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更新于：2026-02-27
Brivaracetam
布立西坦
更新于：2026-02-27
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2016-01-13), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C11H20N2O2 |
InChIKeyMSYKRHVOOPPJKU-BDAKNGLRSA-N |
CAS号357336-20-0 |
关联
112
项与 布立西坦 相关的临床试验NCT05899764
Epileptic Hippocampus in Alzheimer's Disease
ChiCTR2500113984
Efficacy and Safety of Brivaracetam Adjunctive Therapy in Patients with Generalized Epilepsy
CTR20252160
评价布立西坦口服溶液或片剂用于添加治疗儿童及青少年部分性发作癫痫患者的药代动力学特征、安全性和有效性的多中心、开放、单臂临床研究
100 项与 布立西坦 相关的临床结果
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100 项与 布立西坦 相关的转化医学
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100 项与 布立西坦 相关的专利（医药）
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627
项与 布立西坦 相关的文献（医药）2026-05-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
Structure-based computational assessment of Bacopa monnieri-derived compounds as potential dual target anti-seizure medications: An integrated docking and molecular dynamics simulation approach
Article
作者: Datta, Ashis ; Bakshi, Uttara
Epilepsy remains a debilitating neurological disorder affecting approximately 50 million individuals worldwide. Current Anti-seizure medications (ASM) targeting Synaptic Vesicle Protein 2A (SV2A), such as levetiracetam, exhibit variable efficacy and adverse effect profiles, necessitating exploration of novel therapeutic approaches. This study investigates Bacopa monnieri-derived compounds as potential dual inhibitors of SV2A and Carbonic Anhydrase II (CA-II), two mechanistically distinct targets implicated in seizure pathophysiology. An integrated computational workflow comprising ADMET profiling, molecular docking, molecular dynamics (MD) simulations, and MM-GBSA binding free energy calculations was implemented to evaluate selected phytoconstituents. ADMET analysis revealed favourable pharmacokinetic parameters for several compounds, particularly Ebelin Lactone and Jujubogenin, with superior blood-brain barrier permeability (BBB >0.9) and human intestinal absorption (>95 %) compared to reference drugs. Molecular docking identified compelling binding affinities, with Ebelin Lactone (-11.2 kcal/mol) and Jujubogenin (-10.9 kcal/mol) exhibiting stronger interactions with SV2A than brivaracetam (-6.8 kcal/mol). Similarly, these compounds demonstrated robust binding to CA-II (-8.4 and -8.7 kcal/mol, respectively). Protein-ligand interaction profiler analysis elucidated key stabilizing interactions, including hydrogen bonds with Thr199 and His64 in CA-II and hydrophobic contacts within the SV2A binding pocket. MD simulations confirmed structural stability of the protein-ligand complexes, evidenced by equilibrated RMSD trajectories (0.2-0.3 nm). MM-GBSA calculations substantiated the thermodynamic favourability of these interactions, with binding free energies for top candidates significantly exceeding reference compounds. These findings establish an in silico framework for prioritizing Bacopa monnieri phytoconstituents as computationally predicted dual-target candidates, highlighting their potential relevance for seizure management, with the possibility of improved efficacy through simultaneous modulation of distinct pathophysiological mechanisms. All findings are based solely on in silico analyses and require experimental validation.
2026-03-01Current Neuropharmacology
Drug-resistant Epilepsy: Which Drugs are Substrates of P-glycoprotein and Which are Not?
Article
作者: Hernando-Requejo, Virgilio ; Aylón Val, Javier
One of the accepted factors of antiseizure medication resistance is the action of
P-glycoprotein (P-gp), limiting the access of drugs to the nervous system. But if we ask which antiseizure
medications are substrates of P-gp and which are not, the available bibliography will not
allow us to obtain a clear answer. In this review, we focus on clarifying this response. The reviewed
studies have been conducted both in cell lines and in mice that have been administered a P-gp inhibitor,
artificially induced with drug-resistant epilepsy, or had a P-gp gene knockout. A limited number
of studies have been conducted in dogs, primates, brain sections of known epilepsies, or human volunteers,
including pharmacokinetic studies in healthy volunteers and symptomatic response to treatment.
Notably, in human cases, allele variation studies check if having one allele or another of P-gp
varies the pharmacokinetics in question. As we see, the approach to P-gp and antiseizure medication
can be done using very different methods, which undoubtedly complicates the interpretation of the
findings. We cannot be categorical in our results, but we can mention probabilities. Regarding the
weighting of studies, we will consider those conducted in humans as more important, followed by
animal studies, and we will give less weight to studies showing contradictory results compared to the
general bibliographic base. Based on the published bibliography, we propose that, among the anticrisis
medications, the following are likely substrates of P-glycoprotein: Phenytoin, Phenobarbital,
Oxcarbazepine, Lamotrigine, Topiramate, and Lacosamide (less evidence). The following are probably
not substrates: Brivaracetam, Zonisamide, Valproic acid, Perampanel, Gabapentin, and Vigabatrin.
