Page last updated: 2024-12-11

ucb 34714

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Description

brivaracetam: A pyrrolidinone compound that is used to treat partial onset seizures in adult patients; structure in first source. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

brivaracetam : A non-proteinogenic amino acid derivative that is butanamide in which the pro-S hydrogen at position 2 is replaced by a (4R)-2-oxo-4-propylpyrrolidin-1-yl. Used for treatment of partial onset seizures related to epilepsy. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID9837243
CHEMBL ID607400
CHEBI ID133013
SCHEMBL ID122081
MeSH IDM0462698

Synonyms (54)

Synonym
rikelta
ucb-34714
brivaracetam
2-(2-oxo-4-propylpyrrolidin-1-yl)butanamide
ucb34714
briviact
ucb 34714
CHEBI:133013 ,
(2s)-2-[(4r)-2-oxo-4-propylpyrrolidin-1-yl]butanamide
D08879
brivaracetam (jan/usan/inn)
briviact (tn)
357336-20-0
CHEMBL607400
1-pyrrolidineacetamide, alpha-ethyl-2-oxo-4-propyl-, (alphas,4r)-
(2s)-2-((4r)-2-oxo-4-propylpyrrolidin-1-yl)butanamide
brivaracetam [usan:inn]
u863jgg2ia ,
unii-u863jgg2ia
brivaracetam [mart.]
(2s)-2-((4r)-2-oxo-4-propyltetrahydro-1h-pyrrol-1-yl) butanamide
brivaracetam [orange book]
1-pyrrolidineacetamide, .alpha.-ethyl-2-oxo-4-propyl (.alpha.s,4r)-
brivaracetam [inn]
brivaracetam [mi]
brivaracetam [who-dd]
brivaracetam [jan]
brivaracetam [usan]
(2s)-2-((4r)-2-oxo-4-n-propyl-1-pyrrolidinyl)butanamide
MSYKRHVOOPPJKU-BDAKNGLRSA-N
bdbm50422531
SCHEMBL122081
CS-3418
HY-14449
AC-29289
gtpl9041
compound 83alpha
AKOS027324306
mfcd25976668
EX-A2748
DB05541
DTXSID00905081
AS-35277
Q408099
CCG-266666
NCGC00390779-02
(S)-2-((R)-2-OXO-4-PROPYLPYRROLIDIN-1-YL)BUTANAMIDE
BB161996
1-pyrrolidineacetamide, alpha-ethyl-2-oxo-4-propyl-, (alphas,4r)-; (alphas,4r)-alpha-ethyl-2-oxo-4-propyl-1-pyrrolidineacetamide; brivaracetam; briviact; ucb 34714
brivaracetamum
brivaracetam (mart.)
1-pyrrolidineacetamide, alpha-ethyl-2-oxo-4-propyl (alphas,4r)-
n03ax23
ae5 - anti-epileptic drugs 5

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The objective of the study was to evaluate the pharmacokinetics (and how they are affected by food), CNS pharmacodynamics and the adverse event profile of brivaracetam after single increasing doses."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after single increasing oral doses in healthy males.
Connell, J; Jacobs, T; Pigeolet, E; Riethuisen, JM; Rolan, P; Sargentini-Maier, ML; Stockis, A; Tytgat, D, 2007
)
0.34
" The most common adverse events were somnolence and dizziness."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after single increasing oral doses in healthy males.
Connell, J; Jacobs, T; Pigeolet, E; Riethuisen, JM; Rolan, P; Sargentini-Maier, ML; Stockis, A; Tytgat, D, 2007
)
0.34
" This study examined the pharmacokinetics, central nervous system pharmacodynamics and adverse event profile of multiple oral doses of brivaracetam in healthy male subjects."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men.
Pigeolet, E; Rolan, P; Sargentini-Maier, ML; Stockis, A, 2008
)
0.35
" Adverse events were mostly mild to moderate, central nervous system-related and resolved within the first day of treatment."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men.
Pigeolet, E; Rolan, P; Sargentini-Maier, ML; Stockis, A, 2008
)
0.35
" The outcomes of interest included 50% responder rates, seizure freedom, the incidence of withdrawal and treatment-emergent adverse events (TEAEs)."( The efficacy and safety of brivaracetam at different doses for partial-onset epilepsy: a meta-analysis of placebo-controlled studies.
