pimozide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
2172 2062-78-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pimozide
  • primozide
  • R6238
  • R-6238
A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)
  • Molecular weight: 461.56
  • Formula: C28H29F2N3O
  • CLOGP: 6.40
  • LIPINSKI: 1
  • HAC: 4
  • HDO: 1
  • TPSA: 35.58
  • ALOGS: -5.43
  • ROTB: 7
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.01 mg/mL Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.31 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 40 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 4.415 Moderate 0.78
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.186 Moderate 0.78
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 11.858 10^-6 cm/s Moderate 0.78
dh-clint Dog hepatocyte intrinsic clearance 9.462 uL/min/10^6 cells Moderate 0.78
dppb Dog plasma protein binding (% unbound) 0.800 % Moderate 0.78
fcs-ppb Fetal calf serum protein binding (% unbound) 4.630 % Moderate 0.78
herg hERG pIC50 6.129 pIC50 Moderate 0.78
hh-clint Human hepatocyte intrinsic clearance 4.055 uL/min/10^6 cells Moderate 0.78
hlm-clint Human liver microsomal intrinsic clearance 38.637 uL/min/mg protein Moderate 0.78
hppb Human plasma protein binding (% unbound) 0.800 % Moderate 0.78
kinase-safety-class ACVR2B,AKT2,AKT3,ALK,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MARK4,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK 42
kinase-selectivity-class AKT2,AKT3,AXL,CAMK2D,GRK2,PRKCD,SIK2 7
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.530 Moderate 0.78
mh-clint Mouse hepatocyte intrinsic clearance 28.510 Moderate 0.78
mppb Mouse plasma protein binding (% unbound) 0.700 Moderate 0.78
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.312 Moderate 0.78
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 3.210 % Moderate 0.78
rh-clint Rat hepatocyte intrinsic clearance 56.624 uL/min/10^6 cells Moderate 0.78
rh-fuinc Rat hepatocyte fraction unbound in incubation 3.660 % Moderate 0.78
rppb Rat plasma protein binding (% unbound) 0.490 % Moderate 0.78
solubility-dd Solubility at pH 7.4 in DMSO 3.631 uM Moderate 0.78

Approvals:

DateAgencyCompanyOrphan
July 31, 1984 FDA TEVA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Parkinsonism 80.67 63.00 19 639 14046 90613743
Drug interaction 70.83 63.00 36 622 276417 90351372
Congenital central nervous system anomaly 69.82 63.00 10 648 464 90627325
Atrioventricular septal defect 64.59 63.00 9 649 342 90627447

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Parkinsonism 74.51 58.32 19 550 10604 42610162

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Parkinsonism 157.30 49.05 37 953 22150 110566159
Neuroleptic malignant syndrome 99.26 49.05 28 962 34031 110554278
Drug interaction 59.51 49.05 43 947 500140 110088169
Dystonia 56.45 49.05 17 973 25788 110562521

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AG02 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Diphenylbutylpiperidine derivatives
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014150 Antipsychotic Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018492 Dopamine Antagonists
MeSH PA D018726 Anti-Dyskinesia Agents
FDA EPC N0000180182 Typical Antipsychotic
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:37955 H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role CHEBI:48279 serotonergic antagonist
CHEBI has role CHEBI:48561 dopaminergic antagonist
CHEBI has role CHEBI:65190 first generation antipsychotic
CHEBI has role CHEBI:66956 antidyskinesia agent

Related Drugs by ATC class:

