主要研究目的考察中国健康参与者空腹条件下单次口服西诺氨酯片受试制剂(规格：12.5mg，生产企业：江西科睿药业有限公司)及参比制剂(商品名：Xcopri®，规格：12.5mg，持证商：SK Life Science)后的药代动力学特征，评价两制剂在空腹条件下是否具有生物等效性。次要研究目的评价西诺氨酯片受试制剂(规格：12.5mg)及参比制剂(商品名：Xcopri ®，规格：12.5mg)在健康参与者中的安全性。

开始日期2026-03-11

申办/合作机构

江西科睿药业有限公司

CTR20254308

/ RecruitingN/A

西诺氨酯片人体生物等效性试验

主要研究目的：以江苏恩华药业股份有限公司研制生产的西诺氨酯片（规格：12.5 mg）为受试制剂，以持证商是SK Life Science, Inc.的西诺氨酯片（商品名：Xcopri®，规格：12.5 mg）为参比制剂，研究两制剂在中国健康成年试验参与者空腹和餐后状态下的药代动力学特征，并评价两制剂的人体生物等效性。次要研究目的：评估健康试验参与者单次空腹/餐后口服西诺氨酯片受试制剂和参比制剂后的安全性。

开始日期2025-11-26

申办/合作机构

江苏恩华药业股份有限公司

CTR20253859

/ CompletedN/A

苯巴那酯片在餐后条件下的人体生物等效性试验

考察健康受试者在餐后条件下，单次口服由杭州和康药业有限公司提供的苯巴那酯片（受试制剂T，规格：12.5mg）与单次口服由Angelini Pharma S.p.A持证的苯巴那酯片（参比制剂R，商品名：ONTOZRY®，规格：12.5mg）的药动学特征，评价两制剂的生物等效性及安全性，为该受试制剂注册申请提供依据。

开始日期2025-10-21

申办/合作机构

杭州和康药业有限公司

100 项与西诺氨酯相关的临床结果

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100 项与西诺氨酯相关的转化医学

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100 项与西诺氨酯相关的专利（医药）

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277

项与西诺氨酯相关的文献（医药）

2026-04-01·Neurology and Therapy

Long-Term Impact of Cenobamate on Cognition, Adaptive Behavior, and Quality of Life in Patients with Tuberous Sclerosis Complex

Article

作者: Gambardella, Antonio ; Moavero, Romina ; Izzo, Viviana ; Pastorino, Grazia Maria Giovanna ; Martino, Iolanda ; Operto, Francesca Felicia ; Charlier, Bruno ; Olivieri, Miriam ; Sammara, Ilaria ; Mungo, Noemi

INTRODUCTION:

Cenobamate is a recent therapeutic option for epilepsy, but few studies have investigated its impact on cognitive and emotional/behavioral functioning. The aim of our study was to assess cognitive function, adaptive behavior, quality of life, and parental stress in late adolescents and young adults with tuberous sclerosis complex (TSC) and drug-resistant epilepsy, treated with add-on cenobamate over a 12-month period using standardized neuropsychological tests.

METHODS:

Our prospective observational study included 22 patients, aged 18 to 24 years with a diagnosis of TSC and drug-resistant epilepsy who started cenobamate add-on therapy for improving seizure control. At baseline and after 3- and 12-month follow-ups, participants completed a neuropsychological standardized assessment of executive functions (Epitrack©), adaptive behavior (VABS-II), quality of life (QOL), and parental stress (PSI). Cognitive functions (WAIS-IV) were reassessed only at the 12-month follow-up. Changes in standardized scores over time were analyzed using Friedman's two-way analysis of variance and post hoc analysis. Relationships between demographic/clinical variables and neuropsychological scores were analyzed using correlation analysis.

RESULTS:

Our study highlighted a statistically significant improvement in Epitrack, PSI-4-SF, and QOL scores after 3- or 12-month follow-ups (p < 0.05). Stability was maintained for the WAIS and VABS-II scores. The subjects with TSC2 mutations showed significantly lower IQ scores than those carrying TSC1 mutations (p < 0.001). Total parental stress (PSI) was significantly related to the total score of VABS-II at both baseline (p = 0.003) and 12 months (p = 0.001).