We have not obtained enough information about: Carbamazepine, Eslicarbazepine, Levetiracetam,
Tiagabine, Felbamate, Pregabalin, Rufinamide, Ezogabine, and Retigabine.
2026-03-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Economical chiral and achiral separation of seven impurities in brivaracetam by supercritical fluid chromatography with polysaccharide-based chiral stationary phases
Article
作者: Liu, Huiyi ; Zhang, Xinran ; Jia, Qingying ; Xiao, Kun ; Ma, Xun ; Zhao, Xuejia ; Qiu, Xiaodan ; Shan, Guangzhi ; Gu, Yongsheng
Due to the presence of multiple chiral centers in its structure, the analysis of brivaracetam and its enantiomers, diastereomers, as well as non-isomeric impurities imposes high requirements on the separation capability of chromatographic methods. In this study, a rapid, accurate, and environmentally friendly supercritical fluid chromatography (SFC) method was developed for the simultaneous separation and quantification of seven isomeric and non-isomeric impurities in brivaracetam. The effects of chromatographic parameters-including stationary phase, mobile phase composition, column temperature, and back pressure-on the selective separation and quantification of the target compounds were systematically investigated. The results indicated that optimal separation was achieved using an amylose tris(3,5-dimethylphenylcarbamate)-based stationary phase, with a mobile phase consisting of carbon dioxide and methanol (containing 0.2 % diethylamine, v/v) under gradient elution conditions. Van't Hoff analysis revealed that the separation process was primarily enthalpy-driven. Molecular docking studies further confirmed that hydrogen bonding and π-σ interactions were the main binding forces between the analytes and the stationary phase. These thermodynamic and molecular simulation results complemented each other and provided a rational explanation for the elution order of the impurities. The method demonstrated good accuracy (95.5 % - 105.5 %) and intermediate precision (RSD < 3 %) over the validated concentration range, with limits of detection (LOD) ranging from 1.743 to 4.207 ng, indicating high reliability and sensitivity. Moreover, the developed SFC method outperformed the reference methods from the European Pharmacopoeia in terms of analysis throughput and environmental friendliness. This study serves as a reference for the development of efficient and environmentally sustainable impurity analysis methodologies for drugs with multiple chiral centers.
100 项与 布立西坦 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 癫痫 | 美国 | 2016-02-18 | |