Tian, X; Wang, X; Yuan, M; Zhou, Q, 2015
)
0.42
" Treatment-emergent adverse events (TEAEs) occurred in 155 (59."( A randomized, double-blind, placebo-controlled, multicenter, parallel-group study to evaluate the efficacy and safety of adjunctive brivaracetam in adult patients with uncontrolled partial-onset seizures.
Brandt, C; Klein, P; Kwan, P; Liang, W; Schiemann, J; Sperling, MR; Stalvey, T; Whitesides, J, 2015
)
0.42
" Safety and tolerability were assessed using adverse events, electrocardiography, vital signs, and laboratory assessments."( Safety and tolerability of adjunctive brivaracetam as intravenous infusion or bolus in patients with epilepsy.
Barnes, M; Biton, V; Dilley, D; Klein, P; Lu, S; Schiemann, J, 2016
)
0.43
" Treatment-emergent adverse event (TEAE) incidence during IV BRV was similar whether IV BRV was initiated first (70."( Safety and tolerability of adjunctive brivaracetam as intravenous infusion or bolus in patients with epilepsy.
Barnes, M; Biton, V; Dilley, D; Klein, P; Lu, S; Schiemann, J, 2016
)
0.43
" Safety/tolerability data pooled from 2,186 patients: ≥1 treatment-emergent adverse event (TEAE) reported by 1,848 (84."( Safety, tolerability, and seizure control during long-term treatment with adjunctive brivaracetam for partial-onset seizures.
Borghs, S; Eckhardt, K; Johnson, ME; Kwan, P; McDonough, B; Schiemann, J; Toledo, M; Whitesides, J, 2016
)
0.43
" Treatment-emergent adverse events (TEAEs) were reported by 68."( Efficacy and safety of brivaracetam for partial-onset seizures in 3 pooled clinical studies.
Ben-Menachem, E; Eckhardt, K; Gamage, J; Johnson, ME; Klein, P; Mameniškienė, R; McDonough, B; Quarato, PP; Schiemann, J; Whitesides, J, 2016
)
0.43
"3% BRV-treated patients reported treatment-emergent adverse events (TEAEs) during the treatment period; most commonly, headache (25."( Tolerability, safety, and efficacy of adjunctive brivaracetam for focal seizures in older patients: A pooled analysis from three phase III studies.
Brodie, MJ; D'Souza, J; Johnson, ME; Schiemann, J; Whitesides, J, 2016
)
0.43
" In the SGTCS safety population (N=487), treatment-emergent adverse events (TEAEs) were reported by 60."( Efficacy, safety, and tolerability of adjunctive brivaracetam for secondarily generalized tonic-clonic seizures: Pooled results from three Phase III studies.
Asadi-Pooya, AA; Diaz, A; Elmouft, S; Moseley, BD; Schiemann, J; Sperling, MR; Whitesides, J, 2016
)
0.43
"To comprehensively evaluate the adverse events (AEs) significantly associated with brivaracetam (BRV) treatment in a large selection of randomized control trials."( The adverse event profile of brivaracetam: A meta-analysis of randomized controlled trials.
Chen, D; Chen, SH; Chen, T; Liu, L; Xu, D; Zhu, LN, 2017
)
0.46
" Serious AEs (SAEs), withdrawal, and treatment-emergent adverse effects were then assessed for their association with brivaracetam."( The adverse event profile of brivaracetam: A meta-analysis of randomized controlled trials.
Chen, D; Chen, SH; Chen, T; Liu, L; Xu, D; Zhu, LN, 2017
)
0.46
" Serious AEs, overall withdrawal, AE-related withdrawal and psychiatric adverse events (PAEs) were not significantly associated with BRV treatment."( The adverse event profile of brivaracetam: A meta-analysis of randomized controlled trials.
Chen, D; Chen, SH; Chen, T; Liu, L; Xu, D; Zhu, LN, 2017
)
0.46
" The content includes dose-related adverse effects, idiosyncratic reactions, behavioural and psychiatric comorbidities, chronic problems, enzyme induction and teratogenesis."( Tolerability and Safety of Commonly Used Antiepileptic Drugs in Adolescents and Adults: A Clinician's Overview.