CONCLUSION:

Our study suggested that cenobamate add-on therapy was effective and generally well tolerated in this cohort. Neuropsychological assessments suggest beneficial effects on executive functions, emotional well-being, social functioning, and quality of life. Furthermore, an improvement in parental stress also emerged. These findings could support clinicians in the decision-making process, evaluating cenobamate as an early treatment option in drug-resistant epilepsy.

2026-03-01·JOURNAL OF CHILD NEUROLOGY

Adverse Effects of Cenobamate in Pediatric Epilepsy: Demographic Considerations

Article

作者: Iwamoto, Brooke K ; Chiang, Jenna A ; Whitaker, Ashley M ; Kahan, Madeline D ; Mendoza, Leanne ; Hirtum-Das, Michele M Van ; Joshi, Sucheta M ; Agurs, Latanya D ; Jordan, Brittany

This study explores trends and potential risk factors among pediatric patients with drug-resistant epilepsy who were prescribed cenobamate by their epileptologist. Twenty-four patients (54.2% female) with drug-resistant (62.5% focal) epilepsy were administered cenobamate (mean = 13.27 years, standard deviation [SD] = 4.91 years) after failing multiple antiseizure medications (mean = 4.83, SD = 2.94). Fifty percent reported improved seizure frequency, although more than half the sample experienced physiological (n = 12, 50%) and/or psychiatric (n = 4, 16.7%) adverse events, with 39% rapidly discontinuing cenobamate (mean = 4.00 months, SD = 3.21) because of intolerable physiological (n = 4, 57.1%) and/or psychiatric adverse events (n = 3, 42.9%). Of those experiencing a psychiatric adverse event, all but 1 (75%) discontinued cenobamate, as compared to discontinuation by only 40% of those experiencing a physiological adverse event (n = 10). Psychiatric adverse events were significantly associated with sex (100% female), χ 2 (1, N = 24) = 4.06, P = .04. Preliminary analyses also suggest older age (adolescence) may increase risk for psychiatric adverse events of cenobamate among patients with pediatric epilepsy.

2026-03-01·EPILEPSY RESEARCH

Healthcare resource utilization in adults with focal onset seizures before and after initiating cenobamate: A US database analysis

Article

作者: Cattaneo, Agnese ; Rosignoli, Maria Teresa ; Lipone, Paola ; Lovera, Alessandro ; Paltanwale, Queenie ; Eworuke, Efe ; Salvatori, Enrica ; Leach, John Paul ; Bosan, Rafia ; Benoist, Caroline Clare ; Comandini, Alessandro ; Chang, Hsiu-Ching ; Alvarez-Baron, Elena

BACKGROUND:

Antiseizure medications (ASMs) are the mainstay of treatment for patients with epilepsy, though over one third remain uncontrolled after treatment with at least two ASMs. Cenobamate is an ASM indicated for the treatment of adults with focal onset seizures (FOS) in the United States. In Europe cenobamate is approved for the adjunctive treatment of FOS in adult patients with epilepsy who have not been adequately controlled despite at least 2 previous ASMs. Real-world data helps to better describe the impact of cenobamate long-term effectiveness and tolerability/safety balance. Evidence reflecting a reduction of the impact of epilepsy on the daily lives of patients would be important when assessing and eventually predicting the benefit of treatments.

METHODS:

A retrospective observational study was conducted using the IQVIA PharMetrics Plus database among adult patients with both a claim for cenobamate between April 1, 2020, to April 30, 2023, and a diagnosis of FOS prior to the first cenobamate dispensing date (identified in the baseline period). Demographic characteristics were captured on the index date and clinical characteristics were captured in the 6 months baseline period; treatment patterns and healthcare resource utilization (HCRU) were assessed across 3 epochs forming 3 non-mutually exclusive cohorts: Cohort A, 6 months follow-up; Cohort B, 12 months follow-up; Cohort C, 18 months follow-up. Designated treatment regimen was defined by recorded ASMs prescribed in the 90 days following cenobamate dispensing (treatment regimen evaluation window), and patients were classified as 'monotherapy', 'stable polytherapy', or 'changing treatment regimen'.

