Zuranolone

Summary

Zuranolone (CHEMBL4105630) is an approved small-molecule antidepressant (ATC N06AX31); indicated across 6 conditions including postpartum depression and depressive disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N06AX31
• Indications: 6 conditions
• Clinical trials: 15
• Chemistry: 409.6 Da · C25H35N3O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4105630
Name	Zuranolone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	86294073
ChEBI	CHEBI:228302
ATC	N06AX31
Molecular formula	C25H35N3O2
Molecular weight	409.6
InChIKey	HARRKNSQXBRBGZ-GVKWWOCJSA-N

SMILES: C[C@]1(CC[C@H]2[C@@H](C1)CC[C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@@H]4C(=O)CN5C=C(C=N5)C#N)C)O

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

ChEBI definition: A 3-hydroxy steroid that is 5β-19-norpregnane substituted by hydroxy, methyl, oxo, and 4-cyano-1H-pyrazol-1-yl groups at positions 3, 3, 20 and 21, respectively. It is a positive allosteric modulator of GABAA receptor developed by Sage Therapeutics and Biogen for the treatment of postpartum depression in adults.

Pharmacological roles (ChEBI): antidepressant, GABA modulator, anticonvulsant.

Also known as: S-812217, Sage-217, SAGE-217, SGE-797, Zuranolone, Zurzuvae, ZURANOLONE

Patent coverage: 113 distinct patent families (290 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

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: GABA-A receptor; anion channel, GABA-A receptor; alpha-1/beta-2/gamma-2, Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta, Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/delta.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
O09028	8.15	IC50	7	nM	CHEMBL_ACT_26107723
GABRD	6.87	EC50	135	nM	CHEMBL_ACT_26107756
GABRA1	6.82	EC50	152	nM	CHEMBL_ACT_26107607
GABRD	6.79	EC50	163	nM	CHEMBL_ACT_18566144
GABRD	6.52	EC50	299	nM	CHEMBL_ACT_18187278
GABRA1	6.43	EC50	375	nM	CHEMBL_ACT_18187236
GABRA1	6.43	EC50	374	nM	CHEMBL_ACT_18566145

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

6 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).

Indication	Trial phase	MONDO	EFO
postpartum depression	4	MONDO:0005929	EFO:0007453
depressive disorder	4	MONDO:0002050	MONDO:0002009
essential tremor	2	MONDO:0003233	EFO:0003108
Parkinson disease	2	MONDO:0005180	MONDO:0005180
mood disorder	1	MONDO:0005371	EFO:0004247

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

Clinical trials

Total trials: 15.

Phase distribution

Phase	Trials
PHASE3	7
PHASE2	5
Not specified	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03672175	PHASE3	COMPLETED	A Study to Evaluate the Efficacy of SAGE-217 in the Treatment of Adult Participants With Major Depressive Disorder
NCT03771664	PHASE3	TERMINATED	A Study to Evaluate the Safety, Tolerability, and Efficacy of SAGE-217 Compared to Placebo in Adult Participants With Comorbid Major Depressive Disorder (MDD) and Insomnia
NCT03864614	PHASE3	COMPLETED	A Study to Evaluate SAGE-217 in Adult Participants With Major Depressive Disorder (MDD)
NCT04007367	PHASE3	TERMINATED	A Study to Evaluate SAGE-217 for Prevention of Relapse in Adult Participants With Major Depressive Disorder
NCT04442490	PHASE3	COMPLETED	A Study to Evaluate the Efficacy of Sage-217 in the Treatment of Adult Participants With Major Depressive Disorder (MDD)
NCT04442503	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of SAGE-217 in Participants With Severe Postpartum Depression (PPD)
NCT04476030	PHASE3	COMPLETED	A Comparative Study of Sage-217 Plus an Antidepressant (ADT) Versus Placebo Plus an ADT in Adults With Major Depressive Disorder
NCT06759558	PHASE2	RECRUITING	Allopregnanolone (Zuranolone) in Post-stroke Depression
NCT02978781	PHASE2	COMPLETED	A Study to Evaluate SAGE-217 in Participants With Essential Tremor
NCT03000530	PHASE2	COMPLETED	A Study to Evaluate SAGE-217 in Participants With Moderate to Severe Major Depressive Disorder
NCT03000569	PHASE2	COMPLETED	A Study to Evaluate SAGE-217 in Participants With Parkinson’s Disease
NCT03692910	PHASE2	COMPLETED	A Study to Evaluate SAGE-217 in Participants With Bipolar I/II Disorder With a Current Major Depressive Episode
NCT05655507	PHASE1	COMPLETED	Zuranolone Pharmacokinetics (PK) and Safety Study Adolescent Participants With Major Depressive Disorder (MDD)
NCT07047820	Not specified	RECRUITING	A Study to Learn More About How Zuranolone Affects Postpartum Depression Symptoms in Participants Who Took it Within 1 Year After The End of Their Pregnancy
NCT07398469	Not specified	RECRUITING	A Long-Term Study of Patient-Reported Changes in Postpartum Depression Symptoms in People Starting Zuranolone

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).