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 288	0.49 nM [Ki]
Dopamine D3 receptor 91 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Partial Agonist 288	0.085 nM [Ki]
Serotonin 1a (5-HT1a) receptor 171 Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Partial Agonist 288	2.6 nM [Ki]
Serotonin 2a (5-HT2a) receptor 230 Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Antagonist 2760	18.8 nM [Ki]
Serotonin 2b (5-HT2b) receptor 60 Target ID: CHEMBL1833 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956157	Antagonist 2760	0.58 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Schizophrenia 295 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf	Primary		Approved 8360	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
Bipolar I disorder 17 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf	Primary		Approved 8360	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

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 1579 inducer 768	inhibitor 1752	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 CYP2C19 1463 CYP3A5 73 P-gp 1437 BCRP 691 OATP1B1 781 OATP1B3 700 OAT3 636 OCT2 638 CYP2A6 704 CYP2E1 876	CYP3A 189 P-gp 1527 BCRP 555 OATP1B1 403 OATP1B3 347 OAT3 333 OCT2 348	CYP1A2 689

Drug as perpetrator

Target	Modality	Activity	Metabolite
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	inconclusive
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	no
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP3A5 130	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
CYP3A5 130	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
CYP3A5 130	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2A6 736	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP2E1 964	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000LBL.pdf#page=22 Page: 22.0	weak
CYP3A4 1909	inhibitor 3240 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 555	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
BCRP 555	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
BCRP 555	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OAT3 333	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OAT3 333	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OAT3 333	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
OCT2 348	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
OCT2 348	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
OCT2 348	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DCAR 2
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000ClinPharmR.pdf#page=54 Page: 54.0	no	DDCAR 2
CYP3A 189	substrate 3326 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 1193	substrate 3326 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 1632	inhibitor 1613 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000PharmR.pdf#page=473 Page: 473.0
hERG 1632	inhibitor 1613 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/204370Orig1Orig2s000PharmR.pdf#page=473 Page: 473.0	DCAR 2
hERG 1632	inhibitor 1613 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

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 `Thu Jul 06 07:05:44 UTC 2023` Edited by `admin` on `Thu Jul 06 07:05:44 UTC 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