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]

Affected Organisms

Humans and other mammals

ATC Code

N05AX15: Cariprazine

N05AX: Other antipsychotics

N05A: ANTIPSYCHOTICS

N05: PSYCHOLEPTICS

N: NERVOUS SYSTEM

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)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

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: CHEMBL5986307
CAS Number: 839712-12-8
UNII: F6RJL8B278
DrugBank ID: DB06016
TTD ID: D05XGO
INTEDE ID: DR0276
ACDINA ID: D00100

Drug-Molecule Activity Atlas (DMA)^NEW

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Drug Pharmacogenomic Perturbation (DPP)^NEW

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Drug ADMET Endpoint Profile (DAE)^NEW

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Repurposed Drugs (RPD)

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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)

MIA Detail

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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)

MEA Detail

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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]


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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


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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

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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.