U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C21H32Cl2N4O
Molecular Weight 427.4117
Optical Activity UNSPECIFIED
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CARIPRAZINE

SMILES

CN(C)C(=N[C@@]1([H])CC[C@@]([H])(CC1)CCN2CCN(CC2)c3cccc(c3Cl)Cl)O

InChI

InChIKey=KPWSJANDNDDRMB-QAQDUYKDSA-N
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)/t16-,17-

HIDE SMILES / InChI
Molecular Formula C21H32Cl2N4O
Molecular Weight 427.4117
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Cariprazine is an antipsychotic approved by FDA for the treatment of schizophrenia and bipolar I disorder. The drug has a unique clinical action which is explained by its ability to act on dopamine D3 receptors. Pharmacology studies revealed that cariprazine is a dual partial agonist of dopamine D2 and D3 receptors as well as serotonin 5HT1a, 2a and 2b receptors.

CNS Activity

Originator

Approval Year

2015
457
Targets

Targets

Primary TargetPharmacologyConditionPotency
Partial Agonist
266
 0.49 nM [Ki]
Partial Agonist
266
 0.085 nM [Ki]
Partial Agonist
266
 2.6 nM [Ki]
Antagonist
2575
 18.8 nM [Ki]
Antagonist
2575
 0.58 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8043
VRAYLAR

Approved Use

VRAYLAR is indicated for the treatment of schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder.

Launch Date

1.44244802E12
Primary
Approved
8043
VRAYLAR

Approved Use

VRAYLAR is indicated for the treatment of schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder.

Launch Date

1.44244802E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
10.2 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
3 mg 1 times / day multiple, oral
dose: 3 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
22.7 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
6 mg 1 times / day multiple, oral
dose: 6 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
28.8 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
9 mg 1 times / day multiple, oral
dose: 9 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
156 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
3 mg 1 times / day multiple, oral
dose: 3 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
358 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
6 mg 1 times / day multiple, oral
dose: 6 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
466 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
9 mg 1 times / day multiple, oral
dose: 9 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
68.4 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
3 mg 1 times / day multiple, oral
dose: 3 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
44.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
6 mg 1 times / day multiple, oral
dose: 6 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
31.6 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/26834462
9 mg 1 times / day multiple, oral
dose: 9 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
9%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204370s006lbl.pdf
unknown, unknown
 CARIPRAZINE HYDROCHLORIDE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Disc. AE: Schizophrenia aggravated, Psychotic disorder...
AEs leading to
discontinuation/dose reduction:
Schizophrenia aggravated (2.7%)
Psychotic disorder (2%)
ALT increased (2 patients)
AST increased (2 patients)
Bilirubin increased (1 patient)
Akathisia (0.9%)
Extrapyramidal disorder (0.3%)
Restlessness (0.2%)
Dystonia (0.2%)
Parkinsonism (0.2%)
Salivary hypersecretion (0.2%)
Tremor (0.2%)
Musculoskeletal stiffness (0.2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
12 mg 1 times / day steady, oral (mean)
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: steady
Dose: 12 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25562205
unhealthy, 41,2 years (range: 18-65 years)
n = 169
Health Status: unhealthy
Condition: bipolar I disorder
Age Group: 41,2 years (range: 18-65 years)
Sex: M+F
Population Size: 169
Sources:
https://pubmed.ncbi.nlm.nih.gov/25562205
Disc. AE: Akathisia...
AEs leading to
discontinuation/dose reduction:
Akathisia
Sources:
https://pubmed.ncbi.nlm.nih.gov/25562205
6 mg 1 times / day steady, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
unhealthy, Elderly
n = 17
Health Status: unhealthy
Condition: dementia related psychosis
Age Group: Elderly
Population Size: 17
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
Other AEs: Adverse event...
Other AEs:
Adverse event (grade 5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
unhealthy
Health Status: unhealthy
Condition: bipolar mania
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
Disc. AE: Akathisia...
AEs leading to
discontinuation/dose reduction:
Akathisia (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Dystonia 0.2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Musculoskeletal stiffness 0.2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Parkinsonism 0.2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Restlessness 0.2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Salivary hypersecretion 0.2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Tremor 0.2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Extrapyramidal disorder 0.3%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Akathisia 0.9%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Bilirubin increased 1 patient
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
ALT increased 2 patients
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
AST increased 2 patients
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Psychotic disorder 2%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Schizophrenia aggravated 2.7%
Disc. AE
5.7 mg 1 times / day steady, oral (mean)
Recommended
Dose: 5.7 mg, 1 times / day
Route: oral
Route: steady
Dose: 5.7 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
unhealthy, 39.1 years
n = 586
Health Status: unhealthy
Condition: schizophrenia
Age Group: 39.1 years
Sex: M+F
Population Size: 586
Sources:
https://pubmed.ncbi.nlm.nih.gov/28478771
Akathisia Disc. AE
12 mg 1 times / day steady, oral (mean)
Highest studied dose
Dose: 12 mg, 1 times / day
Route: oral
Route: steady
Dose: 12 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25562205
unhealthy, 41,2 years (range: 18-65 years)
n = 169
Health Status: unhealthy
Condition: bipolar I disorder
Age Group: 41,2 years (range: 18-65 years)
Sex: M+F
Population Size: 169
Sources:
https://pubmed.ncbi.nlm.nih.gov/25562205
Adverse event grade 5
6 mg 1 times / day steady, oral
Recommended
Dose: 6 mg, 1 times / day
Route: oral
Route: steady
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
unhealthy, Elderly
n = 17
Health Status: unhealthy
Condition: dementia related psychosis
Age Group: Elderly
Population Size: 17
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
Akathisia 2%
Disc. AE
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
unhealthy
Health Status: unhealthy
Condition: bipolar mania
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1467

