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 | 259.05 | 30.07 | 61 | 2070 | 8591 | 56281345 |
Tardive dyskinesia | 170.66 | 30.07 | 43 | 2088 | 7988 | 56281948 |
Mania | 64.81 | 30.07 | 22 | 2109 | 11498 | 56278438 |
Extrapyramidal disorder | 59.46 | 30.07 | 21 | 2110 | 12335 | 56277601 |
Weight increased | 57.53 | 30.07 | 56 | 2075 | 229647 | 56060289 |
Restlessness | 56.45 | 30.07 | 25 | 2106 | 26561 | 56263375 |
Tremor | 49.36 | 30.07 | 39 | 2092 | 121050 | 56168886 |
Parkinsonism | 45.07 | 30.07 | 16 | 2115 | 9530 | 56280406 |
Suicidal ideation | 43.20 | 30.07 | 27 | 2104 | 57715 | 56232221 |
Hyperprolactinaemia | 41.71 | 30.07 | 12 | 2119 | 3649 | 56286287 |
Bipolar disorder | 40.76 | 30.07 | 14 | 2117 | 7566 | 56282370 |
Off label use | 40.74 | 30.07 | 74 | 2057 | 556106 | 55733830 |
Tongue discomfort | 38.85 | 30.07 | 10 | 2121 | 2006 | 56287930 |
Pregnancy | 36.78 | 30.07 | 20 | 2111 | 33013 | 56256923 |
Atrioventricular block first degree | 34.45 | 30.07 | 12 | 2119 | 6753 | 56283183 |
Dyskinesia | 30.68 | 30.07 | 17 | 2114 | 29091 | 56260845 |
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 | 98.94 | 42.03 | 27 | 1109 | 7226 | 31688982 |
Extrapyramidal disorder | 61.66 | 42.03 | 21 | 1115 | 11757 | 31684451 |
Cataract nuclear | 59.78 | 42.03 | 11 | 1125 | 485 | 31695723 |
Schizophrenia | 55.47 | 42.03 | 19 | 1117 | 10811 | 31685397 |
Off label use | 54.45 | 42.03 | 64 | 1072 | 347210 | 31348998 |
Psychotic symptom | 52.46 | 42.03 | 12 | 1124 | 1560 | 31694648 |
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 | 167.80 | 32.28 | 44 | 2056 | 12249 | 70914095 |
Tardive dyskinesia | 100.06 | 32.28 | 28 | 2072 | 9901 | 70916443 |
Cataract nuclear | 91.27 | 32.28 | 17 | 2083 | 973 | 70925371 |
Parkinsonism | 67.87 | 32.28 | 23 | 2077 | 15302 | 70911042 |
Weight increased | 64.75 | 32.28 | 55 | 2045 | 242276 | 70684068 |
Extrapyramidal disorder | 64.71 | 32.28 | 24 | 2076 | 20726 | 70905618 |
Off label use | 61.36 | 32.28 | 91 | 2009 | 742969 | 70183375 |
Mania | 54.04 | 32.28 | 20 | 2080 | 17154 | 70909190 |
Tremor | 40.80 | 32.28 | 35 | 2065 | 155589 | 70770755 |
Pleurothotonus | 39.71 | 32.28 | 10 | 2090 | 2356 | 70923988 |
Restlessness | 39.64 | 32.28 | 21 | 2079 | 42107 | 70884237 |
Tongue discomfort | 35.30 | 32.28 | 9 | 2091 | 2226 | 70924118 |
Schizophrenia | 33.29 | 32.28 | 14 | 2086 | 16754 | 70909590 |
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 | RE49110 | 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 | RE49110 | 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 | RE49110 | July 16, 2029 | TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE |
EQ 3MG BASE | VRAYLAR | ALLERGAN | 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 3MG BASE | VRAYLAR | ALLERGAN | 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 3MG BASE | VRAYLAR | ALLERGAN | N204370 | Sept. 17, 2015 | RX | CAPSULE | ORAL | RE49110 | July 16, 2029 | TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE |
EQ 4.5MG BASE | VRAYLAR | ALLERGAN | 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 4.5MG BASE | VRAYLAR | ALLERGAN | 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 4.5MG BASE | VRAYLAR | ALLERGAN | N204370 | Sept. 17, 2015 | RX | CAPSULE | ORAL | RE49110 | July 16, 2029 | TREATMENT OF SCHIZOPHRENIA WITH CARIPRAZINE |
EQ 6MG BASE | VRAYLAR | ALLERGAN | 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 6MG BASE | VRAYLAR | ALLERGAN | 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 6MG BASE | VRAYLAR | ALLERGAN | N204370 | Sept. 17, 2015 | RX | CAPSULE | ORAL | RE49110 | 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 | |||
D(4) dopamine receptor | GPCR | Ki | 6.96 | CHEMBL | |||||
5-hydroxytryptamine receptor 2B | GPCR | ANTAGONIST | Ki | 9.24 | SCIENTIFIC LITERATURE | ||||
D(1A) dopamine receptor | GPCR | Ki | 5.68 | CHEMBL | |||||
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 | ||||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.68 | CHEMBL | |||||
D(1B) dopamine receptor | GPCR | Ki | 5.10 | 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 |
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 |
016462 | NDDF |
016463 | NDDF |
1172432002 | SNOMEDCT_US |
715295006 | SNOMEDCT_US |
763607001 | SNOMEDCT_US |
4035436 | VANDF |
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 |
Vraylar | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-3157 | CAPSULE, GELATIN COATED | 6 mg | ORAL | NDA | 35 sections |