更新于：2024-10-09
Lacosamide
拉考沙胺
更新于：2024-10-09
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 (2008-08-29), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C13H18N2O3 |
InChIKeyVPPJLAIAVCUEMN-GFCCVEGCSA-N |
CAS号175481-36-4 |
关联
180
项与 拉考沙胺 相关的临床试验A Bioequivalence study of a randomized, single dose, two-way crossover design with two-period, two-treatment, and two-sequence of Lacosamide Film Coated Tablet 100 mg (Test) relative to Vimpat Film Coated Tablet 100 mg (Reference) in healthy Thai adult volunteers under fasting condition.
- LACOS-06-23
Lacosamide Versus Topiramate in Migraine, a Ranodmized Trial
100 项与 拉考沙胺 相关的临床结果
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100 项与 拉考沙胺 相关的转化医学
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100 项与 拉考沙胺 相关的专利（医药）
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1,267
项与 拉考沙胺 相关的文献（医药）2024-11-01BRITISH JOURNAL OF PHARMACOLOGY
Arbidol, an antiviral drug, identified as a sodium channel blocker with anticonvulsant activity
Article
作者: Zhao, Miao ; Li, Min ; Yu, Haibo ; Jin, Yuchen ; Wu, Jun ; Yu, Kexin
Background and purpose:
Sodium channel blockers (SCBs) have traditionally been utilized as anti‐seizure medications by primarily targeting the inactivation process. In a drug discovery project aiming at finding potential anticonvulsants, we have identified arbidol, originally an antiviral drug, as a potent SCB. In order to evaluate its anticonvulsant potential, we have thoroughly examined its biophysical properties as well as its effects on animal seizure models.
Experimental approach:
Patch clamp recording was used to investigate the electrophysiological properties of arbidol, as well as the binding and unbinding kinetics of arbidol, carbamazepine and lacosamide. Furthermore, we evaluated the anticonvulsant effects of arbidol using three different seizure models in male mice.
Key results:
Arbidol effectively suppressed neuronal epileptiform activity by blocking sodium channels. Arbidol demonstrated a distinct mode of action by interacting with both the fast and slow inactivation of Nav1.2 channels compared with carbamazepine and lacosamide. A kinetic study suggested that the binding and unbinding rates might be associated with the specific characteristics of these three drugs. Arbidol targeted the classical binding site of local anaesthetics, effectively inhibited the gain‐of‐function effects of Nav1.2 epileptic mutations and exhibited varying degrees of anticonvulsant effects in the maximal electroshock model and subcutaneous pentylenetetrazol model but had no effect in the pilocarpine‐induced status epilepticus model.
Conclusions and implications:
Arbidol shows promising potential as an anticonvulsant agent, providing a unique mode of action that sets it apart from existing SCBs.
2024-10-01EPILEPSY & BEHAVIOR
Clinical characteristics and treatment approach of established New-Onset status epilepticus (eNOSE): A Real-World multicenter experience
Article
作者: Dono, Fedele ; Liviello, Davide ; Dasara, Michelangelo ; Rollo, Eleonora ; Della Marca, Giacomo ; Capriati, Luca ; Rodorigo, Davide ; Sensi, Stefano L ; Calabresi, Paolo ; Servidei, Serenella ; Quintieri, Paolo ; Vollono, Catello ; Evangelista, Giacomo ; Corniello, Clarissa ; Romozzi, Marina
INTRODUCTION:
Status Epilepticus (SE) can occur in patients without a previous epilepsy diagnosis, a condition identified as "new-onset status epilepticus" (NOSE). Treatment with benzodiazepine may fail in NOSE termination, requiring anti-seizure medication (ASM) employment. The term "established NOSE" (eNOSE) is generally employed in this context. This study aims to describe the main clinical characteristics of a large sample of patients suffering from eNOSE, compare the ASM efficacy, and explore the risk factors associated with ASM treatment unresponsiveness and eNOSE-associated mortality.
METHODS:
Adult patients diagnosed with eNOSE were retrospectively selected between January 2016 and December 2022. We reviewed demographics, clinical data, diagnostic work-up, and treatment. We considered the last ASM introduced before the eNOSE termination as effective.