inducer
707
inhibitor
1604
substrate
1118

inhibitor
1702
inhibitor
1475

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1383

CYP2C19
1325

CYP3A5
70

P-gp
1330

BCRP
643

OATP1B1
733

OATP1B3
657

OAT3
588

OCT2
594

CYP2A6
627

CYP2E1
790
CYP3A
172

P-gp
1400

BCRP
515

OATP1B1
370

OATP1B3
319

OAT3
305

OCT2
316
CYP1A2
637
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
P-gp
1514
 inconclusive
BCRP
713
 no
BCRP
713
 no
DCAR
2
BCRP
713
 no
DDCAR
2
CYP1A2
1532
 no
CYP1A2
1532
 no
DCAR
2
CYP1A2
1532
 no
DDCAR
2
CYP2C19
1392
 no
DCAR
2
CYP2C19
1392
 no
DDCAR
2
CYP2C9
1648
 no
DCAR
2
CYP2C9
1648
 no
DDCAR
2
CYP2D6
1738
 no
DCAR
2
CYP2D6
1738
 no
DDCAR
2
CYP3A4
1772
 no
CYP3A4
1772
 no
DCAR
2
CYP3A4
1772
 no
DDCAR
2
CYP3A5
122
 no
CYP3A5
122
 no
DCAR
2
CYP3A5
122
 no
DDCAR
2
OAT3
590
 no
OAT3
590
 no
DCAR
2
OAT3
590
 no
DDCAR
2
OATP1B1
748
 no
OATP1B1
748
 no
DCAR
2
OATP1B1
748
 no
DDCAR
2
OATP1B3
666
 no
OATP1B3
666
 no
DCAR
2
OATP1B3
666
 no
DDCAR
2
OCT2
595
 no
OCT2
595
 no
DCAR
2
OCT2
595
 no
DDCAR
2
P-gp
1514
 no
DCAR
2
P-gp
1514
 no
DDCAR
2
CYP1A2
1532
 weak
CYP2A6
659
 weak
CYP2C19
1392
 weak
CYP2C9
1648
 weak
CYP2D6
1738
 weak
CYP2E1
871
 weak
CYP3A4
1772
 weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
515
 no
BCRP
515
 no
DCAR
2
BCRP
515
 no
DDCAR
2
OAT3
305
 no
OAT3
305
 no
DCAR
2
OAT3
305
 no
DDCAR
2
OATP1B1
370
 no
OATP1B1
370
 no
DCAR
2
OATP1B1
370
 no
DDCAR
2
OATP1B3
319
 no
OATP1B3
319
 no
DCAR
2
OATP1B3
319
 no
DDCAR
2
OCT2
316
 no
OCT2
316
 no
DCAR
2
OCT2
316
 no
DDCAR
2
P-gp
1400
 no
P-gp
1400
 no
DCAR
2
P-gp
1400
 no
DDCAR
2
CYP3A
172
 yes
yes (co-administration study)
Comment: In vivo data showed that a strong CYP3A4 inhibitor (i.e., ketoconazole) increased the total effective exposure after cariprazine administration by about 100% (study RGH-PK-07).
Page: 29.0
CYP2D6
1118
 yes
yes (pharmacogenomic study)
Comment: Based on a population PK analysis, steady-state AUC0-24 of DDCAR in poor metabolizers of CYP2D6 was about 16% higher than in extensive metabolizers.
Page: 29.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1507
hERG
1507
DCAR
2
hERG
1507
DDCAR
2
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:90933
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:90933
ChemicalBook
CB22563442
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB22563442
MolPort
MolPort-039-139-594
https://www.molport.com/shop/molecule-link/MolPort-039-139-594
ZINC
ZINC000100907004
http://zinc15.docking.org/substances/ZINC000100907004
PubMed