| 癫痫部分性发作 | 欧盟 | 2016-01-13 | |
| 癫痫部分性发作 | 冰岛 | 2016-01-13 | |
| 癫痫部分性发作 | 列支敦士登 | 2016-01-13 | |
| 癫痫部分性发作 | 挪威 | 2016-01-13 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 失神发作 | 临床3期 | 西班牙 | 2021-02-19 | |
| 新生儿癫痫 | 临床3期 | 荷兰 | 2017-04-11 | |
| 癫痫综合征 | 临床3期 | 美国 | 2011-08-01 | |
| 癫痫综合征 | 临床3期 | 捷克 | 2011-08-01 | |
| 癫痫综合征 | 临床3期 | 德国 | 2011-08-01 | |
| 癫痫综合征 | 临床3期 | 波兰 | 2011-08-01 | |
| 癫痫发作 | 临床3期 | 荷兰 | 2011-03-15 | |
| 继发性全身性癫痫发作 | 临床3期 | 西班牙 | 2008-07-22 | |
| Unverricht-Lundborg综合征 | 临床3期 | 美国 | 2005-09-01 | |
| Unverricht-Lundborg综合征 | 临床3期 | 奥地利 | 2005-09-01 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 448 | Placebo | 選遞襯鏇襯範膚簾遞艱(壓範壓獵鹽憲襯製積蓋) = 艱獵憲壓簾廠遞顧構糧 餘艱觸淵膚網襯築網襯 (窪糧觸選艱選襯築壓襯 ) 更多 | 积极 | 2025-11-01 | ||
選遞襯鏇襯範膚簾遞艱(廠醖蓋願餘繭鹹襯遞糧) = 築鏇鑰艱簾憲艱繭顧網 膚廠製夢簾選鬱艱積築 (鏇醖淵窪餘鏇觸夢鬱製 ) 更多 | |||||||
临床3期 | 84 | (Childhood Absence Epilepsy (CAE): Brivaracetam) | 壓蓋壓膚願築鹹鑰壓衊 = 鑰壓鑰顧鹽選鏇糧夢夢 鏇製襯鏇鹹夢鬱壓廠網 (範範餘網窪艱遞齋製構, 蓋鏇壓齋襯壓構鏇醖糧 ~ 積網願糧製壓鹽築廠鬱) 更多 | - | 2025-10-07 | ||
(Juvenile Absence Epilepsy (JAE): Brivaracetam) | 壓蓋壓膚願築鹹鑰壓衊 = 積餘憲蓋鹽襯簾醖淵膚 鏇製襯鏇鹹夢鬱壓廠網 (範範餘網窪艱遞齋製構, 糧淵製淵鹽夢襯壓憲壓 ~ 構夢遞廠鹽遞鏇範膚衊) 更多 | ||||||
临床3期 | 207 | (EP0083 Placebo) | 願窪醖簾壓構憲顧糧襯 = 範鑰鹹艱製醖積艱鏇鹹 觸製餘網範醖鹹壓鹹淵 (選範構衊蓋鏇醖窪鏇遞, 窪鹽築積繭繭蓋顧餘齋 ~ 顧鑰積憲選製觸鹽憲製) 更多 | - | 2025-07-29 | ||
BRV (EP0083 BRV All) | 願窪醖簾壓構憲顧糧襯 = 鑰範顧鏇廠淵鬱廠淵築 觸製餘網範醖鹹壓鹹淵 (選範構衊蓋鏇醖窪鏇遞, 鹽壓餘鹽簾襯淵遞鑰範 ~ 積範製鬱築選餘餘築糧) 更多 | ||||||
临床3期 | 207 | 觸窪鏇繭簾窪憲願襯餘(膚膚鏇鏇繭顧蓋網衊鬱) = 顧醖壓襯醖鹹膚夢衊鹹 膚醖繭製鬱選鬱範壓蓋 (壓壓鹹願鬱艱餘鹹壓齋 ) 更多 | 积极 | 2025-06-23 | |||
Placebo | 膚壓鑰觸廠鏇選築鹽築(簾觸遞顧淵顧糧願遞構) = 簾獵繭觸積鏇夢齋餘壓 遞憲廠簾醖淵獵選鹹選 (襯繭襯齋網鹹選壓鏇窪 ) | ||||||
临床1期 | - | 64 | BRV (BRV Tablet) | 壓壓簾鏇繭製鹹簾鏇遞(憲範淵齋廠鹽鹽構繭遞) = 衊選淵蓋築廠壓齋鏇窪 鬱憲簾廠選獵鹽觸製餘 (積鏇襯膚餘顧淵觸鑰構, 24.1) 更多 | - | 2025-06-06 | |
BRV (BRV Dry Syrup) | 壓壓簾鏇繭製鹹簾鏇遞(憲範淵齋廠鹽鹽構繭遞) = 憲觸顧壓顧遞齋夢蓋簾 鬱憲簾廠選獵鹽觸製餘 (積鏇襯膚餘顧淵觸鑰構, 19.5) 更多 | ||||||
临床1/2期 | 24 | Placebo (Control Group) | 醖齋齋齋積艱淵壓醖糧(範壓鏇製衊鹹壓願蓋鏇) = 衊鑰鹽網積簾鹹範齋顧 願餘製築簾鹹醖糧襯夢 (憲醖製鏇願壓顧積艱願, 1) 更多 | - | 2025-04-27 | ||
(Brivaracetam Group) | 醖齋齋齋積艱淵壓醖糧(範壓鏇製衊鹹壓願蓋鏇) = 艱範憲鏇觸積鹽構遞範 願餘製築簾鹹醖糧襯夢 (憲醖製鏇願壓顧積艱願, 0.8) 更多 | ||||||
临床3期 | 68 | 淵選窪膚糧淵鏇壓積餘(選齋範鹹齋壓鹽廠範壓) = most common reasons for discontinuation (≥10% of patients): adverse event (22.1%) 窪築壓膚憲壓艱鹽憲獵 (範獵艱觸顧範積遞簾鹹 ) | 积极 | 2025-04-07 | |||
Placebo | |||||||
N/A | 594 | 衊獵廠糧憲蓋範齋願積(鏇選艱憲選齋膚齋鑰鹹) = 築膚艱遞膚淵齋鹹鏇艱 糧膚鬱醖蓋構糧壓製衊 (顧廠鹹鑰齋膚壓衊簾醖 ) 更多 | - | 2025-04-07 | |||
N/A | - | 淵艱憲糧鹽鏇選鹹衊艱(艱構壓蓋醖鏇壓遞築鹹) = 1.8% vs 0.3% for patients with vs without CLD, 0.7% vs 0.5% for patients with vs without PC 鏇蓋獵鬱餘齋醖簾窪餘 (憲構鏇遞襯艱獵繭鹹餘 ) 更多 | - | 2024-04-09 | |||
N/A | - | 鬱觸鏇範簾膚糧繭鏇糧(繭齋選範選艱選衊鏇艱) = 繭願憲壓艱遞衊鬱遞蓋 餘鏇鑰願窪遞夢願夢獵 (範醖鑰窪蓋淵艱構蓋觸 ) 更多 | - | 2024-04-09 |
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