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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)

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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	367.29	24.36	86	3041	9060	63476835
Tardive dyskinesia	325.87	24.36	77	3050	8425	63477470
Extrapyramidal disorder	93.29	24.36	32	3095	13252	63472643
Parkinsonism	76.63	24.36	26	3101	10413	63475482
Mania	76.09	24.36	27	3100	12340	63473555
Weight increased	72.60	24.36	76	3051	260716	63225179
Tremor	69.24	24.36	55	3072	132184	63353711
Suicidal ideation	65.92	24.36	40	3087	62381	63423514
Restlessness	65.51	24.36	31	3096	29422	63456473
Pregnancy	61.80	24.36	32	3095	36804	63449091

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FDA Adverse Event Reporting System (Male)

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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	126.63	39.86	35	1487	8074	34947335
Extrapyramidal disorder	74.52	39.86	26	1496	12854	34942555
Tardive dyskinesia	72.27	39.86	21	1501	5769	34949640
Off label use	60.78	39.86	82	1440	419442	34535967
Psychotic symptom	59.19	39.86	14	1508	1729	34953680
Cataract nuclear	56.73	39.86	11	1511	527	34954882
Parkinsonism	45.40	39.86	16	1506	8122	34947287
Restlessness	41.99	39.86	21	1501	25461	34929948
Treatment noncompliance	40.05	39.86	21	1501	28079	34927330

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FDA Adverse Event Reporting System (Geriatric)

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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	231.87	27.60	60	2776	13199	79728353
Tardive dyskinesia	225.13	27.60	56	2780	10515	79731037
Extrapyramidal disorder	101.77	27.60	36	2800	22643	79718909
Parkinsonism	88.62	27.60	30	2806	16554	79724998
Cataract nuclear	87.21	27.60	17	2819	1029	79740523
Weight increased	77.68	27.60	70	2766	277316	79464236
Off label use	69.94	27.60	119	2717	907096	78834456
Mania	63.38	27.60	24	2812	18236	79723316
Tremor	53.66	27.60	46	2790	170037	79571515
Suicidal ideation	49.81	27.60	32	2804	76308	79665244

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05AX15	NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
CHEBI has role	CHEBI:65191	atypical antipsychotic agent
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

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

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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

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🐶 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)

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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	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE47350	July 16, 2029	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER
EQ 1.5MG BASE	VRAYLAR	ABBVIE	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	ABBVIE	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	ABBVIE	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	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE47350	July 16, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE49110	July 16, 2029	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER
EQ 1.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE49110	July 16, 2029	TREATMENT OF ACUTE MANIC OR MIXED EPISODES ASSOCIATED WITH BIPOLAR I DISORDER WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE49110	July 16, 2029	TREATMENT OF DEPRESSIVE EPISODES ASSOCIATED WITH BIPOLAR I DISORDER (BIPOLAR DEPRESSION) WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE49110	July 16, 2029	TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE
EQ 1.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	RE49302	July 16, 2029	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVE DISORDER

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 1.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	Dec. 16, 2025	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVEDISORDER IN ADULTS
EQ 3MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	Dec. 16, 2025	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVEDISORDER IN ADULTS
EQ 4.5MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	Dec. 16, 2025	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVEDISORDER IN ADULTS
EQ 6MG BASE	VRAYLAR	ABBVIE	N204370	Sept. 17, 2015	RX	CAPSULE	ORAL	Dec. 16, 2025	ADJUNCTIVE THERAPY TO ANTIDEPRESSANTS FOR THE TREATMENT OF MAJOR DEPRESSIVEDISORDER IN ADULTS

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Bioactivity Summary:

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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
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
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.68	CHEMBL
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

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External reference:

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ID	Source
7RU	PDB_CHEM_ID
016462	NDDF
016463	NDDF
1083076-69-0	SECONDARY_CAS_RN
11154555	PUBCHEM_CID
1172432002	SNOMEDCT_US
1667655	RXNORM
236113	MMSL
31191	MMSL
4035436	VANDF

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Pharmaceutical products:

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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	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-115	CAPSULE, GELATIN COATED	1.50 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-130	CAPSULE, GELATIN COATED	3 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-130	CAPSULE, GELATIN COATED	3 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-145	CAPSULE, GELATIN COATED	4.50 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-145	CAPSULE, GELATIN COATED	4.50 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-160	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	61874-160	CAPSULE, GELATIN COATED	6 mg	ORAL	NDA	38 sections
Vraylar	HUMAN PRESCRIPTION DRUG LABEL	1	70518-3157	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

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