Brexanolone

Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator — NERVOUS SYSTEM

Key facts

Brexanolone is an ofm drug in the Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator class catalogued in DrugCentral. It was first approved by the FDA in 2019. Its mechanism of action is classified as GABA A Receptor Positive Modulators. DrugCentral lists 4 molecular targets, including GABRA1|GABRG2|GABRB2, GABRA4|GABRB3|GABRD and GABRA6|GABRB3|GABRD. Recorded indications include Postpartum depression.

• Approval status: ofm (first approved 2019 by the FDA).
• Drug class: Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator.
• Mechanism of action: GABA A Receptor Positive Modulators.
• Molecular targets: GABRA1|GABRG2|GABRB2, GABRA4|GABRB3|GABRD, GABRA6|GABRB3|GABRD and G6PD (4 listed in DrugCentral).
• Indications: Postpartum depression.
• ATC code: N06AX29 (Other antidepressants).
• Molecular formula: C21H34O2; molecular weight 318.50 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Postpartum depression

Mechanism & targets

• Mechanism of action (MoA): GABA A Receptor Positive Modulators
• Established pharmacologic class: Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator

Molecular targets (4)

Target	Gene	Action	Activity
GABA-A receptor alpha-1/beta-2/gamma-2	GABRA1|GABRG2|GABRB2	positive allosteric modulator	EC50 7.22
GABA A receptor alpha-4/beta-3/delta	GABRA4|GABRB3|GABRD	positive allosteric modulator	EC50 7.10
GABA-A receptor alpha-6/beta-3/delta	GABRA6|GABRB3|GABRD	positive allosteric modulator	EC50 6.81
Glucose-6-phosphate 1-dehydrogenase	G6PD	unknown	IC50 4.18

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2019-03-19	FDA	—	SAGE THERAPEUTICS

ATC classification

ATC code	Therapeutic hierarchy
N06AX29	NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTIDEPRESSANTS › Other antidepressants

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Drug monitoring procedure incorrectly performed	130.1
Product administration error	94.9

Chemical structure

• Molecular formula: C₂₁H₃₄O₂
• Molecular weight: 318.50 g/mol
• CAS number: 516-54-1
• InChIKey: AURFZBICLPNKBZ-ZMFJCIRDSA-N
• PubChem CID: 92786

CC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@]12C

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Brexanolone used for?

DrugCentral lists the following indications for Brexanolone: Postpartum depression.

How does Brexanolone work?

Brexanolone is classified as GABA A Receptor Positive Modulators; its molecular targets in DrugCentral include GABRA1|GABRG2|GABRB2 (positive allosteric modulator), GABRA4|GABRB3|GABRD (positive allosteric modulator), GABRA6|GABRB3|GABRD (positive allosteric modulator) and G6PD.

When was Brexanolone first approved?

Brexanolone was first approved by the FDA in 2019.

What drug class does Brexanolone belong to?

Brexanolone is in the Neuroactive Steroid Gamma-Aminobutyric Acid A Receptor Positive Modulator class.

What is the chemical formula of Brexanolone?

Brexanolone has the molecular formula C21H34O2 and a molecular weight of 318.50 g/mol.

Sources

• DrugCentral drug card 5324 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL207538 — compound record and bioactivity
• PubChem CID 92786 — chemical identifiers
• DrugBank DB11859 — drug record
• FDA UNII S39XZ5QV8Y — substance identity
• DailyMed: FDA labels for Brexanolone — current prescribing information (label search)
• UniProt P11413 (G6PD) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.