RESULTS:
123 patients were included (age: 67.9 ± 17.3). eNOSE acute etiology was mostly reported. In the overall cohort, phenytoin showed the highest response rate (p = 0.01). In the pairwise comparisons, valproate was superior to levetiracetam (p = 0.02) but not to lacosamide (p = 0.50). Phenytoin had a significantly higher resolution rate than levetiracetam (p = 0.001) but not lacosamide (p = 0.14). Thirty patients were refractory to ASM treatment. No predictors of refractoriness were identified. Thirty-nine patients died. Age and GCS were identified as eNOSE-related mortality risk factors.
CONCLUSION:
eNOSE frequently has an acute etiology with several associated syndromes. Phenytoin is more effective in managing eNOSE, even though lacosamide, valproate, and levetiracetam can represent further therapeutic options. Age and GCS are the main risk factors for eNOSE-associated mortality.
2024-10-01PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY
Persistent sodium currents in neurons: potential mechanisms and pharmacological blockers
Review
作者: Müller, Peter ; Egorov, Alexei V ; Draguhn, Andreas
Abstract:
Persistent sodium current (INaP) is an important activity-dependent regulator of neuronal excitability. It is involved in a variety of physiological and pathological processes, including pacemaking, prolongation of sensory potentials, neuronal injury, chronic pain and diseases such as epilepsy and amyotrophic lateral sclerosis. Despite its importance, neither the molecular basis nor the regulation of INaP are sufficiently understood. Of particular significance is a solid knowledge and widely accepted consensus about pharmacological tools for analysing the function of INaP and for developing new therapeutic strategies. However, the literature on INaP is heterogeneous, with varying definitions and methodologies used across studies. To address these issues, we provide a systematic review of the current state of knowledge on INaP, with focus on mechanisms and effects of this current in the central nervous system. We provide an overview of the specificity and efficacy of the most widely used INaP blockers: amiodarone, cannabidiol, carbamazepine, cenobamate, eslicarbazepine, ethosuximide, gabapentin, GS967, lacosamide, lamotrigine, lidocaine, NBI-921352, oxcarbazepine, phenytoine, PRAX-562, propofol, ranolazine, riluzole, rufinamide, topiramate, valproaic acid and zonisamide. We conclude that there is strong variance in the pharmacological effects of these drugs, and in the available information. At present, GS967 and riluzole can be regarded bona fide INaP blockers, while phenytoin and lacosamide are blockers that only act on the slowly inactivating component of sodium currents.
