Pimozide
Orap (pimozide) is a small molecule pharmaceutical. Pimozide was first approved as Orap on 1984-07-31. It is used to treat huntington disease, psychotic disorders, schizophrenia spectrum and other psychotic disorders, and tourette syndrome in the USA. The pharmaceutical is active against 5-hydroxytryptamine receptor 2A and D(2) dopamine receptor. In addition, it is known to target D(3) dopamine receptor, potassium voltage-gated channel subfamily A member 10, 5-hydroxytryptamine receptor 1A, voltage-dependent T-type calcium channel subunit alpha-1I, histamine H1 receptor, G protein-activated inward rectifier potassium channel 2, voltage-dependent T-type calcium channel subunit alpha-1G, 5-hydroxytryptamine receptor 7, voltage-dependent T-type calcium channel subunit alpha-1H, and 5-hydroxytryptamine receptor 6.
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Commercial
Trade Name
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EMA
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Drug Products
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EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Pimozide
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| ORAP | Teva | N-017473 DISCN | 1984-07-31 | 2 products, RLD |
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FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| pimozide | ANDA | 2017-11-25 |
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| huntington disease | Orphanet_399 | D006816 | G10 |
| psychotic disorders | — | D011618 | F20.81 |
| schizophrenia spectrum and other psychotic disorders | — | D019967 | — |
| tourette syndrome | EFO_0004895 | D005879 | F95.2 |
Agency Specific
FDA
EMA
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Patent Expiration
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HCPCS
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Clinical
Clinical Trials
142 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Alcoholic hepatitis | D006519 | EFO_1001345 | K70.1 | 1 | 1 | 4 | 1 | 2 | 8 |
| Chronic renal insufficiency | D051436 | N18 | — | 2 | 3 | 2 | — | 6 | |
| Non-alcoholic fatty liver disease | D065626 | EFO_0003095 | K75.81 | — | 2 | 2 | 2 | — | 5 |
| Diabetic nephropathies | D003928 | EFO_0000401 | — | 1 | 2 | 2 | — | 4 | |
| Chronic kidney failure | D007676 | EFO_0003884 | N18.6 | — | 1 | 1 | 2 | — | 4 |
| Hiv infections | D015658 | EFO_0000764 | B20 | 1 | 1 | — | 1 | 1 | 4 |
| Inflammation | D007249 | — | — | 1 | 1 | 1 | 3 | ||
| Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | — | — | — | 3 | — | 3 |
| Heart failure | D006333 | EFO_0003144 | I50 | — | — | — | 1 | 1 | 2 |
| Osteoradionecrosis | D010025 | EFO_1001821 | — | — | — | 1 | 1 | 2 |
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Covid-19 | D000086382 | U07.1 | 1 | 2 | 1 | — | 2 | 4 | |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | — | 3 | 1 | — | — | 4 |
| Fibrosis | D005355 | — | 3 | 1 | — | — | 4 | ||
| Oxidative stress | D018384 | EFO_1001905 | — | — | 1 | — | 2 | 3 | |
| Alcoholic fatty liver | D005235 | K70.0 | — | — | 1 | — | 2 | 3 | |
| Pancreatitis | D010195 | EFO_0000278 | K85 | 2 | — | 1 | — | — | 3 |
| Liver diseases | D008107 | EFO_0001421 | K70-K77 | — | 2 | 1 | — | — | 2 |
| Alcoholic liver diseases | D008108 | EFO_0008573 | K70 | — | — | 1 | — | 1 | 2 |
| Glomerulonephritis | D005921 | N05 | — | — | 1 | — | 1 | 2 | |
| Neonatal sepsis | D000071074 | HP_0040187 | — | — | 2 | — | — | 2 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Cardiovascular diseases | D002318 | EFO_0000319 | I98 | — | 3 | — | — | — | 3 |
| Major depressive disorder | D003865 | EFO_0003761 | F22 | 1 | 2 | — | — | 1 | 3 |
| Behcet syndrome | D001528 | EFO_0003780 | M35.2 | — | 2 | — | — | — | 2 |
