Cariprazine

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Cariprazine is an onp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 2015. DrugCentral lists 30 molecular targets, including DRD3, DRD2 and HTR2B. Recorded indications include Bipolar affective disorder, current episode manic, Mixed bipolar I disorder and Schizophrenia.

• Approval status: onp (first approved 2015 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: DRD3, DRD2, HTR2B and Drd3 (30 listed in DrugCentral).
• Indications: Bipolar affective disorder, current episode manic, Mixed bipolar I disorder and Schizophrenia.
• ATC code: N05AX15 (Other antipsychotics).
• Molecular formula: C21H32Cl2N4O; molecular weight 427.41 g/mol.

Indications & contraindications

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

Indications (3)

• Bipolar affective disorder, current episode manic
• Mixed bipolar I disorder
• Schizophrenia

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (30)

Target	Gene	Action	Activity
D(3) dopamine receptor	DRD3	partial agonist	Ki 10.07
D(2) dopamine receptor	DRD2	partial agonist	Ki 9.31
5-hydroxytryptamine receptor 2B	HTR2B	antagonist	Ki 9.24
D(3) dopamine receptor	Drd3	unknown	IC50 8.80
5-hydroxytryptamine receptor 1A	HTR1A	partial agonist	Ki 8.59
D(2) dopamine receptor	Drd2	unknown	IC50 7.80
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 7.73
Histamine H1 receptor	HRH1	antagonist	Ki 7.63
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 7.11
D(4) dopamine receptor	DRD4	unknown	Ki 6.96
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 6.95
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 6.89
5-hydroxytryptamine receptor 2C	HTR2C	antagonist	Ki 6.87
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 6.68
Beta-1 adrenergic receptor	ADRB1	unknown	Ki 6.65
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 6.63
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 6.62
Transmembrane protein 97	TMEM97	unknown	Ki 6.31
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 6.11
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 5.96

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2015-09-17	FDA	—	FOREST LABS LLC

ATC classification

ATC code	Therapeutic hierarchy
N05AX15	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Other antipsychotics

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: CYP2D6
• FDA label: CYP2D6 · No Clinical PGx
• HCSC label: CYP2D6 · No Clinical 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	1129.1
Tardive dyskinesia	955.8
Extrapyramidal disorder	393.7
Suicidal ideation	326.9
Weight increased	221.0
Tremor	219.7
Mania	208.5
Hallucination, auditory	202.0
Parkinsonism	179.4
Sedation	170.7
Dyskinesia	164.2
Restlessness	143.5

Chemical structure

• Molecular formula: C₂₁H₃₂Cl₂N₄O
• Molecular weight: 427.41 g/mol
• CAS number: 839712-12-8
• InChIKey: KPWSJANDNDDRMB-QAQDUYKDSA-N
• PubChem CID: 11154555

CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCN(CC2)C2=C(Cl)C(Cl)=CC=C2)CC1

Frequently asked questions

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

What is Cariprazine used for?

DrugCentral lists the following indications for Cariprazine: Bipolar affective disorder, current episode manic, Mixed bipolar I disorder and Schizophrenia.

How does Cariprazine work?

Its molecular targets in DrugCentral include DRD3 (partial agonist), DRD2 (partial agonist), HTR2B (antagonist) and Drd3.

When was Cariprazine first approved?

Cariprazine was first approved by the FDA in 2015.

What drug class does Cariprazine belong to?

Cariprazine is in the Atypical Antipsychotic class.

What is the chemical formula of Cariprazine?

Cariprazine has the molecular formula C21H32Cl2N4O and a molecular weight of 427.41 g/mol.

Sources

• DrugCentral drug card 5037 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2024517 — compound record and bioactivity
• PubChem CID 11154555 — chemical identifiers
• DrugBank DB06016 — drug record
• FDA UNII F6RJL8B278 — substance identity
• DailyMed: FDA labels for Cariprazine — current prescribing information (label search)
• UniProt P35462 (DRD3) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P08908 (HTR1A) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P35367 (HRH1) — 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.