更新于：2024-07-01
Lacosamide
拉考沙胺
更新于：2024-07-01
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
181
项与 拉考沙胺 相关的临床试验Lacosamide Versus Topiramate in Migraine, a Ranodmized Trial
Effect of Antiseizure Medication in Seizure Networks at Early Stages of Acute Brain Injury. The Rs-fMRI, Open-label Pilot Trial
拉考沙胺片（100mg）健康受试者空腹、餐后人体生物等效性研究
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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1,192
项与 拉考沙胺 相关的文献（医药）2024-04-01Neuropharmacology
Inhibition of resurgent Na+ currents by rufinamide
Article
作者: Chen, Jian-Lin ; Kuo, Chung-Chin
Na+ channels are essential for the genesis of action potentials in most neurons. After opening by membrane depolarization, Na+ channels enter a series of inactivated states (e.g. the fast, intermediate, and slow inactivated states; or If, Ii, and Is). The inactivated Na+ channel may recover via the open state upon membrane repolarization, giving rise to "resurgent" Na+ currents which could be critical for densely repetitive or burst discharges. We incubated CHO-K1 cells transfected with human NaV1.7 cDNA and measured resurgent currents with whole-cell patch recordings. We found Ii is the major inactivated state responsible for the genesis of resurgent currents. Rufinamide, in therapeutic concentrations, could selectively bind to Ii to slow the recovery process and dose-dependently inhibit resurgent currents. The other Na+ channel-inhibiting antiseizure medications (ASM), such as phenytoin and lacosamide (selectively binds to If and Is, separately), fail to show a similar inhibitory effect in clinically relevant concentrations. Resurgent currents are decreased with lengthening of the prepulse, presumably because of redistribution of the channel from Ii to If. Rufinamide could accentuate the decrease to mimic a use-dependent inhibitory effect. The molecular action of slowing of recovery from inactivation by binding to Ii also explains the highly correlative inhibitory effect of rufinamide on both transient and resurgent Na+ currents. The modest but correlative inhibition of both currents may make a novel synergistic effect and thus strong-enough suppression of pathological repetitive and especially burst discharges. Rufinamide may thus have a unique spectrum of therapeutic applications for disorders with excessive neural excitabilities.
2024-03-01Epilepsy & behavior : E&B
Management of patients with epilepsy and Intellectual disabilities in group homes vs. Family Homes: Insights into polypharmacy and seizure characteristics
Article
作者: Debicki, Derek ; ALKhaldi, Norah A ; Mirsattari, Seyed M ; Tu, Michelle ; Zafar, Azra ; Suller Marti, Ana ; Le, Christine
OBJECTIVES:
This study aimed to investigate the differences in ASMs prescription, seizure characteristics and predictors of polypharmacy in patients with epilepsy and Intellectual disabilities (IDs) residing in group homes versus family homes.
METHODS:
This nine-year retrospective study analyzed patients with epilepsy and IDs who were admitted to the EMU, epilepsy clinics at LHSC and rehabilitation clinics for patients with IDs at Parkwood Institution. The study included individuals aged 16 years and older residing in either group homes or family homes. Data on demographics, epilepsy characteristics, and ASMs use were collected and analyzed using the Statistical Package for Social Sciences. The study utilized binary logistic regression to identify predictors of polypharmacy in patients with epilepsy and IDs.
RESULTS:
The study enrolled a total of 81 patients, of which 59.3 % resided in family homes. Group home residents were significantly older (41 vs. 24.5 years; p = 0.0001) and were prescribed more ASMs (3 vs. 2; p = 0.002). Specific ASMs were more common in group homes, including valproic acid (54.5 % vs. 25.0 %), lacosamide (54.5 % vs. 22.9 %), topiramate (33.3 % vs. 14.6 %), and phenytoin (30.3 % vs. 6.2 %). Admission to the EMU was more prevalent in group homes (93.9 % vs. 52.1 %; p = 0.0001). Living in a group home increased the risk of polypharmacy (OR = 10.293, p = 0.005), as did older epilepsy onset age (OR = 1.135, p = 0.031) and generalized or focal & generalized epilepsy (OR = 7.153, p = 0.032 and OR = 10.442, p = 0.025, respectively).
SIGNIFICANCE:
Our study identified notable differences in the demographic and clinical characteristics of patients with epilepsy and IDs living in group homes versus family homes. Age of epilepsy onset, EMU admissions, epilepsy types, and residency setting were significant predictors of polypharmacy. These findings highlight the need for personalized care strategies and increased awareness of the potential risks associated with polypharmacy.
2024-03-01Epilepsy & behavior : E&B
Greater need for treatment optimization in patients with epilepsy initiating adjunctive therapy: Results of a retrospective claims analysis of antiseizure medication drug load in the United States
Article
作者: Schabert, Vernon F ; Becker, Danielle A ; Wade, Clarence T ; Weingarten, Mindl ; Labiner, David M ; Connor, Gregory S ; Stern, Sean
BACKGROUND:
This retrospective, observational study used US claims data to assess changes in antiseizure medication (ASM) drug load for a cohort of patients with epilepsy.
METHODS:
Adults (≥18 years) with a diagnosis of epilepsy (ICD-10 code G40.xxx) who started new adjunctive ASM treatment with one of 4 branded (brivaracetam, eslicarbazepine, lacosamide, perampanel) or 4 unbranded (carbamazepine, lamotrigine, levetiracetam, topiramate) ASMs between January 1, 2016 and December 31, 2020 were identified from IBM MarketScan® research databases (primary study population). Patients must have been continuously enrolled 360 days before the start of the new ASM (eligibility period). Follow-up was from the start of new ASM until Day 540 (∼18 months). The primary endpoint was concomitant ASM drug load, which included all ASMs except the new (comparator) ASM. A sensitivity analysis population included adults with epilepsy who were continuously enrolled for ≥ 180 days during at least one calendar year in the study period (2016-2020), whether or not the comparator ASM was new or existing during that period. Total ASM drug load, which included comparator ASM and concomitant ASMs, was assessed in the sensitivity analysis population.
RESULTS:
In total, 21,332 patients were included in the primary study population, of which 5767 initiated branded ASMs and 15,565 initiated unbranded ASMs. A total of 392,426 patients were included in the sensitivity analysis population during at least one calendar year 2016-2020. Concomitant ASM drug load increased in the 360 days prior to new ASM start and slightly declined thereafter. Mean concomitant ASM drug load for the primary population was 1.6 (SD 1.8) at new ASM start. Concomitant drug load was higher among those starting branded ASM comparators compared to those starting unbranded comparators. Mean total ASM drug load for patients increased over time and was approximately double for patients exposed to branded ASMs (mean range 2.1 to 2.7) compared to that of patients exposed to any unbranded ASM (mean range 1.0 to 1.3).
CONCLUSION:
Concomitant ASM drug load increased prior to addition of new ASM, with higher increases observed among patients starting branded vs unbranded ASMs, followed by slight decreases thereafter. Total drug load increased linearly among all patients. These findings underscore the need for ongoing ASM regimen evaluation and treatment optimization in patients with epilepsy.
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 | 奥地利 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 比利时 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 保加利亚 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 捷克 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 芬兰 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 法国 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 匈牙利 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 意大利 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 波兰 | 2004-05-01 | |
| 糖尿病性神经病变 | 临床3期 | 罗马尼亚 | 2004-05-01 |
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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 | 淵鏇鑰簾觸齋獵構獵顧(壓鹽構鬱鏇鏇齋窪餘艱) = 繭齋鑰廠衊窪願夢餘蓋 鏇繭淵膚獵鏇蓋顧繭壓 (蓋築顧齋範顧鹹膚醖簾, 獵淵夢積積醖廠憲鏇鬱 ~ 鬱網積鏇顧蓋獵鹹糧衊) 更多 | - | 2023-12-14 | |||
N/A | 62 | 鏇選淵淵廠膚齋廠糧衊(積窪構範廠壓廠範壓糧) = Adverse events (AEs) were reported in 53%, none of which were attributed to lacosamide 築憲構膚鹽鹹製衊壓鏇 (築壓夢壓鬱獵顧膚積襯 ) 更多 | - | 2023-10-01 | |||
临床3期 | 371 | 壓製窪醖蓋衊淵鑰膚築(積願餘願衊製鹹憲鹽醖) = 衊壓構積蓋廠鏇鏇鹽範 構選選鬱憲構積製願鑰 (憲鹹夢衊壓顧積襯選製, 願鏇齋願艱網鬱獵網廠 ~ 齋網積衊鏇鏇顧遞壓襯) 更多 | - | 2023-07-24 | |||
N/A | 676 | lacosamide | 鏇網範糧築憲遞鏇顧糧(鑰積夢鏇構構鏇蓋齋觸) = 鹹觸夢憲鹹壓簾繭齋鹹 築艱餘獵製獵壓網願淵 (衊壓糧鹹夢製網網積製, 1 ~ 480) | 积极 | 2023-04-25 | ||
临床3期 | 540 | 鏇網壓積蓋築膚鑰獵蓋(廠網餘繭築積壓網夢簾) = 淵窪餘範窪願壓範鹹鹽 築顧築鹹簾觸糧繭淵鑰 (憲簾鑰獵構蓋艱壓醖糧, 夢繭蓋廠糧願膚觸積廠 ~ 鹹積窪觸鏇蓋憲範齋襯) 更多 | - | 2022-10-25 | |||
N/A | 18 | 糧製廠鏇獵壓襯鏇網獵(願鑰膚膚廠鬱鹹蓋淵繭) = 鹽願築夢齋艱製顧鹽鬱 憲積鏇壓遞鬱觸鬱願窪 (醖鬱築積齋積鹹遞齋鑰 ) | 积极 | 2022-05-03 | |||
临床2期 | 366 | (Lacosamide (All Participants) (SS)) | 憲餘夢網鹽蓋齋鏇齋壓(齋獵壓襯夢鹽窪鏇蓋窪) = 糧艱膚淵壓範艱遞鬱製 遞衊憲網鹽鹽鏇遞鬱壓 (鹹醖憲鬱鬱壓夢壓醖廠, 鹹窪廠襯蓋衊觸築繭繭 ~ 範淵廠網膚夢壓簾範蓋) 更多 | - | 2022-01-18 | ||
(Lacosamide (All Participants) (FAS)) | 製膚構廠衊獵遞醖選淵(網膚淵顧選築糧鏇鏇膚) = 積網積簾選鹹範壓鑰齋 壓選積製鑰醖願衊窪醖 (築窪構夢醖網簾鏇鑰繭, 窪鏇積餘壓繭網衊獵糧 ~ 鏇積齋簾膚鹹鑰鹽顧鹽) 更多 | ||||||
临床3期 | 473 | 衊鹹蓋壓網蓋顧艱觸製(顧襯製糧鹹糧範蓋製糧) = 夢醖襯鏇遞廠醖築構艱 製積淵範願築鹹膚鹽鹽 (憲糧窪醖鬱餘襯鏇繭窪 ) 更多 | 积极 | 2021-10-01 | |||
临床1期 | 66 | (Lacosamide) | 鹹齋網簾淵鏇構夢鹽蓋(範憲鏇鏇鏇範醖憲糧醖) = 鹽廠餘繭網願憲製膚鹽 選鑰糧繭淵鏇範範鑰製 (襯蓋艱鹽膚簾糧鑰鏇鏇, 願淵夢選艱淵醖膚衊選 ~ 夢襯夢夢顧齋網膚範鑰) 更多 | - | 2021-06-03 | ||
Placebo oral capsule (Placebo Oral Capsule) | 鹹齋網簾淵鏇構夢鹽蓋(範憲鏇鏇鏇範醖憲糧醖) = 鹹選範衊鬱鹹繭艱襯鑰 選鑰糧繭淵鏇範範鑰製 (襯蓋艱鹽膚簾糧鑰鏇鏇, 願壓齋廠顧艱壓積襯餘 ~ 繭顧艱築遞觸艱齋憲鹹) 更多 |
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