Details of the Drug

General Information of Drug (ID: DMJYDVK)

Drug Name
Cariprazine
Synonyms
Cariprazine; 839712-12-8; RGH-188; RGH 188; Cariprazine(RGH188); UNII-F6RJL8B278; F6RJL8B278; CHEMBL3085826; 3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea; Cariprazine [USAN:INN]; Reagila; MP-214; MP 214; Cariprazine (USAN/INN); Cariprazine (RGH-188); C21H32Cl2N4O; SCHEMBL184342; SCHEMBL184343; GTPL7671; SCHEMBL7861573; CHEMBL2028019; CHEBI:90933; HSDB 8310; DTXSID80232867; KPWSJANDNDDRMB-QAQDUYKDSA-N; MolPort-039-139-594; BDBM263449; BCP14691; BDBM50443101; BDBM50382290; ZINC38309313; 3526AH
Indication
Disease Entry ICD 11 Status REF
Bipolar disorder 6A60 Approved [1]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 427.4
Logarithm of the Partition Coefficient (xlogp) 4.3
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
Half-life
The concentration or amount of drug in body reduced by one-half in 1 week [2]
Metabolism
The drug is metabolized via the hydroxylation and demethylation []
Chemical Identifiers
Formula
C21H32Cl2N4O
IUPAC Name
3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea
Canonical SMILES
CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
InChI
InChI=1S/C21H32Cl2N4O/c1-25(2)21(28)24-17-8-6-16(7-9-17)10-11-26-12-14-27(15-13-26)19-5-3-4-18(22)20(19)23/h3-5,16-17H,6-15H2,1-2H3,(H,24,28)
InChIKey
KPWSJANDNDDRMB-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
11154555
ChEBI ID
CHEBI:90933
CAS Number
839712-12-8
DrugBank ID
DB06016
TTD ID
D05XGO
INTEDE ID
DR0276
ACDINA ID
D00100
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Modulator [3]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Modulator [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME 		DE4LYSA CP3A4_HUMAN Substrate [4]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [4]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Bipolar disorder
ICD Disease Classification 6A60
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Dopamine D2 receptor (D2R) DTT DRD2 2.50E-02 -0.08 -0.49
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 7.30E-01 -1.91E-02 -1.41E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Cariprazine (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Metreleptin DM1NOEK Moderate Increased metabolism of Cariprazine caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [5]
Ivosidenib DM8S6T7 Moderate Increased metabolism of Cariprazine caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [5]
Arn-509 DMT81LZ Moderate Increased metabolism of Cariprazine caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [6]
Oliceridine DM6MDCF Major Additive CNS depression effects by the combination of Cariprazine and Oliceridine. Acute pain [MG31] [7]
Mepyramine DMB4SFH Moderate Additive anticholinergic effects by the combination of Cariprazine and Mepyramine. Allergic/hypersensitivity disorder [4A80-4A8Z] [8]
Phenyltoloxamine DMKAEQW Moderate Additive anticholinergic effects by the combination of Cariprazine and Phenyltoloxamine. Allergic/hypersensitivity disorder [4A80-4A8Z] [8]
Troleandomycin DMUZNIG Major Decreased metabolism of Cariprazine caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [6]
Pexidartinib DMS2J0Z Moderate Increased metabolism of Cariprazine caused by Pexidartinib mediated induction of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [6]
Tucatinib DMBESUA Major Decreased metabolism of Cariprazine caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [6]
Palbociclib DMD7L94 Moderate Decreased metabolism of Cariprazine caused by Palbociclib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [5]
Osilodrostat DMIJC9X Moderate Decreased metabolism of Cariprazine caused by Osilodrostat mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [5]
Ivacaftor DMZC1HS Moderate Decreased metabolism of Cariprazine caused by Ivacaftor mediated inhibition of CYP450 enzyme. Cystic fibrosis [CA25] [5]
MK-8228 DMOB58Q Moderate Decreased metabolism of Cariprazine caused by MK-8228 mediated inhibition of CYP450 enzyme. Cytomegaloviral disease [1D82] [6]
OPC-34712 DMHG57U Moderate Additive anticholinergic effects by the combination of Cariprazine and OPC-34712. Depression [6A70-6A7Z] [9]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Cariprazine and Esketamine. Depression [6A70-6A7Z] [10]
Cenobamate DM8KLU9 Moderate Increased metabolism of Cariprazine caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [6]
Rufinamide DMWE60C Moderate Increased metabolism of Cariprazine caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [5]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Cariprazine caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [6]
Tazemetostat DMWP1BH Moderate Increased metabolism of Cariprazine caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [5]
Boceprevir DMBSHMF Major Decreased metabolism of Cariprazine caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [6]
Etravirine DMGV8QU Moderate Increased metabolism of Cariprazine caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [6]
BMS-201038 DMQTAGO Moderate Decreased metabolism of Cariprazine caused by BMS-201038 mediated inhibition of CYP450 enzyme. Hyper-lipoproteinaemia [5C80] [5]
Levamlodipine DM92S6N Moderate Additive hypotensive effects by the combination of Cariprazine and Levamlodipine. Hypertension [BA00-BA04] [11]
TAK-491 DMCF6SX Moderate Additive hypotensive effects by the combination of Cariprazine and TAK-491. Hypertension [BA00-BA04] [11]
Belladonna DM2RBWK Moderate Additive anticholinergic effects by the combination of Cariprazine and Belladonna. Infectious gastroenteritis/colitis [1A40] [9]
Berotralstat DMWA2DZ Moderate Decreased metabolism of Cariprazine caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [6]
Suvorexant DM0E6S3 Moderate Decreased metabolism of Cariprazine caused by Suvorexant mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [5]