Brodie, MJ, 2017
)
0.46
" Safety findings were generally similar to those of pivotal trials, with no major safety risks identified and with several specific adverse drug effects, such as hyponatremia, reported."( Comparing Safety and Efficacy of "Third-Generation" Antiepileptic Drugs: Long-Term Extension and Post-marketing Treatment.
Johnson, EL; Krauss, GL; Kwok, CS, 2017
)
0.46
" Behavioral changes are the most significant adverse effects reported by patients taking LEV."( Favorable adverse effect profile of brivaracetam vs levetiracetam in a preclinical model.
Aboulamer, S; Bosoi, CM; Carmant, L; Desgent, S; Gagné, J; Messiet, E; Sanon, NT; Simard, A; Wolf, DC, 2018
)
0.48
" In the LTG and TPM safety populations (n=245 versus n=125), treatment-emergent adverse events (TEAEs) were reported with LTG 68."( Efficacy, safety, and tolerability of brivaracetam with concomitant lamotrigine or concomitant topiramate in pooled Phase III randomized, double-blind trials: A post-hoc analysis.
Benbadis, S; Diaz, A; Elmoufti, S; Klein, P; Schiemann, J; Whitesides, J, 2018
)
0.48
" Treatment-emergent adverse events (TEAEs) considered drug related by the investigator were reported by 32/99 (32."( Safety and Tolerability of Adjunctive Brivaracetam in Pediatric Patients < 16 Years with Epilepsy: An Open-Label Trial.
Daniels, T; Dilley, D; Liu, E; McDonough, B; Stockis, A, 2019
)
0.51
"4%) and adverse events (AEs) (27%) of other antiepileptic drugs (AEDs)."( Efficacy, retention, and safety of brivaracetam in adult patients with genetic generalized epilepsy.
Abraira, L; Fonseca, E; Guzmán, L; Quintana, M; Salas-Puig, X; Santamarina, E; Toledo, M, 2020
)
0.56
" Treatment-emergent adverse events (TEAEs) were reported by 140/149 (94."( Safety and tolerability of adjunctive brivaracetam in children with focal seizures: Interim analysis of pooled data from two open-label trials.
Badalamenti, V; Elmoufti, S; Elshoff, JP; Gasalla, T; Patel, AD, 2020
)
0.56
" Adverse events (AEs) of interest were summarized in relevant categories."( Safety and tolerability of adjunctive brivaracetam in epilepsy: In-depth pooled analysis.
Badalamenti, V; Brandt, C; Gasalla, T; Klein, P; Whitesides, J, 2020
)
0.56
" Overall, the incidence of treatment-emergent adverse events (TEAEs) was 66."( Safety and tolerability of adjunctive brivaracetam in epilepsy: In-depth pooled analysis.
Badalamenti, V; Brandt, C; Gasalla, T; Klein, P; Whitesides, J, 2020
)
0.56
" Treatment-emergent adverse events (TEAEs) occurred in 91."( Long-term safety, efficacy, and quality of life outcomes with adjunctive brivaracetam treatment at individualized doses in patients with epilepsy: An up to 11-year, open-label, follow-up trial.
Biton, V; Borghs, S; He, QJ; O'Brien, TJ; Schulz, AL; Yates, S, 2020
)
0.56
"Treatment-emergent adverse events (TEAEs) in clinical trials are typically reported for the full duration of the treatment period including titration and maintenance."( Time course of drug-related treatment-emergent adverse side effects of brivaracetam.
Elmoufti, S; Fishman, J; Gasalla, T; Klein, P; Laloyaux, C; Martin, MS; Meador, KJ, 2020
)
0.56
" Safety variables included treatment-emergent adverse events (TEAEs)."( Long-term safety and efficacy of brivaracetam in adults with focal seizures: Results from an open-label, multinational, follow-up trial.
Arnold, S; Elmoufti, S; Fakhoury, T; Laloyaux, C; Schulz, AL; Yates, S, 2020
)
0.56
"3 %)] and adverse events [16 (14."( Long-term safety and efficacy of brivaracetam in adults with focal seizures: Results from an open-label, multinational, follow-up trial.
Arnold, S; Elmoufti, S; Fakhoury, T; Laloyaux, C; Schulz, AL; Yates, S, 2020
)
0.56
" Safety variables included treatment-emergent adverse events (TEAEs)."( Safety, tolerability, and efficacy of brivaracetam as adjunctive therapy in patients with focal seizures, generalized onset seizures, or Unverricht-Lundborg disease: An open-label, long-term follow-up trial.
