Brexpiprazole

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Brexpiprazole is an ofp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 2015. DrugCentral lists 34 molecular targets, including Htr1a, HTR1A and ADRA1B. Recorded indications include Major depressive disorder and Schizophrenia.

• Approval status: ofp (first approved 2015 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: Htr1a, HTR1A, ADRA1B and Drd2 (34 listed in DrugCentral).
• Indications: Major depressive disorder and Schizophrenia.
• ATC code: N05AX16 (Other antipsychotics).
• Molecular formula: C25H27N3O2S; molecular weight 433.57 g/mol.

Indications & contraindications

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

Indications (2)

• Major depressive disorder
• Schizophrenia

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (34)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 1A	Htr1a	unknown	Ki 10.05
5-hydroxytryptamine receptor 1A	HTR1A	agonist	Ki 9.92
Alpha-1B adrenergic receptor	ADRA1B	antagonist	Ki 9.77
D(2) dopamine receptor	Drd2	unknown	Ki 9.70
D(2) dopamine receptor	DRD2	agonist	Ki 9.52
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 9.33
Alpha-2C adrenergic receptor	ADRA2C	antagonist	Ki 9.23
D(3) dopamine receptor	DRD3	agonist	Ki 8.96
5-hydroxytryptamine receptor 2B	HTR2B	antagonist	Ki 8.72
5-hydroxytryptamine receptor 2A	Htr2a	unknown	Ki 8.64
Alpha-1D adrenergic receptor	ADRA1D	antagonist	Ki 8.59
5-hydroxytryptamine receptor 7	HTR7	antagonist	Ki 8.43
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 8.42
D(4) dopamine receptor	DRD4	agonist	Ki 8.20
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 7.82
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 7.77
Histamine H1 receptor	HRH1	antagonist	Ki 7.72
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 7.62
Sodium-dependent serotonin transporter	SLC6A4	inhibitor	IC50 7.54
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 7.50

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2018-07-27	EMA	—	OTSUKA PHARM CO LTD
2018-01-19	PMDA	—	Otsuka Pharmaceutical Co., Ltd.
2015-07-10	FDA	—	OTSUKA PHARM CO LTD

ATC classification

ATC code	Therapeutic hierarchy
N05AX16	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Other antipsychotics

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2D6 · Actionable PGx
• FDA label: CYP2D6 · Actionable PGx
• HCSC label: CYP2D6 · Actionable PGx
• Swissmedic label: CYP2D6 · Actionable PGx

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
Akathisia	1647.5
Tardive dyskinesia	1099.5
Weight increased	753.1
Schizoaffective disorder	693.4
Suicidal ideation	552.9
Product use in unapproved indication	426.5
Hallucination, auditory	373.5
Drug level increased	316.9
Electrocardiogram QT prolonged	298.0
Tremor	292.9
Extrapyramidal disorder	291.5
Restlessness	274.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Brexpiprazole is on its molecule page.

• Molecular formula: C₂₅H₂₇N₃O₂S
• Molecular weight: 433.57 g/mol
• CAS number: 913611-97-9
• InChIKey: ZKIAIYBUSXZPLP-UHFFFAOYSA-N
• PubChem CID: 11978813

O=C1NC2=C(C=C1)C=CC(OCCCCN1CCN(CC1)C1=C3C=CSC3=CC=C1)=C2

Frequently asked questions

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

What is Brexpiprazole used for?

DrugCentral lists the following indications for Brexpiprazole: Major depressive disorder and Schizophrenia.

How does Brexpiprazole work?

Its molecular targets in DrugCentral include Htr1a, HTR1A (agonist), ADRA1B (antagonist) and Drd2.

When was Brexpiprazole first approved?

Brexpiprazole was first approved by the FDA in 2015.

What drug class does Brexpiprazole belong to?

Brexpiprazole is in the Atypical Antipsychotic class.

What is the chemical formula of Brexpiprazole?

Brexpiprazole has the molecular formula C25H27N3O2S and a molecular weight of 433.57 g/mol.

Sources

• DrugCentral drug card 5014 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2105760 — compound record and bioactivity
• PubChem CID 11978813 — chemical identifiers
• DrugBank DB09128 — drug record
• FDA UNII 2J3YBM1K8C — substance identity
• DailyMed: FDA labels for Brexpiprazole — current prescribing information (label search)
• UniProt P08908 (HTR1A) — target protein
• UniProt P35368 (ADRA1B) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P18825 (ADRA2C) — target protein
• UniProt P35462 (DRD3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

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