PubMed

TitleDatePubMed
Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile.
2010 Apr
Cariprazine, an orally active D2/D3 receptor antagonist, for the potential treatment of schizophrenia, bipolar mania and depression.
2010 Jul
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.
2012 May 15
Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability.
2013 Feb
Cariprazine: First Global Approval.
2015 Nov
Patents

Patents

JP2010527984A
2
JP2011528374A
2

Sample Use Guides

In Vivo Use Guide
The recommended dose is from 1.5 mg to 6 mg/day (schizophrenia) and 3 mg to 6 mg/day (bipolar mania).
Route of Administration: Oral
In Vitro Use Guide
Rat striatal and hippocampal membrane preparation were treated with a range of cariprazine concentrations from 0.1 nM to 0.1 mM to study [35S]GTPgammaS binding.
Substance Class Chemical
Created
by admin
on Sat Jun 26 09:29:47 UTC 2021
Edited
by admin
on Sat Jun 26 09:29:47 UTC 2021
Record UNII
F6RJL8B278
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CARIPRAZINE
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
CARIPRAZINE [USAN]
Common Name English
FRI-7000188
Common Name English
CARIPRAZINE [WHO-DD]
Common Name English
CARIPRAZINE [INN]
Common Name English
CARIPRAZINE [MI]
Common Name English
GED-129
Code English
3-(TRANS-4-(2-(4-(2,3-DICHLOROPHENYL)PIPERAZIN-1-YL)ETHYL)CYCLOHEXYL)-1,1-DIMETHYLUREA
Systematic Name English
MP-214
Code English
RGH-188
Code English
Classification Tree Code System Code
NDF-RT N0000175430
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
WHO-ATC N05AX15
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
Code System Code Type Description
LACTMED
Cariprazine
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
MESH
C533287
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
PUBCHEM
11154555
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
EPA CompTox
839712-12-8
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
FDA UNII
F6RJL8B278
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
NCI_THESAURUS
C169826
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
CAS
839712-12-8
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
EVMPD
SUB34830
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
WIKIPEDIA
Cariprazine
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
IUPHAR
7671
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
MERCK INDEX
M11853
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
INN
8920
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
RXCUI
1667655
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY RxNorm
HSDB
8310
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
ChEMBL
CHEMBL2028019
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
DRUG BANK
DB06016
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
DRUG CENTRAL
5037
Created by admin on Sat Jun 26 09:29:48 UTC 2021 , Edited by admin on Sat Jun 26 09:29:48 UTC 2021
PRIMARY
Related Record Type Details
5-HYDROXYTRYPTAMINE RECEPTOR 2C
TARGET->WEAK INHIBITOR
Ki
D(2) DOPAMINE RECEPTOR
TARGET->PARTIAL AGONIST
Ki
D(3) DOPAMINE RECEPTOR
TARGET->PARTIAL AGONIST
Most of the clinically used antipsychotics display fairly high affinity for D3 receptors in vitro, they lack significant D3 receptor binding in vivo. They also do not occupy D3 receptors in schizophrenic patients at clinically-relevant doses, despite having significant and expected D2 receptor occupancy. The lack of in vivo D3 receptor occupancy of currently used antipsychotics may be due to their inability to displace endogenous DA from these sites; especially since DA has approximately 20- fold higher affinity for D3 vs D2 receptors and D3 (but not D2) receptors exist predominantly in a high affinity state for DA”
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 2A
TARGET->WEAK INHIBITOR
Ki
Structure of CARIPRAZINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
5-HYDROXYTRYPTAMINE RECEPTOR 1A
TARGET->PARTIAL AGONIST
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 2B
TARGET -> INHIBITOR
Ki
5-HYDROXYTRYPTAMINE RECEPTOR 4
TRANSPORTER -> NON-INHIBITOR
Ki
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of DESMETHYL CARIPRAZINE
METABOLITE ACTIVE -> PARENT
minor enzyme involved in metabolism
MINOR
PLASMA
Structure of DIDESMETHYL CARIPRAZINE
METABOLITE ACTIVE -> PARENT
activity same as CARIPRAZINE; steady state plasma level 400% of CARIPRAZINE
MAJOR
PLASMA
Structure of DIDESMETHYL CARIPRAZINE
METABOLITE ACTIVE -> PARENT
MINOR
PLASMA
Structure of DESMETHYL CARIPRAZINE
METABOLITE ACTIVE -> PARENT
activity same as CARIPRAZINE, steady state level 30% of CARIPRAZINE
MAJOR
PLASMA
Related Record Type Details
Structure of CARIPRAZINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
NIH
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