Baulac, M; Ben-Menachem, E; Brandt, C; Cleveland, JM; Hong, SB; Reichel, C; Schulz, AL; Wagener, G, 2021
)
0.62
" Treatment-emergent adverse events (TEAEs) were reported by 643 (83."( Long-term safety, efficacy, and quality of life during adjunctive brivaracetam treatment in patients with uncontrolled epilepsy: An open-label follow-up trial.
Brandt, C; Cleveland, JM; Klein, P; Quarato, PP; Schulz, AL; Toledo, M; Wagener, G, 2021
)
0.62
"In this select group of patients who entered the LTFU trial, BRV was generally safe and well tolerated."( Long-term safety, efficacy, and quality of life during adjunctive brivaracetam treatment in patients with uncontrolled epilepsy: An open-label follow-up trial.
Brandt, C; Cleveland, JM; Klein, P; Quarato, PP; Schulz, AL; Toledo, M; Wagener, G, 2021
)
0.62
"To understand the currently available post-marketing real-world evidence of the incidences of and discontinuations due to the BAEs of irritability, anger, and aggression in people with epilepsy (PWE) treated with the anti-seizure medications (ASMs) brivaracetam (BRV), levetiracetam (LEV), perampanel (PER), and topiramate (TPM), as well as behavioral adverse events (BAEs) in PWE switching from LEV to BRV."( Behavioral adverse events with brivaracetam, levetiracetam, perampanel, and topiramate: A systematic review.
Klein, P; Klitgaard, H; Laloyaux, C; Moseley, BD; Ricchetti-Masterson, K; Rosenow, F; Sirven, JI; Smith, B; Steinhoff, BJ; Stern, JM; Toledo, M; Villanueva, V; Zipfel, PA, 2021
)
0.62
" Behavioral and psychiatric adverse events in PWE switching from LEV to BRV were summarized descriptively."( Behavioral adverse events with brivaracetam, levetiracetam, perampanel, and topiramate: A systematic review.
Klein, P; Klitgaard, H; Laloyaux, C; Moseley, BD; Ricchetti-Masterson, K; Rosenow, F; Sirven, JI; Smith, B; Steinhoff, BJ; Stern, JM; Toledo, M; Villanueva, V; Zipfel, PA, 2021
)
0.62
" Outcomes included BRV plasma concentrations before and after IV administration, treatment-emergent adverse events (TEAEs), and discontinuations due to TEAEs."( Pharmacokinetics, safety, and tolerability of intravenous brivaracetam in pediatric patients with epilepsy: An open-label trial.
Bozorg, A; Elshoff, JP; Farkas, MK; Fogarasi, A; James, GD; Kang, H; Krauwinkel, W; Morita, D; Will, E, 2022
)
0.72
" Efficacy variables were derived from seizure-related changes, and tolerability and safety variables from reported treatment-emergent adverse events (TEAEs), BRV withdrawal, and changes to questionnaire scores."( BRIVEST: A 'real-world' observational, single-centre study investigating the efficacy, safety and tolerability of Brivaracetam.
Cavill, R; Manuel, M; Naddell, S; Sieradzan, K; White, P, 2023
)
0.91
" Adverse events, vital signs, electrocardiograms, laboratory tests, general and neurological examinations, and psychometric rating scales were recorded at regular intervals."( Pharmacokinetics, Safety, and Tolerability of Brivaracetam in Healthy Elderly Participants.
Krauwinkel, W; Nicolas, JM; Sargentini-Maier, ML; Stockis, A, 2023
)
0.91
" Outcomes included treatment-emergent adverse events (TEAEs), behavior assessments (Achenbach Child Behavior Checklist [CBCL], Behavior Rating Inventory of Executive Function [BRIEF]/BRIEF-Preschool version [BRIEF-P]), and efficacy outcomes (percent change in focal seizure frequency, 50% responder rate for all seizure types for patient subgroups <2 years and ≥2 years of age using daily record card data)."( Long-term safety and efficacy of adjunctive brivaracetam in pediatric patients with epilepsy: An open-label, follow-up trial.
