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cariprazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	5037	839712-12-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: cariprazine cariprazine hydrochloride vraylar RGH-188	The efficacy of cariprazine could be mediated through a combination of partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors. Molecular weight: 427.41 Formula: C21H32Cl2N4O CLOGP: 4.78 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 38.82 ALOGS: -4.19 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

cariprazine
cariprazine hydrochloride
vraylar
RGH-188

The efficacy of cariprazine could be mediated through a combination of partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors.

Molecular weight: 427.41
Formula: C21H32Cl2N4O
CLOGP: 4.78
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 38.82
ALOGS: -4.19
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
3	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Sept. 17, 2015	FDA	FOREST LABS LLC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Akathisia	232.56	30.48	55	1796	8174	50595099
Tardive dyskinesia	161.18	30.48	40	1811	7239	50596034
Weight increased	59.41	30.48	53	1798	201838	50401435
Mania	51.04	30.48	18	1833	10898	50592375
Restlessness	48.86	30.48	22	1829	25151	50578122
Off label use	47.18	30.48	71	1780	474355	50128918
Tremor	45.80	30.48	36	1815	114867	50488406
Hyperprolactinaemia	43.12	30.48	12	1839	3353	50599920
Parkinsonism	42.93	30.48	15	1836	8832	50594441
Suicidal ideation	39.99	30.48	25	1826	55360	50547913
Tongue discomfort	39.96	30.48	10	1841	1858	50601415
Pregnancy	39.52	30.48	20	1831	29557	50573716
Extrapyramidal disorder	38.75	30.48	15	1836	11755	50591518
Atrioventricular block first degree	35.89	30.48	12	1839	6189	50597084
Bipolar disorder	34.88	30.48	12	1839	6745	50596528

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Akathisia	80.86	39.68	22	897	6720	29566888
Off label use	68.17	39.68	63	856	300737	29272871
Cataract nuclear	61.63	39.68	11	908	473	29573135

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Akathisia	140.32	32.71	37	1715	11473	64485507
Tardive dyskinesia	95.27	32.71	26	1726	9152	64487828
Cataract nuclear	93.14	32.71	17	1735	950	64496030
Off label use	79.44	32.71	91	1661	632715	63864265
Weight increased	64.11	32.71	50	1702	213298	64283682
Parkinsonism	63.20	32.71	21	1731	14352	64482628
Mania	41.92	32.71	16	1736	16270	64480710
Restlessness	39.55	32.71	20	1732	39765	64457215
Tongue discomfort	36.64	32.71	9	1743	2090	64494890
Tremor	34.47	32.71	30	1722	148200	64348780
Atrioventricular block first degree	32.94	32.71	12	1740	10722	64486258

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N05AX15	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
FDA EPC	N0000175430	Atypical Antipsychotic
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
CHEBI has role	CHEBI:65191	atypical antipsychotic agent

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Mixed bipolar I disorder	indication	16506000	DOID:3312
Schizophrenia	indication	58214004	DOID:5419
Bipolar affective disorder, current episode manic	indication	191618007

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.04	acidic
pKa2	8.38	Basic
pKa3	1.21	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE47350	July 16, 2029	TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE47350	July 16, 2029	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE47350	July 16, 2029	TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE47350	July 16, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 3MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 3MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 3MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 3MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 4.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 4.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 4.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 6MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 6MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA AND/OR ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 6MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	7737142	Sept. 17, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 1.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	May 24, 2022	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)
EQ 3MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	May 24, 2022	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)
EQ 4.5MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	May 24, 2022	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)
EQ 6MG BASE	VRAYLAR	ALLERGAN	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	May 24, 2022	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	PARTIAL AGONIST	Ki	9.31	SCIENTIFIC LITERATURE	DRUG LABEL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	PARTIAL AGONIST	Ki	8.59	SCIENTIFIC LITERATURE	DRUG LABEL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	7.73	SCIENTIFIC LITERATURE	DRUG LABEL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.68	CHEMBL
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN		Ki	5.10	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	6.96	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	9.24	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	6.95	SCIENTIFIC LITERATURE
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	PARTIAL AGONIST	Ki	10.07	SCIENTIFIC LITERATURE
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.63	SCIENTIFIC LITERATURE
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.68	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	6.87	SCIENTIFIC LITERATURE
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.68	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		IC50	7.80	CHEMBL
D(3) dopamine receptor	GPCR		DRD3_RAT		IC50	8.80	CHEMBL

External reference:

ID	Source
F6RJL8B278	UNII
D09997	KEGG_DRUG
1083076-69-0	SECONDARY_CAS_RN
4035436	VANDF
C2936870	UMLSCUI
CHEBI:90933	CHEBI
7RU	PDB_CHEM_ID
CHEMBL2028019	ChEMBL_ID
11154555	PUBCHEM_CID
DB06016	DRUGBANK_ID
CHEMBL2024517	ChEMBL_ID
8920	INN_ID
C533287	MESH_SUPPLEMENTAL_RECORD_UI
7671	IUPHAR_LIGAND_ID
1667655	RXNORM
236113	MMSL
31191	MMSL
d08379	MMSL
1172432002	SNOMEDCT_US
715295006	SNOMEDCT_US
763607001	SNOMEDCT_US
016462	NDDF
016463	NDDF

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-115	CAPSULE, GELATIN COATED	1.50 mg	ORAL	NDA	35 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-130	CAPSULE, GELATIN COATED	3 mg	ORAL	NDA	35 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-145	CAPSULE, GELATIN COATED	4.50 mg	ORAL	NDA	35 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-160	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	35 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	70518-3157	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	35 sections