N05AG Diphenylbutylpiperidine derivatives 2 drugs
fluspirilenepenfluridol

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Gilles de la Tourette's syndrome indication 5158005 DOID:11119
Neuroleptic malignant syndrome contraindication 15244003 DOID:14464
Senile dementia contraindication 15662003
Agranulocytosis contraindication 17182001 DOID:12987
Glaucoma contraindication 23986001 DOID:1686
Torsades de pointes contraindication 31722008
Parkinsonism contraindication 32798002
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Leukopenia contraindication 84828003 DOID:615
Kidney disease contraindication 90708001 DOID:557
Tardive dyskinesia contraindication 102449007
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Hypomagnesemia contraindication 190855004
Motor tic disorder contraindication 230337001
Disease of liver contraindication 235856003 DOID:409
Hyperprolactinemia contraindication 237662005 DOID:12700
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Neutropenic disorder contraindication 303011007 DOID:1227
Coma contraindication 371632003
Congenital long QT syndrome contraindication 442917000
Carcinoma of female breast contraindication 447782002
Drug Induced CNS Depression contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.93 acidic
pKa2 8.42 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1MG PIMOZIDE NOVITIUM PHARMA A219897 April 13, 2026 RX TABLET ORAL Oct. 18, 2026 COMPETITIVE GENERIC THERAPY
2MG PIMOZIDE NOVITIUM PHARMA A219897 April 13, 2026 RX TABLET ORAL Oct. 18, 2026 COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR ANTAGONIST Ki 8.86 WOMBAT-PK CHEMBL
D(1A) dopamine receptor GPCR Ki 6.23 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 5.80 PDSP
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.84 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 7.75 WOMBAT-PK
Multidrug resistance protein 1 Transporter IC50 5.54 WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 6.63 WOMBAT-PK
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 7.56 WOMBAT-PK
5-hydroxytryptamine receptor 2C GPCR Ki 6.06 PDSP
5-hydroxytryptamine receptor 6 GPCR Ki 7.15 WOMBAT-PK
5-hydroxytryptamine receptor 7 GPCR Ki 9.30 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 6.70 WOMBAT-PK
Alpha-2B adrenergic receptor GPCR Ki 6.09 WOMBAT-PK
D(3) dopamine receptor GPCR ANTAGONIST Ki 9.05 WOMBAT-PK
Histamine H1 receptor GPCR Ki 6.71 WOMBAT-PK
Histamine H4 receptor GPCR Ki 5.70 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 5.71 PDSP
5-hydroxytryptamine receptor 1D GPCR Ki 5.51 PDSP
Alpha-2C adrenergic receptor GPCR Ki 6.42 WOMBAT-PK
D(4) dopamine receptor GPCR ANTAGONIST Ki 8.75 WOMBAT-PK
Kappa-type opioid receptor GPCR IC50 6 CHEMBL
Multidrug resistance-associated protein 1 Transporter IC50 6 WOMBAT-PK
Glycine receptor subunit alpha-1 Ion channel EC50 5.77 CHEMBL
Voltage-dependent T-type calcium channel subunit alpha-1G Ion channel Kd 7.40 CHEMBL
Calmodulin Cytosolic other IC50 5.22 WOMBAT-PK
Delta-type opioid receptor GPCR IC50 5.42 CHEMBL
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel BLOCKER IC50 6.80 IUPHAR
Voltage-dependent T-type calcium channel subunit alpha-1I Ion channel BLOCKER IC50 7.50 IUPHAR
Potassium channel subfamily K member 2 Ion channel IC50 5.75 CHEMBL
Potassium voltage-gated channel subfamily A member 10 Ion channel BLOCKER IC50 6.50 IUPHAR
Solute carrier family 22 member 2 Transporter IC50 4.47 CHEMBL
Ubiquitin carboxyl-terminal hydrolase 1 Enzyme IC50 5.70 CHEMBL
Mu-type opioid receptor GPCR IC50 6.43 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 9.30 CHEMBL
Sodium channel protein type 2 subunit alpha Ion channel IC50 6.47 CHEMBL
D(2) dopamine receptor GPCR Ki 9.22 CHEMBL
5-hydroxytryptamine receptor 6 GPCR ANTAGONIST Ki 7.20 IUPHAR
Dopamine receptor GPCR IC50 9.40 CHEMBL
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel BLOCKER IC50 7.30 IUPHAR
G protein-activated inward rectifier potassium channel 2 Ion channel GATING INHIBITOR EC50 5.50 IUPHAR
Voltage-dependent T-type calcium channel subunit alpha-1G Ion channel BLOCKER IC50 7.50 IUPHAR

External reference:

IDSource
4018479 VUID
N0000146801 NUI
D00560 KEGG_DRUG
4018479 VANDF
C0031935 UMLSCUI
CHEBI:8212 CHEBI
CHEMBL1423 ChEMBL_ID
D010868 MESH_DESCRIPTOR_UI
DB01100 DRUGBANK_ID
90 IUPHAR_LIGAND_ID
2330 INN_ID
1HIZ4DL86F UNII
16362 PUBCHEM_CID
8331 RXNORM
131104 MMSL
5301 MMSL
d00898 MMSL
001492 NDDF
108438008 SNOMEDCT_US
386848009 SNOMEDCT_US
1II PDB_CHEM_ID
1HIZ4DL86F INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Pimozide HUMAN PRESCRIPTION DRUG LABEL 1 49884-347 TABLET 1 mg ORAL ANDA 22 sections
Pimozide HUMAN PRESCRIPTION DRUG LABEL 1 49884-348 TABLET 2 mg ORAL ANDA 22 sections
Pimozide Human Prescription Drug Label 1 70954-853 TABLET 1 mg ORAL ANDA 22 sections
Pimozide Human Prescription Drug Label 1 70954-854 TABLET 2 mg ORAL ANDA 22 sections