Stem definition | Drug id | CAS RN |
---|---|---|
5037 | 839712-12-8 |
Dose | Unit | Route |
---|---|---|
3 | mg | O |
None
Date | Agency | Company | Orphan |
---|---|---|---|
Sept. 17, 2015 | FDA | FOREST LABS LLC |
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 |
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 |
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 |
None
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 |
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 13.04 | acidic |
pKa2 | 8.38 | Basic |
pKa3 | 1.21 | Basic |
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 |
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) |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
D(2) dopamine receptor | GPCR | PARTIAL AGONIST | Ki | 9.31 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
5-hydroxytryptamine receptor 1A | GPCR | PARTIAL AGONIST | Ki | 8.59 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
5-hydroxytryptamine receptor 2A | GPCR | ANTAGONIST | Ki | 7.73 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.68 | CHEMBL | |||||
D(1B) dopamine receptor | GPCR | Ki | 5.10 | CHEMBL | |||||
D(4) dopamine receptor | GPCR | Ki | 6.96 | CHEMBL | |||||
5-hydroxytryptamine receptor 2B | GPCR | ANTAGONIST | Ki | 9.24 | SCIENTIFIC LITERATURE | ||||
5-hydroxytryptamine receptor 7 | GPCR | Ki | 6.95 | SCIENTIFIC LITERATURE | |||||
D(3) dopamine receptor | GPCR | PARTIAL AGONIST | Ki | 10.07 | SCIENTIFIC LITERATURE | ||||
Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 7.63 | SCIENTIFIC LITERATURE | ||||
Alpha-1D adrenergic receptor | GPCR | Ki | 6.68 | SCIENTIFIC LITERATURE | |||||
5-hydroxytryptamine receptor 2C | GPCR | ANTAGONIST | Ki | 6.87 | SCIENTIFIC LITERATURE | ||||
D(1A) dopamine receptor | GPCR | Ki | 5.68 | CHEMBL | |||||
D(2) dopamine receptor | GPCR | IC50 | 7.80 | CHEMBL | |||||
D(3) dopamine receptor | GPCR | IC50 | 8.80 | CHEMBL |
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 |
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 |