Elshoff, JP; Fleyshman, S; Floricel, F; Fogarasi, A; Kang, H; Klotz, KA; Lagae, L; Reichel, C, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" Brivaracetam was found to have desirable pharmacokinetic properties."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after single increasing oral doses in healthy males.
Connell, J; Jacobs, T; Pigeolet, E; Riethuisen, JM; Rolan, P; Sargentini-Maier, ML; Stockis, A; Tytgat, D, 2007
)
0.34
" Pharmacodynamic tests showed dose-related sedation and decreased alertness that only persisted at 800 mg daily."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men.
Pigeolet, E; Rolan, P; Sargentini-Maier, ML; Stockis, A, 2008
)
0.35
" Brivaracetam had a favourable pharmacokinetic profile in this population, characterized by rapid absorption, volume of distribution limited to total body water, apparent single-compartment elimination and dose proportionality."( The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men.
Pigeolet, E; Rolan, P; Sargentini-Maier, ML; Stockis, A, 2008
)
0.35
" A physiologically based pharmacokinetic model was developed for predicting BRV concentrations in human plasma and brain tissue."( Physiologically based pharmacokinetic/pharmacodynamic animal-to-man prediction of therapeutic dose in a model of epilepsy.
Brochot, A; Stockis, A; Zamacona, M, 2010
)
0.36
" A population pharmacokinetic (PK) model and a population pharmacokinetic/pharmacodynamic (PKPD) model were developed describing brivaracetam plasma concentration and the relationship with daily seizure counts in adequate well-controlled efficacy trials."( Brivaracetam Population Pharmacokinetics and Exposure-Response Modeling in Adult Subjects With Partial-Onset Seizures.
Schoemaker, R; Stockis, A; Wade, JR, 2016
)
0.43
"The aims of the study were to develop a population pharmacokinetic model of orally administered brivaracetam in paediatric patients and to provide dosing suggestions."( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years.
Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
" Pharmacokinetic analysis was performed using non-linear mixed effects modelling, and a stepwise covariate search was used to determine factors influencing brivaracetam clearance."( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years.
Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
" BRV shares many of the pharmacokinetic characteristics of an ideal ASMs."( Brivaracetam for the treatment of focal-onset seizures: pharmacokinetic and pharmacodynamic evaluations.
de Biase, S; Gigli, GL; Valente, M, 2020
)
0.56
"We present pharmacokinetic data during pregnancy and lactation for brivaracetam, lacosamide and perampanel based on two case studies."( Pharmacokinetic data on brivaracetam, lacosamide and perampanel during pregnancy and lactation.
Brodtkorb, E; Burns, ML; Johannessen, SI; Landmark, CJ; Rektorli, L; Revdal, E, 2021
)
0.62
" No unexpected safety or pharmacokinetic differences were observed between patients receiving 15-min infusions or bolus, and plasma concentrations were in the expected range."( Pharmacokinetics, safety, and tolerability of intravenous brivaracetam in pediatric patients with epilepsy: An open-label trial.
Bozorg, A; Elshoff, JP; Farkas, MK; Fogarasi, A; James, GD; Kang, H; Krauwinkel, W; Morita, D; Will, E, 2022
)
0.72
" The purpose of this study was to evaluate clinical experience with BRV with focus on efficacy, tolerability and pharmacokinetic variability among adult patients with difficult-to-treat epilepsy."( Efficacy, tolerability and pharmacokinetic variability of brivaracetam in adults with difficult-to-treat epilepsy.
Brodtkorb, E; Burns, ML; Johannessen, SI; Landmark, CJ; Linge, HL; Lossius, MI; Nakken, KO; Svendsen, T, 2022
)
0.72
" Pharmacokinetic variability between patients was considerable; 14-fold variation in concentration/dose (C/D)-ratios."( Efficacy, tolerability and pharmacokinetic variability of brivaracetam in adults with difficult-to-treat epilepsy.
Brodtkorb, E; Burns, ML; Johannessen, SI; Landmark, CJ; Linge, HL; Lossius, MI; Nakken, KO; Svendsen, T, 2022
)
0.72
" The combination of clinical and pharmacokinetic data provides insight into factors contributing to efficacy and tolerability of new ASMs."( Efficacy, tolerability and pharmacokinetic variability of brivaracetam in adults with difficult-to-treat epilepsy.
