brivaracetam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
amide type nootrope agents, piracetam derivatives 5068 357336-20-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • brivaracetam
  • briviact
  • UCB 34714
  • UCB-34714
Brivaracetam displays a high and selective affinity for synaptic vesicle protein 2A (SV2A) in the brain, which may contribute to the anticonvulsant effect.
  • Molecular weight: 212.29
  • Formula: C11H20N2O2
  • CLOGP: 1.01
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 63.40
  • ALOGS: -0.66
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.10 g O
0.10 g P

ADMET properties:

PropertyValueReference
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:

DateAgencyCompanyOrphan
Jan. 14, 2016 EMA UCB Pharma SA
Feb. 18, 2016 FDA UCB INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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)

DiseaseRelationSNOMED_IDDOID
Partial seizure indication 29753000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.83 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Synaptic vesicle glycoprotein 2A Transporter MODULATOR Ki 7.10 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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