RESULTS:

Among the 1132 patients included in Cohort A, approximately half (45.1 %) had stable polytherapy, 1.5 % had monotherapy, and 53.5 % had a changing treatment regimen following initiation of cenobamate. Similar distribution of designation was present among the 800 patients in Cohort B and 554 patients in Cohort C. A lower proportion of patients required hospitalization and emergency department visits in the 6 months after cenobamate initiation compared to the 6-month pre-index period (Cohort A: 15.4 % vs. 21.9 % and 24.9 % vs. 30.9 % respectively). Lower HCRU reduction rates (%) per patient per month were found at 6, 12 and 18 months of follow-up.

CONCLUSION:

Epilepsy-related hospitalizations and Emergency Room visits (indicators of seizures) were reduced in adult FOS patients with epilepsy 6, 12 and 18 months after initiating cenobamate as monotherapy or stable polytherapy, leading to reduced HCRUs and epilepsy costs.

157

项与西诺氨酯相关的新闻（医药）

2026-03-11

·CATO分析标准品

阿普昔腾坦（Aprocitentan）：靶向内皮素通路的难治性高血压新药，杂质研究面临哪些结构性挑战？

难治性高血压（resistant hypertension）约占全球高血压患者的10%～18%¹，在足量三联降压方案基础上血压仍不达标，心脑血管事件风险显著偏高。现有四联方案依赖螺内酯作为第四线选择，但其高钾血症和内分泌不良反应在肾病合并高血压人群中受限明显；而真正的机制空白在于：内皮素-1（ET-1）经ETA/ETB受体驱动的血管收缩、醛固酮合成与血管壁纤维化通路，尽管已被确认参与高血压病理生理逾三十年，却始终未被任何系统性降压药靶向干预。¹ 2024年3月19日，FDA批准阿普昔腾坦（商品名Tryvio，Idorsia制药），成为全球首个靶向内皮素通路的系统性降压药，也是近四十年来真正意义上的全新降压机制获批。此前选择性ETA拮抗剂达卢生坦在III期试验受挫，而阿普昔腾坦以双重ETA/ETB拮抗和更优安全性数据完成了对这一靶点的突破。一、分子结构解析中文名：阿普昔腾坦英文名：Aprocitentan（研发代号 ACT-132577）化学名：N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺分子式：C₁₆H₁₄Br₂N₆O₄S 分子量：546.19 g/mol CAS号：1103522-45-7 ³ 阿普昔腾坦是马西替坦（macitentan，已获批用于肺动脉高压）氧化脱丙基后的主要活性代谢产物，经结构优化后独立开发成新药实体，分子中不含手性中心。¹ 关键结构特征一：双溴取代芳环苯环对位（4-溴苯基）和嘧啶5位各含一个芳香C-Br键，溴原子通过疏水效应和电子效应强化受体结合亲和力（ETA IC₅₀ = 3.4 nM，ETB IC₅₀ = 987 nM）¹。两处芳香C-Br键在合成偶联反应和氧化降解条件下均存在脱卤风险，是工艺杂质的主要来源之一。关键结构特征二：磺酰胺官能团核心-SO₂NH-基团赋予分子与受体氨基酸残基形成关键氢键的能力。磺酰胺NH在极端pH或高温下存在水解风险；仲胺NH在特定制造环境中还具有N-亚硝化倾向，是ICH M7框架下的重点监管对象。