Brodtkorb, E; Burns, ML; Johannessen, SI; Landmark, CJ; Linge, HL; Lossius, MI; Nakken, KO; Svendsen, T, 2022
)
0.72
" This study utilized physiologically based pharmacokinetic (PBPK) modeling to explore the pharmacokinetics of BRV and drug interactions between BRV and rifampin (RIF), a CYP2C19 inducer, based on CYP2C19 genetic polymorphisms."( Physiologically based pharmacokinetic modeling of brivaracetam and its interactions with rifampin based on CYP2C19 phenotypes.
Jiang, X; Wang, L; Yang, H; Yang, L; Zheng, L; Zhong, X, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" Brivaracetam does not interact with most metabolizing enzymes and drug transporters, and therefore does not interfere with drugs that use these metabolic routes."( A review of the drug-drug interactions of the antiepileptic drug brivaracetam.
Chanteux, H; Gidal, B; Laloyaux, C; Moseley, BD; Nicolas, JM; Stockis, A, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
"To determine the bioequivalence of brivaracetam oral tablet formulations (10, 75, and 100 mg) versus 50 mg oral tablet and to compare the bioavailability of brivaracetam 100 mg intravenous (i."( Bioavailability and bioequivalence comparison of brivaracetam 10, 50, 75, and 100 mg tablets and 100 mg intravenous bolus.
Hadi, S; Hartstra, J; Mollet, M; Stockis, A, 2016
)
0.43
" Bioavailability comparisons were based on the 90% confidence intervals (CIs) around the geometric least squares mean ratios (test: reference)."( Bioavailability and bioequivalence comparison of brivaracetam 10, 50, 75, and 100 mg tablets and 100 mg intravenous bolus.
Hadi, S; Hartstra, J; Mollet, M; Stockis, A, 2016
)
0.43
", bolus had bioavailability similar to that of 50 and 100 mg tablets."( Bioavailability and bioequivalence comparison of brivaracetam 10, 50, 75, and 100 mg tablets and 100 mg intravenous bolus.
Hadi, S; Hartstra, J; Mollet, M; Stockis, A, 2016
)
0.43
" Furthermore, the pharmacokinetic studies in volunteers exhibited that the bioavailability of F5 and F10 was 95."( Design and evaluation of gastro-swelling/gastro-floating sustained-release tablets of brivaracetam for epilepsy therapy.
Cheng, X; Ding, J; Hou, Z; Li, Y; Lin, J; Zhang, H; Zhao, X, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" Plasma samples were obtained before and up to 12 h after last dosing for drug determination."( Effect of brivaracetam on cardiac repolarisation--a thorough QT study.
Astruc, B; Hulhoven, R; Meeus, MA; Rosillon, D; Stockis, A; Troenaru, MM; Watanabe, S, 2008
)
0.35
" Various dosing regimens of the new compound were simulated in order to reach the same brain SV2A occupancy as for the reference compound."( Physiologically based pharmacokinetic/pharmacodynamic animal-to-man prediction of therapeutic dose in a model of epilepsy.
Brochot, A; Stockis, A; Zamacona, M, 2010
)
0.36
"A randomized, double-blind, placebo-controlled, four-way cross-over design was employed in 16 healthy volunteers comparing acute dosing (i."( Neurocognitive effects of brivaracetam, levetiracetam, and lorazepam.
Gevins, A; Leese, PT; Loring, DW; Meador, KJ; Otoul, C, 2011
)
0.37
" Further large clinical and pharmacovigilance studies are needed to investigate the long-term efficacy and safety of BRV and, furthermore, to suggest an optimal BRV dosage for clinical use."( Adjunctive brivaracetam for patients with refractory partial seizures: A meta-analysis of randomized placebo-controlled trials.
Huang, S; Ma, J; You, C, 2015
)
0.42
" Plasma and brain levels were measured over time after single oral dosing to audiogenic mice and were correlated with anticonvulsant activity."( Brivaracetam, a selective high-affinity synaptic vesicle protein 2A (SV2A) ligand with preclinical evidence of high brain permeability and fast onset of action.