ITI-007 DMUQ1DO Moderate Additive anticholinergic effects by the combination of Cariprazine and ITI-007. Insomnia [7A00-7A0Z] [9]
Polyethylene glycol DM4I1JP Moderate Increased risk of lowers seizure threshold by the combination of Cariprazine and Polyethylene glycol. Irritable bowel syndrome [DD91] [12]
Ceritinib DMB920Z Major Decreased metabolism of Cariprazine caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [6]
PF-06463922 DMKM7EW Moderate Increased metabolism of Cariprazine caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [6]
Idelalisib DM602WT Major Decreased metabolism of Cariprazine caused by Idelalisib mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [6]
IPI-145 DMWA24P Moderate Decreased metabolism of Cariprazine caused by IPI-145 mediated inhibition of CYP450 enzyme. Mature B-cell leukaemia [2A82] [6]
Dabrafenib DMX6OE3 Moderate Increased metabolism of Cariprazine caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [5]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Cariprazine and Lasmiditan. Migraine [8A80] [13]
Netupitant DMEKAYI Moderate Decreased metabolism of Cariprazine caused by Netupitant mediated inhibition of CYP450 enzyme. Nausea/vomiting [MD90] [5]
Rucaparib DM9PVX8 Moderate Decreased metabolism of Cariprazine caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [5]
Abametapir DM2RX0I Moderate Decreased metabolism of Cariprazine caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [14]
Methylscopolamine DM5VWOB Moderate Additive anticholinergic effects by the combination of Cariprazine and Methylscopolamine. Peptic ulcer [DA61] [9]
Lefamulin DME6G97 Moderate Decreased metabolism of Cariprazine caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [15]
Lonafarnib DMGM2Z6 Major Decreased metabolism of Cariprazine caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [6]
Enzalutamide DMGL19D Moderate Increased metabolism of Cariprazine caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [6]
Silodosin DMJSBT6 Moderate Additive hypotensive effects by the combination of Cariprazine and Silodosin. Prostate hyperplasia [GA90] [11]
Asenapine DMSQZE2 Moderate Additive anticholinergic effects by the combination of Cariprazine and Asenapine. Schizophrenia [6A20] [9]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Cariprazine caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [6]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Cariprazine caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [5]
Larotrectinib DM26CQR Moderate Decreased metabolism of Cariprazine caused by Larotrectinib mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [5]
Armodafinil DMGB035 Moderate Increased metabolism of Cariprazine caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [5]
LEE011 DMMX75K Moderate Decreased metabolism of Cariprazine caused by LEE011 mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [6]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Cariprazine caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [16]
Brilinta DMBR01X Moderate Decreased metabolism of Cariprazine caused by Brilinta mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [5]
Acrivastine DMTIGA0 Moderate Additive anticholinergic effects by the combination of Cariprazine and Acrivastine. Vasomotor/allergic rhinitis [CA08] [9]
⏷ Show the Full List of 52 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Allura red AC dye E00338 33258 Colorant
Erythrosine sodium anhydrous E00324 27872 Colorant
FD&C blue no. 1 E00263 19700 Colorant
FD&C red no. 3 E00629 Not Available Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Ferric oxide black E00522 16211978 Colorant
Ferrosoferric oxide E00231 14789 Colorant
Gelatin E00630 Not Available Other agent
Magnesium stearate E00208 11177 lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Colcothar yellow E00436 518696 Colorant
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
Shellac E00695 Not Available Coating agent; Film/membrane-forming agent; Microencapsulating agent; Modified-release agent
⏷ Show the Full List of 13 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Cariprazine 3 mg capsule 3 mg Oral Capsule Oral
Cariprazine 4.5 mg capsule 4.5 mg Oral Capsule Oral
Cariprazine 6 mg capsule 6 mg Oral Capsule Oral
Cariprazine Hydrochloride eq 3mg base capsule eq 3mg base Capsule Oral
Cariprazine Hydrochloride eq 6mg base capsule eq 6mg base Capsule Oral
Cariprazine Hydrochloride eq 4.5mg base capsule eq 4.5mg base Capsule Oral
Cariprazine Hydrochloride eq 1.5mg base capsule eq 1.5mg base Capsule Oral
Cariprazine 1.5 mg capsule 1.5 mg Oral Capsule Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7671).
2 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
4 Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206.
5 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
6 Product Information. Vraylar (cariprazine). Actavis Pharma, Inc., Parsippany, NJ.
7 US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
8 Kulik AV, Wilbur R "Delirium and stereotypy from anticholinergic antiparkinson drugs." Prog Neuropsychopharmacol Biol Psychiatry 6 (1982): 75-82. [PMID: 7202232]
9 Cohen MA, Alfonso CA, Mosquera M. Development of urinary retention during treatment with clozapine and meclizine [published correction appears in Am J Psychiatry 1994 Jun;151(6):952]. Am J Psychiatry. 1994;151(4):619-620. [PMID: 8147469]
10 Cerner Multum, Inc. "Australian Product Information.".
11 Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028]
12 Product Information. Suprep Bowel Prep Kit (magnesium/potassium/sodium sulfates). Braintree Laboratories, Braintree, MA.
13 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
14 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
15 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
16 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.