brivaracetam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| amide type nootrope agents, piracetam derivatives | 5068 | 357336-20-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Brivaracetam displays a high and selective affinity for synaptic vesicle protein 2A (SV2A) in the brain, which may contribute to the anticonvulsant effect.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
| 0.10 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.56 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.75 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.83 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 8.98 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 14, 2016 | EMA | UCB Pharma SA | |
| Feb. 18, 2016 | FDA | UCB INC |
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 |
|---|---|---|---|---|---|---|
| Seizure | 377.45 | 45.11 | 152 | 1750 | 122902 | 46561258 |
| Off label use | 159.17 | 45.11 | 127 | 1775 | 379714 | 46304446 |
| Generalised tonic-clonic seizure | 119.71 | 45.11 | 44 | 1858 | 27078 | 46657082 |
| Partial seizures | 95.57 | 45.11 | 25 | 1877 | 4985 | 46679175 |
| Petit mal epilepsy | 85.84 | 45.11 | 21 | 1881 | 3199 | 46680961 |
| Anticonvulsant drug level increased | 68.49 | 45.11 | 15 | 1887 | 1405 | 46682755 |
| Multiple-drug resistance | 64.67 | 45.11 | 16 | 1886 | 2549 | 46681611 |
| JC polyomavirus test | 59.25 | 45.11 | 8 | 1894 | 36 | 46684124 |
| Irritability | 58.89 | 45.11 | 27 | 1875 | 28919 | 46655241 |
| Overdose | 55.08 | 45.11 | 40 | 1862 | 101939 | 46582221 |
| Suicidal ideation | 54.82 | 45.11 | 32 | 1870 | 56350 | 46627810 |
| Aggression | 48.72 | 45.11 | 22 | 1880 | 22722 | 46661438 |
| Depression | 46.50 | 45.11 | 45 | 1857 | 170059 | 46514101 |
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 |
|---|---|---|---|---|---|---|
| Seizure | 319.35 | 52.70 | 136 | 1438 | 98339 | 29852565 |
| Off label use | 127.26 | 52.70 | 104 | 1470 | 249186 | 29701718 |
| Status epilepticus | 113.49 | 52.70 | 36 | 1538 | 11036 | 29939868 |
| Generalised tonic-clonic seizure | 89.89 | 52.70 | 35 | 1539 | 19516 | 29931388 |
| Aggression | 89.62 | 52.70 | 42 | 1532 | 36865 | 29914039 |
| Drug level fluctuating | 81.36 | 52.70 | 15 | 1559 | 451 | 29950453 |
| Hyperammonaemic encephalopathy | 76.24 | 52.70 | 18 | 1556 | 1826 | 29949078 |
| Aura | 74.36 | 52.70 | 13 | 1561 | 287 | 29950617 |
| Drug ineffective | 71.70 | 52.70 | 88 | 1486 | 340299 | 29610605 |
| Focal dyscognitive seizures | 55.22 | 52.70 | 13 | 1561 | 1300 | 29949604 |
| Irritability | 55.14 | 52.70 | 26 | 1548 | 23024 | 29927880 |
| Myoclonus | 54.71 | 52.70 | 22 | 1552 | 13290 | 29937614 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N03AX23 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| FDA MoA | N0000192345 | Epoxide Hydrolase Inhibitors |
| CHEBI has role | CHEBI:35623 | antiepileptic |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Partial seizure | indication | 29753000 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.83 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 100MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 10, 2021 | NEW PATIENT POPULATION |
| 10MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 10, 2021 | NEW PATIENT POPULATION |
| 25MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 10, 2021 | NEW PATIENT POPULATION |
| 50MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 10, 2021 | NEW PATIENT POPULATION |
| 75MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 10, 2021 | NEW PATIENT POPULATION |
| 10MG/ML | BRIVIACT | UCB INC | N205838 | May 12, 2016 | RX | SOLUTION | ORAL | May 10, 2021 | NEW PATIENT POPULATION |
| 100MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 12, 2021 | NEW CHEMICAL ENTITY |
| 10MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 12, 2021 | NEW CHEMICAL ENTITY |
| 25MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 12, 2021 | NEW CHEMICAL ENTITY |
| 50MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 12, 2021 | NEW CHEMICAL ENTITY |
| 75MG | BRIVIACT | UCB INC | N205836 | May 12, 2016 | RX | TABLET | ORAL | May 12, 2021 | NEW CHEMICAL ENTITY |
| 50MG/5ML (10MG/ML) | BRIVIACT | UCB INC | N205837 | May 12, 2016 | RX | SOLUTION | INTRAVENOUS | May 12, 2021 | NEW CHEMICAL ENTITY |
| 10MG/ML | BRIVIACT | UCB INC | N205838 | May 12, 2016 | RX | SOLUTION | ORAL | May 12, 2021 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Synaptic vesicle glycoprotein 2A | Transporter | MODULATOR | Ki | 7.10 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| U863JGG2IA | UNII |
| D08879 | KEGG_DRUG |
| 4035741 | VANDF |
| C1699861 | UMLSCUI |
| CHEBI:133013 | CHEBI |
| CHEMBL607400 | ChEMBL_ID |
| DB05541 | DRUGBANK_ID |
| 8642 | INN_ID |
| C482793 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9837243 | PUBCHEM_CID |
| 9041 | IUPHAR_LIGAND_ID |
| 1739745 | RXNORM |
| 238946 | MMSL |
| 31471 | MMSL |
| d08414 | MMSL |
| 016704 | NDDF |
| 420813001 | SNOMEDCT_US |
| 421052000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-370 | TABLET, FILM COATED | 10 mg | ORAL | NDA | 31 sections |
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-470 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 31 sections |
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-570 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 31 sections |
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-670 | TABLET, FILM COATED | 75 mg | ORAL | NDA | 31 sections |
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-770 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 31 sections |
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-870 | SOLUTION | 10 mg | ORAL | NDA | 31 sections |
| Briviact | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50474-970 | INJECTION, SUSPENSION | 50 mg | INTRAVENOUS | NDA | 31 sections |