Carson, RE; Chanteux, H; Hannestad, J; Holden, D; Huang, Y; Kervyn, S; Klitgaard, H; Matagne, A; Mathy, FX; Mercier, J; Nabulsi, N; Nicolas, JM; Staelens, L; Stockis, A; Tytgat, D, 2016
)
0.43
" Simulation allowed characterization of the dose-response curve, suggesting maximum response is obtained at brivaracetam 150-200 mg/day."( Brivaracetam Population Pharmacokinetics and Exposure-Response Modeling in Adult Subjects With Partial-Onset Seizures.
Schoemaker, R; Stockis, A; Wade, JR, 2016
)
0.43
" There is no need to limit brivaracetam dosing when used concomitantly with carbamazepine."( Pharmacokinetic interaction of brivaracetam on carbamazepine in adult patients with epilepsy, with and without valproate co-administration.
Brodie, MJ; Sargentini-Maier, ML; Stockis, A, 2016
)
0.43
"The aims of the study were to develop a population pharmacokinetic model of orally administered brivaracetam in paediatric patients and to provide dosing suggestions."( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years.
Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
" Simulations were performed to investigate dosing regimens."( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years.
Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
" Data suggest no need to change brivaracetam dosing when used concomitantly with carbamazepine, phenobarbital or valproate."( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years.
Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
"Simulation with the adult brivaracetam PK/PD model in combination with an existing pediatric brivaracetam population PK model allowed characterization of the dose-response curve, suggesting maximum response at brivaracetam 4 mg/kg/day dosing (capped at 200 mg/day, the maximum adult dose) in children aged ≥4 years."( Extrapolation of a Brivaracetam Exposure-Response Model from Adults to Children with Focal Seizures.
Schoemaker, R; Stockis, A; Wade, JR, 2018
)
0.48
" The goal of the present analysis was to determine if the dose-response of brivaracetam as monotherapy would fall within the range associated with brivaracetam efficacy as adjunctive therapy."( Evaluation of brivaracetam efficacy as monotherapy in adult patients with focal seizures.
D'Souza, J; Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
" AED extension studies evaluate treatment retention, drug tolerability, and drug safety during individualized treatment with flexible dosing and thus provide information not available in rigid pivotal trials."( Comparing Safety and Efficacy of "Third-Generation" Antiepileptic Drugs: Long-Term Extension and Post-marketing Treatment.
Johnson, EL; Krauss, GL; Kwok, CS, 2017
)
0.46
"The number of patients in each of the three BRV dosage groups was small, particularly for the TPM subgroup."( Efficacy, safety, and tolerability of brivaracetam with concomitant lamotrigine or concomitant topiramate in pooled Phase III randomized, double-blind trials: A post-hoc analysis.
Benbadis, S; Diaz, A; Elmoufti, S; Klein, P; Schiemann, J; Whitesides, J, 2018
)
0.48
" Target dosage was achieved by 30."( BRIVA-LIFE-A multicenter retrospective study of the long-term use of brivaracetam in clinical practice.
López-González, FJ; Mauri, JA; Montoya, J; Olivé-Gadea, M; Rodriguez-Uranga, J; Ruiz-Giménez, J; Villanueva, V; Zurita, J, 2019
)
0.51
" Responders received significantly greater median loading dosage per body weight (3."( Intravenous brivaracetam in status epilepticus: Correlation between loading dose, plasma levels and clinical response.
Aicua-Rapun, I; André, P; Buclin, T; Decosterd, LA; Novy, J; Rossetti, AO, 2019
)
0.51
" In vitro and in vivo animal studies suggest faster brain penetration and SV2A occupancy (SO) after dosing with BRV than LEV."( A single-center, open-label positron emission tomography study to evaluate brivaracetam and levetiracetam synaptic vesicle glycoprotein 2A binding in healthy volunteers.
Carson, RE; DeBruyn, S; Finnema, SJ; Gao, H; Hannestad, J; Henry, S; Huang, Y; Kaminski, RM; Kervyn, S; Klitgaard, H; Maguire, RP; Martin, P; Matuskey, D; Mercier, J; Muglia, P; Nabulsi, NB; Naganawa, M; Nicolas, JM; Otoul, C; Pracitto, R; Rossano, S; Stockis, A, 2019
)
0.51
" Cohort 3 (n = 4) was examined at baseline and steady state after 4 days of twice-daily oral dosing of BRV (50-100 mg) and 4 hours postdose of LEV (250-600 mg)."( A single-center, open-label positron emission tomography study to evaluate brivaracetam and levetiracetam synaptic vesicle glycoprotein 2A binding in healthy volunteers.
