Pimozide

Typical Antipsychotic — NERVOUS SYSTEM

Key facts

Pimozide is an ofp drug in the Typical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 1984. DrugCentral lists 41 molecular targets, including Drd1|Drd3|Drd5|Drd4|Drd2, HTR7 and Htr7. Recorded indications include Gilles de la Tourette's syndrome.

• Approval status: ofp (first approved 1984 by the FDA).
• Drug class: Typical Antipsychotic.
• Molecular targets: Drd1|Drd3|Drd5|Drd4|Drd2, HTR7, Htr7 and DRD2 (41 listed in DrugCentral).
• Indications: Gilles de la Tourette's syndrome.
• ATC code: N05AG02 (Diphenylbutylpiperidine derivatives).
• Molecular formula: C28H29F2N3O; molecular weight 461.56 g/mol.

Indications & contraindications

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

Indications (1)

• Gilles de la Tourette's syndrome

Contraindications (24)

• Agranulocytosis
• Benign prostatic hyperplasia
• Carcinoma of female breast
• Coma
• Conduction disorder of the heart
• Congenital long QT syndrome
• Disease of liver
• Drug Induced CNS Depression
• Glaucoma
• Hyperprolactinemia
• Hypokalemia
• Hypomagnesemia
• Kidney disease
• Leukopenia
• Motor tic disorder
• Neuroleptic malignant syndrome
• Neutropenic disorder
• Parkinsonism
• Prolonged QT interval
• Retention of urine
• Seizure disorder
• Senile dementia
• Tardive dyskinesia
• Torsades de pointes

Mechanism & targets

• Established pharmacologic class: Typical Antipsychotic

Molecular targets (41)

Target	Gene	Action	Activity
Dopamine receptor	Drd1|Drd3|Drd5|Drd4|Drd2	unknown	IC50 9.40
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 9.30
5-hydroxytryptamine receptor 7	Htr7	unknown	Ki 9.30
D(2) dopamine receptor	DRD2	unknown	Ki 9.22
D(3) dopamine receptor	DRD3	antagonist	Ki 9.05
D(2) dopamine receptor	DRD2	antagonist	Ki 8.86
D(4) dopamine receptor	DRD4	antagonist	Ki 8.74
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 7.75
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 7.56
Voltage-dependent T-type calcium channel subunit alpha-1G	Cacna1g	blocker	IC50 7.50
Voltage-dependent T-type calcium channel subunit alpha-1I	CACNA1I	blocker	IC50 7.50
Voltage-dependent T-type calcium channel subunit alpha-1G	CACNA1G	unknown	Kd 7.40
Voltage-dependent T-type calcium channel subunit alpha-1H	Cacna1h	blocker	IC50 7.30
5-hydroxytryptamine receptor 6	Htr6	antagonist	Ki 7.20
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 7.15
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 6.84
Voltage-dependent T-type calcium channel subunit alpha-1H	CACNA1H	blocker	IC50 6.80
Histamine H1 receptor	HRH1	unknown	Ki 6.71
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 6.70
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 6.63

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1984-07-31	FDA	—	TEVA

ATC classification

ATC code	Therapeutic hierarchy
N05AG02	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diphenylbutylpiperidine derivatives

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• FDA label: CYP2D6 · Testing Required
• HCSC label: CYP2D6

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
Parkinsonism	159.5
Atrioventricular septal defect	139.4
Drug interaction	107.3
Neuroleptic malignant syndrome	104.1
Dysmorphism	92.5
Dystonia	75.1
Placental infarction	72.0
Hypertelorism	68.2
Craniosynostosis	51.7
Congenital central nervous system anomaly	51.0
Tic	48.1
Hallucination	45.9

Chemical structure

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

• Molecular formula: C₂₈H₂₉F₂N₃O
• Molecular weight: 461.56 g/mol
• CAS number: —
• InChIKey: YVUQSNJEYSNKRX-UHFFFAOYSA-N
• PubChem CID: 16362

FC1=CC=C(C=C1)C(CCCN1CCC(CC1)N1C(=O)NC2=C1C=CC=C2)C1=CC=C(F)C=C1

Frequently asked questions

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

What is Pimozide used for?

DrugCentral lists the following indications for Pimozide: Gilles de la Tourette's syndrome.

How does Pimozide work?

Its molecular targets in DrugCentral include Drd1|Drd3|Drd5|Drd4|Drd2, HTR7, Htr7 and DRD2.

When was Pimozide first approved?

Pimozide was first approved by the FDA in 1984.

What drug class does Pimozide belong to?

Pimozide is in the Typical Antipsychotic class.

What is the chemical formula of Pimozide?

Pimozide has the molecular formula C28H29F2N3O and a molecular weight of 461.56 g/mol.

Sources

• DrugCentral drug card 2172 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1423 — compound record and bioactivity
• PubChem CID 16362 — chemical identifiers
• DrugBank DB01100 — drug record
• FDA UNII 1HIZ4DL86F — substance identity
• DailyMed: FDA labels for Pimozide — current prescribing information (label search)
• UniProt P34969 (HTR7) — target protein
• UniProt P35462 (DRD3) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P21917 (DRD4) — target protein
• UniProt Q12809 (KCNH2) — target protein
• UniProt P28223 (HTR2A) — 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.