⁴ 关键结构特征三：氧乙氧基连接臂 -O-CH₂CH₂-O-链段连接核心嘧啶环与5-溴嘧啶，其醚键在氧化降解条件下可产生N-氧化物类代谢相关杂质，对应已知代谢路径（M9）。² 二、作用机制与获批现状阿普昔腾坦通过同时阻断ETA和ETB两种内皮素受体，直接拮抗内皮素-1引起的强烈血管收缩，从而达到降低难治性高血压的效果。¹ 获批时间线：FDA 2024年3月19日（NDA 217686）²；EMA CHMP正面意见2024年4月（商品名Jeraygo）；中国NMPA截至目前尚无获批信息。三、阿普昔腾坦结构的风险维度 1.磺酰胺NH的N-亚硝化风险（监管优先级最高）磺酰胺仲胺NH在合成后处理阶段接触亚硝酸盐（NO₂⁻、NOₓ），或在成品制剂贮存中与辅料残留亚硝酸盐缓慢反应，均可生成N-亚硝基磺酰胺类化合物。监管层面，依据ICH M7（2023修订版）⁴，亚硝胺可接受摄入量（AI）通常在18～1500 ng/天范围，以NDMA的18 ng/天为参考下限；对应12.5 mg日服用量，杂质限度极为苛刻，常规HPLC-UV无法达到检测要求，需配套LC-MS/MS或GC-MS/MS高灵敏度专属方法。控制重点：工艺开发阶段须对所有含氮试剂进行亚硝胺形成风险评估，成品稳定性研究中应增加贮存期亚硝胺蓄积专项考察节点。 2. 双溴芳环脱卤杂质（合成工艺核心风险）苯环4位C-Br和嘧啶5位C-Br化学环境不同，在Pd催化偶联反应中可因不完全反应或去卤副反应，分别产生苯环脱溴类似物、嘧啶脱溴类似物及双去溴产物三类工艺杂质，须依据ICH Q3A⁵进行全面识别与限度制定。分析难点：单去溴类似物与原料药分子量仅差约79 Da，反相HPLC保留时间差异小，须通过梯度优化或质谱确认；MS鉴定时需利用Br同位素丰度比（含两溴分子[M]:[M+2]:[M+4] ≈ 1:2:1）精确识别脱溴产物。光照稳定性（ICH Q1B⁷，5000 lux·h）可诱发嘧啶脱溴，应作为必要应力条件纳入考察。 3.磺酰胺水解与N-氧化降解产物（安全性关联风险）磺酰胺在酸性（pH<3）或碱性（pH>10）及高温条件下可水解，主要生成代谢物M1（氨基嘧啶片段），该路径已在FDA NDA审评报告中经化学与酶促双途径证实²。嘧啶环氮在氧化条件下发生N-氧化，生成M9类似降解产物；两条路径在强制降解实验（ICH Q1A⁶应力条件）中均可在无酶促参与的情况下直接发生。分析挑战：M1为亲水性氨基嘧啶化合物，反相HPLC保留弱，方法开发需考虑离子对试剂或HILIC色谱柱；M9需高分辨质谱（精确质量误差<5 ppm）才能与同分异构体可靠区分。依据ICH Q3B⁸，制剂中含量超过0.05%或1 mg/天（取较低值）的降解产物须提供毒理学评估数据，M1目前安全性数据尚不完整，需特别关注。 CATO标准品解决方案 CATO（佳途科技）作为专注于药物杂质标准品的专业供应商，已针对阿普昔腾坦（Aprocitentan）的杂质质控研究布局了相关系列标准品目前已上架3款阿普昔腾坦（Aprocitentan）相关杂质标准品，与上述三个风险维度逐一对应：阿普昔腾坦杂质1（C4X-33551）分子式 C₈H₁₂N₂O₄，分子量 200.19。为氧乙氧基连接臂裂解后释放的嘧啶二醇片段，对应4.3节磺酰胺水解/链段断裂降解路径的定性定量参照。阿普昔腾坦杂质2（C4X-33552）分子式 C₁₆H₁₃Br₂N₅O₅S，分子量 547.18。结构显示磺酰胺氮位氧化（多一个氧原子），对应4.3节N-氧化降解路径（与M9形成机制相关），是氧化应力实验和制剂贮存期降解监控的关键对照品。阿普昔腾坦杂质3（C4X-33553）分子式 C₃₂H₂₂Br₄N₈O₅，分子量 918.18，含4个溴原子，为双分子偶联类工艺杂质，对应4.2节双溴芳环偶联副反应风险，是工艺杂质来源分析的专属参照标准品。全部产品均附有批次CoA（含¹H NMR结构确认图谱、MS特征碎片数据、HPLC纯度报告），并经CNAS及ANAB双重ISO 17034认可，量值可溯源至国际参考标准，支持NMPA和FDA注册申报的标准品使用场景。扫码添加CATO企业微信如需了解阿普昔腾坦杂质标准品规格或定制合成方案，欢迎联系CATO 📧 联系邮箱：info@cato-chem.com 🌐 官网：www.cato-chem.com 常见问题解答 Q1：阿普昔腾坦的杂质研究中，ICH M7亚硝胺筛查是必做项吗？是的。阿普昔腾坦含磺酰胺仲胺NH，属于ICH M7定义的潜在亚硝胺形成结构，FDA和EMA均要求进行系统性风险评估，不可跳过。即便评估结论为低风险，也须在申报资料中提供书面论证。若工艺涉及含氮试剂或亚硝酸盐暴露环节，需建立AI限度（≤18 ng/天，参照NDMA）内的定量检测方法，LC-MS/MS为标准配置。 Q2：仿制药研发早期，阿普昔腾坦杂质标准品如何选择供应商？选择标准品供应商时，监管可接受性是第一优先级。用于NMPA和FDA注册申报的标准品，须具备ISO 17034认可资质，量值溯源链完整，并附有¹H NMR、MS、HPLC全套结构确认数据，缺少任何一项均可能在技术审评环节被质疑。 CATO（佳途科技）持有CNAS及ANAB双重ISO 17034认可，目前已上架阿普昔腾坦杂质1、2、3三款现货标准品，覆盖N-氧化降解、水解降解及工艺偶联副产物三条主要杂质线，CoA文件可直接用于申报资料附件，省去定制合成的周期和沟通成本，对研发时间节点较紧的团队而言具有实际价值。 Q3：强制降解实验中，哪种应力条件最容易产生阿普昔腾坦的主要降解产物？根据FDA NDA审评报告及代谢数据，氧化应力（3% H₂O₂，室温）最敏感，主要产生N-氧化物类降解产物（对应M9路径）；酸性水解（0.1 M HCl，60°C）次之，主要生成氨基嘧啶片段M1。光照条件（ICH Q1B，5000 lux·h）可诱发嘧啶5位C-Br脱溴，需单独考察。碱性水解和热降解产物种类相对较少，但仍需纳入六应力完整研究框架。 Q4：阿普昔腾坦目前在中国尚未获批，国内仿制药企业现阶段做杂质研究是否过早？并不过早。核心化合物专利挑战窗口自2028年3月开放，仿制药最早入市约在2029年，但NMPA技术审评通常需要2～3年，意味着最迟2026年前后即须启动系统性杂质研究。杂质谱分析、强制降解方法建立、分析方法验证均属于耗时较长的前置工作，提前布局标准品体系是正常的研发节奏。 Q5：实验室临时需要某款阿普昔腾坦杂质标准品，但用量少、时间紧，有没有合适的采购渠道？这是药物分析实验室的常见痛点——需要的品种冷门、用量小、但等不起定制合成的周期。CATO（佳途科技）在这类场景下有一定优势：现货品种支持小规格起订，标准品附带全套检测图谱，可直接用于方法开发，不需要再做额外的结构确认实验。对于有NMPA或FDA申报需求的团队，其ISO 17034认可资质也省去了供应商资质审核的额外工作量。有采购需求可直接访问产品页查询库存与规格。参考文献 DrugBank DB15059. Aprocitentan. Accessed March 2026. https://go.drugbank.com/drugs/DB15059 Schlaich MP, et al. Dual endothelin antagonist aprocitentan for resistant hypertension (PRECISION). Lancet. 2022;400(10367):1876-1888. / FDA NDA 217686 Integrated Review, CDER, 2024. PubChem CID 25099191. Aprocitentan. Accessed March 2026. ICH M7(R2): Assessment and Control of DNA Reactive (Mutagenic) Impurities in Pharmaceuticals to Limit Potential Carcinogenic Risk. 2023. ICH Q3A(R2): Impurities in New Drug Substances. 2006. ICH Q1A(R2): Stability Testing of New Drug Substances and Products. 2003. ICH Q1B: Stability Testing: Photostability Testing of New Drug Substances and Products. 1996. ICH Q3B(R2): Impurities in New Drug Products. 2006. 往期 RECOMMEND 推荐伊曲莫德（Etrasimod）：新一代S1P受体调节剂的药学解析与杂质研究要点 2026全球化妆品新规密集生效！这些检测项目你准备好了吗? IgA肾病靶向新药阿曲生坦 (Atrasentan) 的机制解析与杂质控制策略 60亿癫痫蓝海市场爆发！西诺氨酯(Cenobamate)杂质分析难点突破

临床3期上市批准临床结果

2026-03-10

·allsci.com

Xenon targets US FDA filing for azetukalner after positive Phase III epilepsy data

Vancouver and Boston-based Xenon Pharmaceuticals announced positive topline results from the Phase III X-TOLE2 study of azetukalner, a KV7 potassium channel opener, in adults with focal onset seizures. The X-TOLE2 study results position azetukalner as the first drug in its mechanistic class to reach a potential US FDA filing since retigabine (from GSK/Valeant Pharma) was withdrawn from the market in 2017 due to safety concerns, and the data exceeded those from the earlier Phase IIb X-TOLE trial. X-TOLE2 was a randomized, double-blind, placebo-controlled, multicenter Phase III study evaluating azetukalner as adjunctive oral therapy, administered once daily with food, in adults with focal onset seizures. The trial randomized 380 participants across three arms — azetukalner 25 mg, azetukalner 15 mg, and placebo — with 374 entering the modified intent-to-treat population. Participants had treatment-resistant epilepsy, with a median of five prior antiseizure medications and a baseline seizure frequency of 12.75 per month; 51.3% were taking three concomitant antiseizure medications. The primary endpoint was median percent change in monthly focal onset seizure frequency from baseline to week 12. The 25 mg group achieved a -53.2% reduction (p=0.000000000006) and the 15 mg group achieved -34.5% (p=0.00007), compared with -10.4% for placebo. The placebo-adjusted reduction for the 25 mg dose was -42.7%, compared with -34.6% in the Phase IIb X-TOLE study. The key secondary endpoint, the proportion of participants with at least 50% seizure reduction, was 54.8% at 25 mg and 37.6% at 15 mg, versus 20.8% for placebo. The most common adverse events across azetukalner groups were dizziness (20.5%), headache (8.8%), somnolence (8.8%), and fatigue (7.6%). Discontinuation due to adverse events occurred in 14.5% of the 25 mg group, 4.8% at 15 mg, and 3.2% on placebo. Of 332 participants completing the double-blind period, 322 entered the open-label extension. Xenon anticipates submitting a New Drug Application to the US FDA in Q3 2026. If approved, it would be the only KV7 potassium channel opener available for epilepsy treatment. Azetukalner opens KV7.2/KV7.3 potassium channels in the central nervous system, enhancing the M-current that stabilizes neuronal resting membrane potential and reduces excessive firing — the core pathophysiology of seizure generation. This mechanism was clinically validated by retigabine (ezogabine), which received US FDA approval for focal seizures in 2011 but was voluntarily withdrawn after reports of skin and retinal discoloration linked to off-target activity at KV7.4/KV7.5 subtypes. Azetukalner was designed with selectivity for KV7.2/KV7.3 to avoid those liabilities. Epilepsy affects approximately three million adults in the US, and focal epilepsy is its most common form. Despite more than 30 approved antiseizure medications, up to half of patients with focal epilepsy continue to experience uncontrolled seizures. Most available therapies act through sodium channel blockade or GABAergic modulation, and few mechanistically distinct options have emerged in recent years. Key competitors and pipeline assets include: Cenobamate (SK Life Science), a dual sodium channel blocker and GABAA receptor modulator approved by the US FDA in 2019 for focal onset seizures in adults, currently in additional Phase III studies. PRAX-562 (Praxis Precision Medicines), a selective persistent sodium current blocker in Phase II development for focal onset seizures. Brivaracetam (UCB Pharma), an SV2A ligand approved by the US FDA in 2016 for focal onset seizures, with ongoing Phase III trials in pediatric populations. Your email address will not be published. Required fields are marked * Comment * Name * Email * Website

临床结果临床2期临床3期上市批准

2026-03-09

·FierceBiotech

Xenon phase 3 epilepsy readout \'blows away\' expectations, stock soars

Investors are glowing about the results, bestowing Xenon with a more than 40% stock boost. \n Xenon Pharmaceuticals’ anti-seizure candidate has smashed a pivotal trial out of the park, lowering seizure rates by more than 50% for some patients as it looks to position itself to become the standard of care in the field.In the phase 3 X-Tole2 study, Xenon’s KV7 potassium channel opener azetukalner significantly reduced focal onset seizure frequency at the 12-week mark by 53.2% when given at 25 milligrams daily and by 34.5% at 15 milligrams daily. The placebo group’s seizure rate, meanwhile, dropped by about 10%. Xenon revealed the results March 9 along with plans to submit the pill for FDA approval in the third quarter of this year.“Good things come to those who wait,” analysts from William Blair wrote in a March 9 note. The result “blows away” their expectations of an about 30% reduction in seizures, the analysts wrote, and, coupled with a solid tolerability profile, the pill’s ease of use and ability to be combined with other drugs, sets up azetukalner to become the epilepsy medicine of choice.The most common side effect of treatment was dizziness, which affected one-fifth of patients given azetukalner. Adverse events became worse at higher doses, with 14.5% of patients given 25 mg daily discontinuing treatment compared to 4.8% in the 15-mg group, according to Xenon’s release. The placebo group saw just 3.2% of patients discontinue due to side effects. “As expected, adverse events are dose-dependent, which actually makes the 15 mg dose very attractive commercially,” the analysts wrote, also noting that azetukalner led to fewer cases of fatigue, dizziness and sleepiness than other anti-seizure meds such as SK Biopharmaceuticals’ Xcopri.“We are very happy to announce these data for azetukalner, which exceeded expectations and, to our knowledge, show the highest placebo-adjusted efficacy ever observed in a pivotal epilepsy study,” Xenon CEO Ian Mortimer said in the release. Investors are glowing about the results, too, bestowing Xenon with a more than 40% stock boost. Xenon shares were trading at $59.80 at 10:00 a.m. ET on Monday after previously closing at $41.94.William Blair analysts had previously highlighted Xenon as one of their top five stock picks for 2026, citing the high potential of azetukalner. The small molecule is not alone in targeting KV7 ion channels; Biohaven’s opakalim uses the same mechanism and is currently in phase 3 trials for focal epilepsy and generalized epilepsy.Xenon is testing azetukalner in a phase 3 generalized epilepsy trial as well, and both biotechs are also considering their candidates for depression. On that front, though, neither ion channel activator looks too hot, with both flunking their phase 2 trials in the indication.By pursuing KV7 activators, Xenon and Biohaven are following in the footsteps of GSK and Valeant Therapeutics, who previously teamed up to make the first approved medicine in the class. That drug, ezogabine, was ultimately pulled from the market in 2017 due to the potential for vision loss. Xenon added ezogabine to its pipeline the following year, and its work with the molecule ultimately led to azetukalner.