Carson, RE; DeBruyn, S; Finnema, SJ; Gao, H; Hannestad, J; Henry, S; Huang, Y; Kaminski, RM; Kervyn, S; Klitgaard, H; Maguire, RP; Martin, P; Matuskey, D; Mercier, J; Muglia, P; Nabulsi, NB; Naganawa, M; Nicolas, JM; Otoul, C; Pracitto, R; Rossano, S; Stockis, A, 2019
)
0.51
" Gender, duration of epilepsy, and dosage did not affect epilepsy control."( Treatment with brivaracetam in children - The experience of a pediatric epilepsy center.
Bar-Yosef, O; Ben-Zeev, B; Nissenkorn, A; Tzadok, M, 2019
)
0.51
" Furthermore, most preclinical antiepileptogenic studies lack information needed for translation, such as dose-blood level relationship, brain target engagement, and dose-response, and many use treatment parameters that cannot be applied clinically, for example, treatment initiation before or at the time of injury and dosing higher than tolerated human equivalent dosing."( Repurposed molecules for antiepileptogenesis: Missing an opportunity to prevent epilepsy?
Bar-Klein, G; Friedman, A; Hameed, MQ; Jozwiak, S; Kaminski, RM; Klein, P; Klitgaard, H; Koepp, M; Löscher, W; Prince, DA; Rotenberg, A; Twyman, R; Vezzani, A; Wong, M, 2020
)
0.56
" Patients entered LTFU at a recommended BRV dose of 100 mg/day, with flexible dosing of 50-200 mg/day, as monotherapy or adjunctive therapy; additional AEDs could be prescribed and adapted in dose if clinically indicated."( Long-term safety and efficacy of brivaracetam in adults with focal seizures: Results from an open-label, multinational, follow-up trial.
Arnold, S; Elmoufti, S; Fakhoury, T; Laloyaux, C; Schulz, AL; Yates, S, 2020
)
0.56
" Target dosing was 200 mg/day."( Adjunctive brivaracetam - A prospective audit of outcomes from an epilepsy clinic.
Brodie, MJ; Stephen, L, 2021
)
0.62
"0 mg and the mean daily dosage was 195."( Real-life evidence about the use of intravenous brivaracetam in urgent seizures: The BRIV-IV study.
Asensio, M; Campos, D; Castillo, A; Chavarria, B; Escalza, I; Falip, M; Fernández-Cabrera, A; Garcés, M; García-Morales, I; Gifreu, A; Giménez, J; Guillén, V; Hampel, K; Hernández Pérez, G; Juiz-Fernández, Á; Martínez, AB; Massot, M; Montoya, J; Parejo-Carbonell, B; Rocamora, R; Rodriguez-Osorio, X; Rubio-Nazábal, E; Ruiz-Giménez, J; Santamarina, E; Sayas, D; Villanueva, V, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
anticonvulsantA drug used to prevent seizures or reduce their severity.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
gamma-lactamA lactam in which the amide bond is contained within a five-membered ring, which includes the amide nitrogen and the carbonyl carbon.
non-proteinogenic amino acid derivativeAny derivative of a non-proteinogenic amino acid resulting from reaction at an amino group or carboxy group, or from the replacement of any hydrogen by a heteroatom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID10673Maximum time to achieve peak plasma concentration was determined in rat at 10 mg/kg2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
AID11197Total clearance at 10 mg/kg was determined in rat2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
AID10445Half life at 10 mg/kg was determined in rat2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
AID102959In vitro inhibitory activity against [3H](2S)-2-[4-(3-azidophenyl)-2-oxopyrrolidin-1-yl]butanamide binding to levetiracetam binding site2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
AID13327Oral bioavailability at 10 mg/kg was determined in rat2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
AID113197In vivo dose required to protect 50% audiogenic seizure prone mice against clonic convulsions2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
AID1346078Rat synaptic vesicle glycoprotein 2A (Atypical major facilitator superfamily (MSF) proteins)2004Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (244)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's15 (6.15)29.6817
2010's129 (52.87)24.3611
2020's100 (40.98)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials64 (25.40%)5.53%
Reviews61 (24.21%)6.00%
Case Studies8 (3.17%)4.05%
Observational8 (3.17%)0.25%
Other111 (44.05%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]