| Colorectal neoplasms | D015179 | 1 | 1 | — | — | — | 2 | ||
| Hiv | D006678 | O98.7 | — | 2 | — | — | — | 2 | |
| Atherosclerosis | D050197 | EFO_0003914 | I25.1 | — | 2 | — | — | — | 2 |
| Duchenne muscular dystrophy | D020388 | 2 | 2 | — | — | — | 2 | ||
| Inflammatory bowel diseases | D015212 | EFO_0003767 | — | 2 | — | — | — | 2 | |
| Coronary artery disease | D003324 | I25.1 | — | 1 | — | — | — | 1 | |
| Heart diseases | D006331 | EFO_0003777 | I51.9 | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hepatopulmonary syndrome | D020065 | EFO_1001346 | K76.81 | 1 | — | — | — | 2 | 3 |
| Central nervous system neoplasms | D016543 | 1 | — | — | — | — | 1 | ||
| Anemia | D000740 | EFO_0004272 | D64.9 | 1 | — | — | — | — | 1 |
| Female infertility | D007247 | EFO_0008560 | N97 | 1 | — | — | — | — | 1 |
| Bipolar disorder | D001714 | EFO_0000289 | F30.9 | 1 | — | — | — | — | 1 |
| Healthy volunteers/patients | — | 1 | — | — | — | — | 1 | ||
| Crohn disease | D003424 | EFO_0000384 | K50 | 1 | — | — | — | — | 1 |
| Male infertility | D007248 | EFO_0004248 | N46 | 1 | — | — | — | — | 1 |
| Mucositis | D052016 | EFO_1001898 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Type 1 diabetes mellitus | D003922 | EFO_0001359 | E10 | — | — | — | — | 1 | 1 |
| Viral pneumonia | D011024 | EFO_0007541 | J12.9 | — | — | — | — | 1 | 1 |
| Hepatorenal syndrome | D006530 | K76.7 | — | — | — | — | 1 | 1 | |
| Graves ophthalmopathy | D049970 | EFO_1001466 | — | — | — | — | 1 | 1 | |
| Vertigo | D014717 | H81.39 | — | — | — | — | 1 | 1 | |
| Dizziness | D004244 | HP_0002321 | R42 | — | — | — | — | 1 | 1 |
| Diabetes mellitus | D003920 | EFO_0000400 | E08-E13 | — | — | — | — | 1 | 1 |
| Olfaction disorders | D000857 | R43.0 | — | — | — | — | 1 | 1 | |
| Aphthous stomatitis | D013281 | EFO_0003938 | K12.0 | — | — | — | — | 1 | 1 |
| Cytokine release syndrome | D000080424 | D89.83 | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | PIMOZIDE |
| INN | pimozide |
| Description | Pimozide is a member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. It has a role as a H1-receptor antagonist, a serotonergic antagonist, a first generation antipsychotic, an antidyskinesia agent and a dopaminergic antagonist. It is a member of benzimidazoles, an organofluorine compound and a heteroarylpiperidine. |
| Classification | Small molecule |
| Drug class | Typical antipsychotic |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | O=c1[nH]c2ccccc2n1C1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 |
Identifiers
| PDB | — |
| CAS-ID | 2062-78-4 |
| RxCUI | 8331 |
| ChEMBL ID | CHEMBL1423 |
| ChEBI ID | 8212 |
| PubChem CID | 16362 |
| DrugBank | DB01100 |
| UNII ID | 1HIZ4DL86F (ChemIDplus, GSRS) |
Target
Agency Approved
HTR2A
HTR2A
DRD2
DRD2
Organism
Homo sapiens
Gene name
HTR2A
Gene synonyms
HTR2
NCBI Gene ID
Protein name
5-hydroxytryptamine receptor 2A
Protein synonyms
5-HT2 receptor, 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled, serotonin 5-HT-2A receptor, Serotonin receptor 2A
Uniprot ID
Mouse ortholog
Htr2a (15558)
5-hydroxytryptamine receptor 2A (P35363)
Alternate
DRD3
DRD3
KCNA10
KCNA10
HTR1A
HTR1A
CACNA1I
CACNA1I
HRH1
HRH1
KCNJ6
KCNJ6
CACNA1G
CACNA1G
HTR7
HTR7
CACNA1H
CACNA1H
HTR6
HTR6
Variants
Clinical Variant
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Financial
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Trends
PubMed Central
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Safety
Black-box Warning
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Adverse Events
Top Adverse Reactions
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1,290 adverse events reported
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