpartum Depression

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

81 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
APALUTAMIDEChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
CLONAZEPAMChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
DIAZEPAMChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
ENZALUTAMIDEChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
FLUMAZENILChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
GANAXOLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
LIOTHYRONINEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
PROPOFOLChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
ALFAXALONEChEMBL + PubChemPhase 2 (approved)GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
ABECARNILChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
BAICALEINChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
DELORAZEPAMChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
FLAVONEChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
PROGABIDEChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6
BRETAZENILChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5, GABRA6
ALPRAZOLAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
CHLORDIAZEPOXIDEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
ESZOPICLONEChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA4
FLUNITRAZEPAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
TRIAZOLAMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3, GABRA5
AZD7325ChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
BASMISANILChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
MK-0777ChEMBLPhase 2GABRA1, GABRA2, GABRA3, GABRA5
ZOLPIDEMChEMBLPhase 4 (approved)GABRA1, GABRA2, GABRA3
DARIGABATChEMBLPhase 2GABRA1, GABRA3, GABRA5
PANADIPLONChEMBLPhase 2GABRA1, GABRA3, GABRA6
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)GABRA1, GABRA2
ASENAPINEChEMBLPhase 4 (approved)GABRA1, GABRA2
AZELASTINEChEMBLPhase 4 (approved)GABRA1, GABRA2
BENPERIDOLChEMBLPhase 4 (approved)GABRA1, GABRA2
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)GABRA1, GABRA2
CHLORAMBUCILChEMBLPhase 4 (approved)GABRA1, GABRA2
CLOZAPINEChEMBLPhase 4 (approved)GABRA1, GABRA2
EPINASTINEChEMBLPhase 4 (approved)GABRA1, GABRA2
ETOMIDATEChEMBLPhase 4 (approved)GABRA1, GABRA2
GLAFENINEChEMBLPhase 4 (approved)GABRA1, GABRA2
LINDANEChEMBLPhase 4 (approved)GABRA1, GABRA6
SIMVASTATINChEMBLPhase 4 (approved)GABRA1, GABRA2
TIPRANAVIRChEMBLPhase 4 (approved)GABRA1, GABRA2
TROGLITAZONEChEMBLPhase 4 (approved)GABRA1, GABRA2
ZALEPLONChEMBLPhase 4 (approved)GABRA1, GABRA2
ZURANOLONEChEMBLPhase 4 (approved)GABRA1, GABRA4
SURAMINChEMBLPhase 3GABRA1, GABRA2
TIRATRICOLChEMBLPhase 3GABRA1, GABRA2
SARIPIDEMChEMBLPhase 2GABRA1, GABRA5
ZOTEPINEChEMBLPhase 2GABRA1, GABRA2
.gamma.-aminobutyric acidPubChemApprovedGABRA4, GABRA6
AfatinibPubChemApprovedGABRA1, GABRA2
ApixabanPubChemApprovedGABRA1, GABRA2
BinimetinibPubChemApprovedGABRA1, GABRA2
CaffeinePubChemApprovedGABRA4, GABRA6
chenodiolPubChemApprovedGABRA1, GABRA2
CiprofloxacinPubChemApprovedGABRA4, GABRA6
FipronilPubChemApprovedGABRA4, GABRA6
FulvestrantPubChemApprovedGABRA1, GABRA2
gentian violetPubChemApprovedGABRA1, GABRA2
ImipenemPubChemApprovedGABRA1, GABRA2
LactulosePubChemApprovedGABRA1, GABRA2
levocarnitinePubChemApprovedGABRA1, GABRA2
PhenytoinPubChemApprovedGABRA4, GABRA6

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot