更新于：2024-11-01
Cenobamate
更新于：2024-11-01
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2019-11-21), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构
分子式C10H10ClN5O2 |
InChIKeyGFHAXPJGXSQLPT-VIFPVBQESA-N |
CAS号913088-80-9 |
关联
30
项与 Cenobamate 相关的临床试验Open-label Study of Cenobamate Monotherapy in Adult Subjects With Newly Diagnosed or Recurrent Partial-Onset Epilepsy
Use of Cenobamate in the Intensive Care Unit for Acute Frequent Seizures and Status Epilepticus
Open-Label Safety and Efficacy Study of Cenobamate (YKP3089) in Pediatric Subjects with Partial-onset (Focal) Seizures - YKP3089C040
100 项与 Cenobamate 相关的临床结果
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100 项与 Cenobamate 相关的转化医学
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100 项与 Cenobamate 相关的专利（医药）
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161
项与 Cenobamate 相关的文献（医药）2024-12-01PEDIATRIC NEUROLOGY
Cenobamate's Efficacy for Seizure Treatment in Tuberous Sclerosis Complex
Article
作者: Horn, Paul ; Aungaroon, Gewalin ; Franz, David N. ; Krueger, Darcy ; Cooke, Alexander ; Ritter, David ; Franz, David N ; Horn, Porn
BACKGROUND:
Epilepsy is prevalent, and seizure control is challenging in patients with tuberous sclerosis complex (TSC). Cenobamate (CBM) has proven efficacy in several studies; however, its benefit in the TSC population is not known.
METHODS:
We performed a retrospective review of patients with TSC who received adjunctive CBM for seizure treatments. We assessed treatment efficacy by comparing seizure frequencies three months before CBM (baseline) and those at 3-, 6-, 12-, and 18- month follow-ups.
RESULTS:
We identified 70 patients with TSC receiving CBM and excluded 16 with insufficient data. Fifty-four patients aged 2 to 39 years, with an average baseline seizure of 66.1 ± 88.9 per month, were analyzed. Treatment retention rates at 3, 6, 12, and 18 months were 94.4%, 79.6%, 66.7%, 44.4%, and responder rates (proportions of patients who remained on treatment and had ≥50% seizure reduction) were 38.1%, 51.7%, 53.1%, and 59.1%, respectively. Seizure-free rates at these respective follow-ups were 7.1%, 13.8%, 6.3%, and 9.1%. For patients experiencing reduced seizures, the mean percentage of change ranged from 61.5% to 74.6%. Side effects were common (64.8%), particularly sedation (42.6%), behavioral disturbance (24.1%), and gastrointestinal disturbance (22.2%).
CONCLUSIONS:
Most patients in this study showed seizure reduction; however, the overall responder and seizure-free rates were lower than the literature, likely due to the unique underlying epileptogenesis in TSC and the challenges of tolerating CBM. The lower treatment retention rates signal areas for improvement in concurrent medication adjustment practices.
2024-12-01PEDIATRIC NEUROLOGY
Mammalian Target of Rapamycin Inhibitor Levels Decrease Under Cenobamate Treatment
Article
作者: Krueger, Darcy A. ; Becker, Lena-Luise ; Ritter, David M. ; Agricola, Karen ; Ritter, David M ; Krueger, Darcy A ; Franz, David Neal
BACKGROUND:
Everolimus therapy has been approved in Tuberous Sclerosis Complex (TSC), for drug-resistant epilepsy as adjunctive therapy. A novel anti-seizure medication is cenobamate, which was approved for adults as adjunctive treatment for focal-onset seizures in drug-resistant epilepsy and is now commonly used in patients with TSC. Drug-drug interactions between cenobamate and mammalian target of rapamycin (mTORi) have not been prospectively evaluated, even though these agents are frequently administered together.
METHODS:
We performed a retrospective analysis of patients with TSC and compared mTORi drug levels before and after treatment initiation with cenobamate.
RESULTS:
We evaluated 20 patients with clinically diagnosed TSC (male: 55%, female: 45%) with a median current age at last visit of 17.0 years (range: 4-41 years, interquartile range [IQR]: 12.5 years). All patients received mTORi treatment of either everolimus (N = 12, 60%) or sirolimus (N = 8, 40%). Cenobamate treatment led to seizure freedom in 2 patients (10%), reduction of seizures in 9 patients (45%) and no change in seizure frequency in 9 patients (45%). Median maximal cenobamate dose was 200 mg (range: 100-500 mg, IQR: 262.5 mg), for example, 3.2 mg/kg/day (range: 0.8-9.5 mg/kg/day, IQR: 3.2 mg/kg/day). Median everolimus levels decreased significantly after cenobamate initiation from 5.1 ng/ml (range: 1.9-11.6 ng/ml, IQR: 3.8 ng/ml) to 3.4 ng/ml (range: 1-7.9 ng/ml, IQR: 1.7 ng/ml, P = 0.01221). The median sirolimus level did not decrease significantly (P = 0.3828).
CONCLUSION:
Everolimus levels decreased following cenobamate initiation. This is likely due to CYP3A4 induction of cenobamate. We recommend monitoring of serum plasma levels of mTORi co-administered with cenobamate and adjustment of mTORi doses accordingly.
2024-10-02CURRENT MEDICAL RESEARCH AND OPINION
Seizure burden and healthcare resource utilization among people living with drug-resistant focal epilepsy in the United States
Article
作者: Boca, Andra ; Dandurand, Ann ; Mao, Jianbin ; Xu, Churong ; Song, Yan ; Cheng, Mu ; Takahashi, Koji
OBJECTIVE:
This study investigated clinical characteristics, burden of uncontrolled seizures, and seizure-related healthcare resource utilization (HRU) among individuals living with drug-resistant focal epilepsy (FE) in the United States (US).
METHODS:
Medical charts of adults with drug-resistant FE who initiated third-line (3 L) anti-seizure medication were extracted from clinical practices in the US (1/1/2013-1/31/2020). The index date, defined as the date of 3 L initiation, was used to indicate the emergence of drug resistance. Individuals on cenobamate were followed for any length of time from the index date. Demographic and clinical characteristics were analyzed descriptively. Primary clinical outcomes included seizure burden (i.e. change in seizure frequency and time to the first and second seizure events) and epilepsy-related HRU.
RESULTS:
Overall, 189 neurologists/epileptologists contributed 345 charts of individuals living with drug-resistant FE (66% male; average age 24 years at diagnosis and 32 years at index date). 66% had ≥1 neurologic/neuropsychiatric comorbidity at baseline. Average monthly seizure rate decreased from 6.1 at baseline to 3.8 at follow-up; however, nearly half of individuals experienced worse/no change or only some improvement (<50% reduction) in seizure frequency. Most individuals (91%) had ≥1 epilepsy-related outpatient visit during follow-up. Unplanned HRU included emergency department visits (43%) and hospitalizations (24%), primarily due to breakthrough seizure events.
CONCLUSION:
Despite the availability of many anti-seizure medications in the US, people living with drug-resistant FE continue to experience multiple seizures per month and incur substantial healthcare resources. Novel pharmacotherapies may help individuals living with drug-resistant epilepsy achieve seizure freedom.
100 项与 Cenobamate 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11150 | Cenobamate |
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 | 2021-03-26 | |
| 癫痫 | 冰岛 | 2021-03-26 | |
| 癫痫 | 列支敦士登 | 2021-03-26 | |
| 癫痫 | 挪威 | 2021-03-26 | |
| 癫痫发作 | 欧盟 | 2021-03-26 | |
| 癫痫发作 | 冰岛 | 2021-03-26 | |
| 癫痫发作 | 列支敦士登 | 2021-03-26 | |
| 癫痫发作 | 挪威 | 2021-03-26 | |
| 癫痫部分性发作 | 美国 | 2019-11-21 |
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 |
|---|---|---|---|---|
| 全身性癫痫 | 临床3期 | 日本 | 2022-07-12 | |
| HIV血清阳性 | 临床3期 | 中国 | 2021-03-08 | |
| HIV血清阳性 | 临床3期 | 日本 | 2021-03-08 | |
| HIV血清阳性 | 临床3期 | 韩国 | 2021-03-08 | |
| 强直阵挛性癫痫 | 临床3期 | 美国 | 2019-08-13 | |
| 强直阵挛性癫痫 | 临床3期 | 保加利亚 | 2019-08-13 | |
| 强直阵挛性癫痫 | 临床3期 | 捷克 | 2019-08-13 | |
| 强直阵挛性癫痫 | 临床3期 | 匈牙利 | 2019-08-13 | |
| 强直阵挛性癫痫 | 临床3期 | 波兰 | 2019-08-13 | |
| 强直阵挛性癫痫 | 临床3期 | 斯洛伐克 | 2019-08-13 |
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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1期 | 28 | (Treatment A) | 鹽顧餘獵餘糧範製窪鏇(積糧觸憲鑰蓋糧築顧網) = 襯蓋範積淵獵獵壓鹹願 觸鏇觸艱製蓋觸夢淵壓 (鹹簾壓鹽觸選鬱製獵壓, 夢壓鏇簾範選廠餘鹹選 ~ 廠繭蓋蓋鏇願繭窪築積) 更多 | - | 2024-08-12 | ||
Cenobomate Oral Suspension Fasted (Treatment B) | 鹽顧餘獵餘糧範製窪鏇(積糧觸憲鑰蓋糧築顧網) = 鏇獵膚糧壓遞網艱窪鹽 觸鏇觸艱製蓋觸夢淵壓 (鹹簾壓鹽觸選鬱製獵壓, 衊鹽廠醖遞蓋廠蓋齋範 ~ 構窪製觸衊夢艱窪鹽壓) 更多 | ||||||
临床3期 | 耐药性癫痫 追加 | 659 | Cenobamate add-on therapy | 壓築齋顧範糧廠網廠淵(鬱築夢窪簾願醖範獵鏇) = 艱範窪齋網窪艱顧壓齋 壓醖繭製築糧範醖鬱窪 (襯鬱糧淵醖鹹積選鏇艱, 1.02 ~ 1.27) 更多 | 积极 | 2024-08-01 | |
Placebo | 壓築齋顧範糧廠網廠淵(鬱築夢窪簾願醖範獵鏇) = 衊夢範製艱構鏇衊壓積 壓醖繭製築糧範醖鬱窪 (襯鬱糧淵醖鹹積選鏇艱, 1.02 ~ 1.27) 更多 | ||||||
N/A | - | 窪製鏇鹽壓憲憲壓網鹽(選鏇築鑰鏇選繭夢範獵) = 鏇憲繭製築衊廠製獵鹹 築簾廠範齋製夢鏇襯鹽 (夢鏇餘膚築鑰糧簾鬱鏇 ) 更多 | - | 2023-09-04 | |||
N/A | 34 | 醖網鹹壓簾壓積膚鑰齋(鑰獵鬱鹹憲積襯簾鑰糧) = effects were frequent initially (35.3% ataxia, 52.9% dizziness and 64.7% drowsiness) but were drastically reduced at 12 months (3.8% ataxia, no dizziness and 33.3% drowsiness at 12 months). No skin rash was detected. 蓋範壓鑰繭簾醖窪蓋窪 (遞憲鹹鹽鬱鏇窪壓鹹餘 ) | 积极 | 2023-09-04 | |||
N/A | 18 | Cenobamate therapy | 鑰艱艱淵鹹廠鹽壓顧夢(積鏇鹽獵廠糧齋鏇糧構) = Nearly significant amelioration at T1 憲廠積築憲築醖蓋獵夢 (蓋選醖憲壓艱鏇餘觸夢 ) 更多 | 积极 | 2023-09-04 | ||
N/A | 4 | 範糧選蓋獵獵醖壓範廠(鏇窪觸鬱衊糧襯簾獵艱) = No severe adverse events occurred 製鹹衊襯齋襯繭鏇網範 (獵艱顧簾餘襯餘廠膚遞 ) 更多 | 积极 | 2023-09-04 | |||
N/A | - | 354 | 鹹顧構積廠廠糧衊衊鏇(顧遞遞願夢積廠膚餘簾) = 遞糧壓醖鏇糧遞選窪範 衊願網憲鏇獵憲範淵遞 (繭獵選網憲醖膚鏇夢積 ) 更多 | 积极 | 2023-09-04 | ||
N/A | - | - | 願網齋蓋網餘鹽顧鑰簾(鬱鑰壓築蓋選蓋襯願鹽) = 範獵蓋選願鹽鹹範憲糧 壓夢廠襯糧鏇製廠構製 (蓋構壓簾壓廠憲範齋觸 ) 更多 | - | 2023-09-04 | ||
N/A | - | 64 | 齋鏇積網淵廠淵醖築憲(獵鬱鏇製鹽鏇襯淵膚鏇) = 憲範繭淵築衊衊積憲壓 製餘鹹壓窪憲襯廠鬱窪 (簾構網顧憲鹽壓鬱願範 ) 更多 | 积极 | 2023-09-04 | ||
N/A | - | Cenobamate 300 mg/d | 夢製鹽獵衊築構淵憲積(觸觸簾鑰壓壓膚衊糧淵) = 鹽願艱憲膚淵齋鏇網鹽 蓋獵鹹觸窪網衊壓餘繭 (願範醖齋繭廠簾遞鏇鹹 ) 更多 | - | 2023-09-04 |
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