cariprazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5037 839712-12-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cariprazine
  • cariprazine hydrochloride
  • vraylar
  • RGH-188
The efficacy of cariprazine could be mediated through a combination of partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors.
  • Molecular weight: 427.41
  • Formula: C21H32Cl2N4O
  • CLOGP: 4.78
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 38.82
  • ALOGS: -4.19
  • ROTB: 5

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
3 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 17, 2015 FDA FOREST LABS LLC

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
Akathisia 259.05 30.07 61 2070 8591 56281345
Tardive dyskinesia 170.66 30.07 43 2088 7988 56281948
Mania 64.81 30.07 22 2109 11498 56278438
Extrapyramidal disorder 59.46 30.07 21 2110 12335 56277601
Weight increased 57.53 30.07 56 2075 229647 56060289
Restlessness 56.45 30.07 25 2106 26561 56263375
Tremor 49.36 30.07 39 2092 121050 56168886
Parkinsonism 45.07 30.07 16 2115 9530 56280406
Suicidal ideation 43.20 30.07 27 2104 57715 56232221
Hyperprolactinaemia 41.71 30.07 12 2119 3649 56286287
Bipolar disorder 40.76 30.07 14 2117 7566 56282370
Off label use 40.74 30.07 74 2057 556106 55733830
Tongue discomfort 38.85 30.07 10 2121 2006 56287930
Pregnancy 36.78 30.07 20 2111 33013 56256923
Atrioventricular block first degree 34.45 30.07 12 2119 6753 56283183
Dyskinesia 30.68 30.07 17 2114 29091 56260845

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
Akathisia 98.94 42.03 27 1109 7226 31688982
Extrapyramidal disorder 61.66 42.03 21 1115 11757 31684451
Cataract nuclear 59.78 42.03 11 1125 485 31695723
Schizophrenia 55.47 42.03 19 1117 10811 31685397
Off label use 54.45 42.03 64 1072 347210 31348998
Psychotic symptom 52.46 42.03 12 1124 1560 31694648

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
Akathisia 167.80 32.28 44 2056 12249 70914095
Tardive dyskinesia 100.06 32.28 28 2072 9901 70916443
Cataract nuclear 91.27 32.28 17 2083 973 70925371
Parkinsonism 67.87 32.28 23 2077 15302 70911042
Weight increased 64.75 32.28 55 2045 242276 70684068
Extrapyramidal disorder 64.71 32.28 24 2076 20726 70905618
Off label use 61.36 32.28 91 2009 742969 70183375
Mania 54.04 32.28 20 2080 17154 70909190
Tremor 40.80 32.28 35 2065 155589 70770755
Pleurothotonus 39.71 32.28 10 2090 2356 70923988
Restlessness 39.64 32.28 21 2079 42107 70884237
Tongue discomfort 35.30 32.28 9 2091 2226 70924118
Schizophrenia 33.29 32.28 14 2086 16754 70909590

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05AX15 NERVOUS SYSTEM
PSYCHOLEPTICS
ANTIPSYCHOTICS
Other antipsychotics
FDA EPC N0000175430 Atypical Antipsychotic
MeSH PA D014150 Antipsychotic Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D011619 Psychotropic Drugs
MeSH PA D014149 Tranquilizing Agents
CHEBI has role CHEBI:48279 serotonin antagonists
CHEBI has role CHEBI:51065 Dopamine receptor agonist
CHEBI has role CHEBI:65191 atypical antipsychotic agent

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

DiseaseRelationSNOMED_IDDOID
Mixed bipolar I disorder indication 16506000 DOID:3312
Schizophrenia indication 58214004 DOID:5419
Bipolar affective disorder, current episode manic indication 191618007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.04 acidic
pKa2 8.38 Basic
pKa3 1.21 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE47350 July 16, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE47350 July 16, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE47350 July 16, 2029 TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE47350 July 16, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL RE49110 July 16, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL 7737142 Sept. 17, 2029 TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 1.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL May 24, 2022 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)
EQ 3MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL May 24, 2022 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)
EQ 4.5MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL May 24, 2022 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)
EQ 6MG BASE VRAYLAR ALLERGAN N204370 Sept. 17, 2015 RX CAPSULE ORAL May 24, 2022 TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
D(2) dopamine receptor GPCR PARTIAL AGONIST Ki 9.31 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 1A GPCR PARTIAL AGONIST Ki 8.59 SCIENTIFIC LITERATURE DRUG LABEL
5-hydroxytryptamine receptor 2A GPCR ANTAGONIST Ki 7.73 SCIENTIFIC LITERATURE DRUG LABEL
D(4) dopamine receptor GPCR Ki 6.96 CHEMBL
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 9.24 SCIENTIFIC LITERATURE
D(1A) dopamine receptor GPCR Ki 5.68 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 6.95 SCIENTIFIC LITERATURE
D(3) dopamine receptor GPCR PARTIAL AGONIST Ki 10.07 SCIENTIFIC LITERATURE
Histamine H1 receptor GPCR ANTAGONIST Ki 7.63 SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor GPCR Ki 6.68 SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2C GPCR ANTAGONIST Ki 6.87 SCIENTIFIC LITERATURE
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.68 CHEMBL
D(1B) dopamine receptor GPCR Ki 5.10 CHEMBL
D(2) dopamine receptor GPCR IC50 7.80 CHEMBL
D(3) dopamine receptor GPCR IC50 8.80 CHEMBL

External reference:

IDSource
F6RJL8B278 UNII
D09997 KEGG_DRUG
1083076-69-0 SECONDARY_CAS_RN
C2936870 UMLSCUI
CHEBI:90933 CHEBI
7RU PDB_CHEM_ID
CHEMBL2028019 ChEMBL_ID
11154555 PUBCHEM_CID
DB06016 DRUGBANK_ID
CHEMBL2024517 ChEMBL_ID
8920 INN_ID
C533287 MESH_SUPPLEMENTAL_RECORD_UI
7671 IUPHAR_LIGAND_ID
1667655 RXNORM
236113 MMSL
31191 MMSL
d08379 MMSL
016462 NDDF
016463 NDDF
1172432002 SNOMEDCT_US
715295006 SNOMEDCT_US
763607001 SNOMEDCT_US
4035436 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vraylar HUMAN PRESCRIPTION DRUG LABEL 1 61874-115 CAPSULE, GELATIN COATED 1.50 mg ORAL NDA 35 sections
Vraylar HUMAN PRESCRIPTION DRUG LABEL 1 61874-130 CAPSULE, GELATIN COATED 3 mg ORAL NDA 35 sections
Vraylar HUMAN PRESCRIPTION DRUG LABEL 1 61874-145 CAPSULE, GELATIN COATED 4.50 mg ORAL NDA 35 sections
Vraylar HUMAN PRESCRIPTION DRUG LABEL 1 61874-160 CAPSULE, GELATIN COATED 6 mg ORAL NDA 35 sections
Vraylar HUMAN PRESCRIPTION DRUG LABEL 1 70518-3157 CAPSULE, GELATIN COATED 6 mg ORAL NDA 35 sections
Vraylar HUMAN PRESCRIPTION DRUG LABEL 1 70518-3157 CAPSULE, GELATIN COATED 6 mg ORAL NDA 35 sections