CARIPRAZINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H32Cl2N4O
Molecular Weight	427.411
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)C(=O)N[C@H]1CC[C@H](CCN2CCN(CC2)C3=C(Cl)C(Cl)=CC=C3)CC1

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	427.411
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/26956157

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

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 297 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Partial Agonist 290	0.49 nM [Ki]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Partial Agonist 290	0.085 nM [Ki]
Serotonin 1a (5-HT1a) receptor 172 Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Partial Agonist 290	2.6 nM [Ki]
Serotonin 2a (5-HT2a) receptor 231 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Antagonist 2778	18.8 nM [Ki]
Serotonin 2b (5-HT2b) receptor 60 Target ID: CHEMBL1833 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Antagonist 2778	0.58 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 298 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf	Primary		Approved 8429	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 2015
Bipolar I disorder 17 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf	Primary		Approved 8429	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 2015

C_max

Value	Dose	Analyte	Population
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

Value	Dose	Analyte	Population
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

T_1/2

Value	Dose	Analyte	Population
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

F_unbound

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse 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

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1587 inducer 781	inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2C19 1478 CYP3A5 73 P-gp 1461 BCRP 699 OATP1B1 788 OATP1B3 706 OAT3 642 OCT2 647 CYP2A6 707 CYP2E1 882	CYP3A 191 P-gp 1537 BCRP 561 OATP1B1 406 OATP1B3 350 OAT3 339 OCT2 355	CYP1A2 701

Drug as perpetrator

Target	Modality	Activity	Metabolite
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	inconclusive
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP3A5 130	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
CYP3A5 130	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP3A5 130	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP3A 191	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=29 Page: 29.0	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). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=29 Page: 29.0
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=29 Page: 29.0	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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=29 Page: 29.0

Tox targets

Target	Modality	Metabolite
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000PharmR.pdf#page=473 Page: 473.0
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000PharmR.pdf#page=473 Page: 473.0	DCAR 2
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000PharmR.pdf#page=473 Page: 473.0	DDCAR 2

Sourcing

Vendor/Aggregator	ID	URL
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

Title	Date	PubMed
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	20093397
Cariprazine, an orally active D2/D3 receptor antagonist, for the potential treatment of schizophrenia, bipolar mania and depression.	2010 Jul	20571978
Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.	2012 May 15	22537450
Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability.	2013 Feb	23320989
Cariprazine: First Global Approval.	2015 Nov	26510944

Patents

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 Dec 16 00:42:14 GMT 2023` Edited by `admin` on `Sat Dec 16 00:42:14 GMT 2023`
Record UNII	F6RJL8B278
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CARIPRAZINE

Official Name

English

CARIPRAZINE [USAN]

Common Name

English

FRI-7000188

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

Cariprazine [WHO-DD]

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175430