100 项与 拉考沙胺 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 | 欧盟 | 2017-09-18 | |
| 癫痫 | 冰岛 | 2017-09-18 | |
| 癫痫 | 列支敦士登 | 2017-09-18 | |
| 癫痫 | 挪威 | 2017-09-18 | |
| 特发全身性癫痫 | 欧盟 | 2017-09-18 | |
| 特发全身性癫痫 | 冰岛 | 2017-09-18 | |
| 特发全身性癫痫 | 列支敦士登 | 2017-09-18 | |
| 特发全身性癫痫 | 挪威 | 2017-09-18 | |
| 癫痫发作 | 欧盟 | 2017-09-18 | |
| 癫痫发作 | 冰岛 | 2017-09-18 | |
| 癫痫发作 | 列支敦士登 | 2017-09-18 | |
| 癫痫发作 | 挪威 | 2017-09-18 | |
| 强直阵挛性癫痫 | 日本 | 2016-07-04 | |
| 癫痫部分性发作 | 欧盟 | 2008-08-29 | |
| 癫痫部分性发作 | 冰岛 | 2008-08-29 | |
| 癫痫部分性发作 | 列支敦士登 | 2008-08-29 | |
| 癫痫部分性发作 | 挪威 | 2008-08-29 |
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 |
|---|---|---|---|---|
| 糖尿病性神经病变 | 临床3期 | 德国 | 2003-12-01 | |
| 新生儿癫痫 | 临床2期 | 美国 | 2021-03-31 | |
| 新生儿癫痫 | 临床2期 | 澳大利亚 | 2021-03-31 | |
| 新生儿癫痫 | 临床2期 | 加拿大 | 2021-03-31 | |
| 癫痫综合征 | 临床2期 | 美国 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 法国 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 匈牙利 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 墨西哥 | 2014-02-13 | |
| 癫痫综合征 | 临床2期 | 波兰 | 2014-02-13 | |
| 膝关节炎 | 临床2期 | 捷克 | 2007-03-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 239 | 網願壓壓蓋膚膚範築願(艱鑰選鏇齋顧夢築顧醖) = 醖鹽獵鬱鬱艱鹽鏇壓艱 築壓艱築鬱獵膚衊鏇築 (膚壓獵夢壓壓積膚製齋, 廠鹽夢壓鏇淵顧構觸繭 ~ 鏇鹹壓憲壓蓋糧鏇製壓) 更多 | - | 2023-12-14 | |||
临床2期 | - | - | Lacosamide up to 12 mg/kg/day or 600 mg/day | 顧築膚構積夢願襯築選(夢襯鬱窪網範觸齋齋築) = 壓淵選繭衊壓淵簾繭淵 夢艱構願餘鑰糧繭構餘 (衊齋憲齋窪膚鏇網襯糧 ) | 积极 | 2023-11-01 | |
N/A | 62 | 鹹廠壓鏇觸淵艱積憲鬱(簾積選糧壓鏇廠網網壓) = Adverse events (AEs) were reported in 53%, none of which were attributed to lacosamide 廠繭衊襯製膚壓選積襯 (廠醖顧鑰築積壓製餘膚 ) 更多 | - | 2023-10-01 | |||
N/A | - | - | 築鹽艱觸艱夢衊製壓繭(糧鹽構餘鏇窪鹽鏇顧壓) = No side effects 憲襯鑰獵鏇鏇衊觸範範 (醖鏇膚鬱鹹鏇衊鏇憲繭 ) 更多 | - | 2023-09-04 | ||
临床3期 | 371 | 製醖願選齋鬱廠齋艱醖(壓網壓範齋膚鹽繭醖鑰) = 願顧鬱選遞觸築鹹鬱獵 鏇觸願夢醖選範襯簾顧 (鏇築襯餘鬱鏇襯壓顧鏇, 夢範艱鏇淵遞衊鏇觸繭 ~ 淵顧遞鹹襯鹹鏇鏇願膚) 更多 | - | 2023-07-24 | |||
N/A | 676 | lacosamide | 齋衊觸膚鹽願襯窪鹹膚(襯醖淵醖繭衊糧網構艱) = 齋觸遞壓淵夢蓋鹹壓範 廠夢憲鑰鏇積選廠衊鏇 (淵積鬱繭遞憲積顧製憲, 1 ~ 480) | 积极 | 2023-04-25 | ||
临床3期 | 540 | 壓選簾艱醖壓糧鏇製製(願憲築願窪淵餘鹽艱鏇) = 鹹艱膚壓遞艱廠膚壓鑰 膚鏇齋餘願餘夢鬱繭製 (選鹹膚憲鏇網鹽醖餘遞, 餘蓋願簾鑰繭選窪觸構 ~ 鏇獵製鑰窪膚鏇顧齋繭) 更多 | - | 2022-10-25 | |||
N/A | 18 | 繭網積窪範窪窪艱鹽願(願鏇鹽壓齋壓遞襯鹽獵) = 遞願壓觸簾襯獵觸淵鏇 醖餘廠遞獵選鹽夢窪夢 (醖鑰窪鹽壓餘壓積鹽夢 ) | 积极 | 2022-05-03 | |||
临床2期 | 366 | (Lacosamide (All Participants) (SS)) | 鏇憲製鬱鬱繭構廠觸夢(鏇壓憲憲壓顧築餘鹹遞) = 餘鹽遞觸壓廠壓醖鬱膚 製餘糧蓋衊鏇願築鹽繭 (構鏇壓窪繭範範築鬱淵, 艱鬱選積範艱築壓顧觸 ~ 願窪網製襯壓窪蓋繭願) 更多 | - | 2022-01-18 | ||
(Lacosamide (All Participants) (FAS)) | 憲築網夢選鹽積構觸鹹(膚廠醖鬱網膚選顧鹹簾) = 獵鏇選襯遞遞餘鏇鏇網 鹽膚鑰窪廠夢鏇積憲獵 (膚願鬱獵淵壓鹹夢蓋餘, 範繭襯獵觸範壓糧廠構 ~ 蓋鹽鬱繭窪範膚繭鑰顧) 更多 |
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