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: ONP

  • 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 232.56 30.48 55 1796 8174 50595099
Tardive dyskinesia 161.18 30.48 40 1811 7239 50596034
Weight increased 59.41 30.48 53 1798 201838 50401435
Mania 51.04 30.48 18 1833 10898 50592375
Restlessness 48.86 30.48 22 1829 25151 50578122
Off label use 47.18 30.48 71 1780 474355 50128918
Tremor 45.80 30.48 36 1815 114867 50488406
Hyperprolactinaemia 43.12 30.48 12 1839 3353 50599920
Parkinsonism 42.93 30.48 15 1836 8832 50594441
Suicidal ideation 39.99 30.48 25 1826 55360 50547913
Tongue discomfort 39.96 30.48 10 1841 1858 50601415
Pregnancy 39.52 30.48 20 1831 29557 50573716
Extrapyramidal disorder 38.75 30.48 15 1836 11755 50591518
Atrioventricular block first degree 35.89 30.48 12 1839 6189 50597084
Bipolar disorder 34.88 30.48 12 1839 6745 50596528

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 80.86 39.68 22 897 6720 29566888
Off label use 68.17 39.68 63 856 300737 29272871
Cataract nuclear 61.63 39.68 11 908 473 29573135

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 140.32 32.71 37 1715 11473 64485507
Tardive dyskinesia 95.27 32.71 26 1726 9152 64487828
Cataract nuclear 93.14 32.71 17 1735 950 64496030
Off label use 79.44 32.71 91 1661 632715 63864265
Weight increased 64.11 32.71 50 1702 213298 64283682
Parkinsonism 63.20 32.71 21 1731 14352 64482628
Mania 41.92 32.71 16 1736 16270 64480710
Restlessness 39.55 32.71 20 1732 39765 64457215
Tongue discomfort 36.64 32.71 9 1743 2090 64494890
Tremor 34.47 32.71 30 1722 148200 64348780
Atrioventricular block first degree 32.94 32.71 12 1740 10722 64486258

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 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
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.68 CHEMBL
D(1B) dopamine receptor GPCR Ki 5.10 CHEMBL
D(4) dopamine receptor GPCR Ki 6.96 CHEMBL
5-hydroxytryptamine receptor 2B GPCR ANTAGONIST Ki 9.24 SCIENTIFIC LITERATURE
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
D(1A) dopamine receptor GPCR Ki 5.68 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
4035436 VANDF
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
1172432002 SNOMEDCT_US
715295006 SNOMEDCT_US
763607001 SNOMEDCT_US
016462 NDDF
016463 NDDF

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