$Xenon phase 3 epilepsy readout \'blows away\' expectations, stock soars$

临床3期临床结果临床2期

100 项与西诺氨酯相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11150	西诺氨酯	N03A	DB06119

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
癫痫	加拿大	ENDO VENTURES LTD	2023-06-12
癫痫发作	欧盟	Angelini Pharma, Inc.	2021-03-26
癫痫发作	冰岛	Angelini Pharma, Inc.	2021-03-26
癫痫发作	列支敦士登	Angelini Pharma, Inc.	2021-03-26
癫痫发作	挪威	Angelini Pharma, Inc.	2021-03-26
癫痫部分性发作	美国	SK Life Science, Inc.	2019-11-21

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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	Ono Pharmaceutical Co., Ltd.	2022-07-12
癫痫的复杂部分性发作	临床3期	中国	SK Life Science, Inc.	2021-03-08
癫痫的复杂部分性发作	临床3期	日本	SK Life Science, Inc.	2021-03-08
癫痫的复杂部分性发作	临床3期	韩国	SK Life Science, Inc.	2021-03-08
HIV血清阳性	临床3期	中国	SK Life Science, Inc.	2021-03-08
HIV血清阳性	临床3期	日本	SK Life Science, Inc.	2021-03-08
HIV血清阳性	临床3期	韩国	SK Life Science, Inc.	2021-03-08
继发性全身性癫痫发作	临床3期	中国	SK Life Science, Inc.	2021-03-08
继发性全身性癫痫发作	临床3期	日本	SK Life Science, Inc.	2021-03-08
继发性全身性癫痫发作	临床3期	韩国	SK Life Science, Inc.	2021-03-08

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04557085 (Pubmed \| Seizure)	临床3期	癫痫部分性发作	519	Cenobamate 200 mg/day	廠築願鑰網鬱襯遞餘簾(網獵艱鑰鏇淵獵積齋構) = The most common cenobamate-related treatment-emergent adverse events (≥20 %) were dizziness and somnolence. 淵鏇夢蓋鹹壓選夢餘鹹 (廠網選鬱醖願選願蓋廠 )	积极	2025-12-01
				Cenobamate 400 mg/day
NCT03678753 (NEWS) 人工标引	临床3期	癫痫发作	169	Cenobamate	簾製餘壓願顧繭選鏇獵(遞餘餘鏇願襯鏇齋積廠) = 蓋齋壓淵夢繭膚構構壓壓鏇網廠簾憲獵製蓋構 (繭齋衊遞遞廠鑰網鬱淵 ) 达到更多	积极	2025-09-16
				Placebo	簾製餘壓願顧繭選鏇獵(遞餘餘鏇願襯鏇齋積廠) = 鏇願襯餘衊廠積夢窪獵壓鏇網廠簾憲獵製蓋構 (繭齋衊遞遞廠鑰網鬱淵 ) 达到更多
NCT02535091 (Company_Website) 人工标引	临床3期	癫痫部分性发作	129	Cenobamate	鹽構觸淵鬱壓餘淵鏇簾(觸壓鬱衊範淵蓋鹹獵艱) = 獵壓鏇衊餘廠選網願網網襯製顧糧獵遞窪鏇築 (簾蓋糧製製襯選襯範鹹 ) 更多	积极	2025-09-01
P5-9.011 (AAN2025)	N/A	癫痫发作追加	-	Cenobamate	夢艱簾積窪夢網遞繭鏇(築願淵獵觸夢餘淵壓網) = Dizziness and lethargy were the most commonly reported adverse events during cenobamate treatment; these resolved with slower titration and/or reductions in concomitant ASMs 願構窪壓築簾鑰鑰餘醖 (鑰觸構餘簾製鑰簾遞鹹 ) 更多	积极	2025-04-07
NCT04557085 (YKP3089C035, AAN2025)	临床3期	癫痫发作	519	Placebo	觸衊願構簾顧鬱艱齋蓋(糧廠遞簾觸遞衊鹽網窪) = The most common treatment-emergent adverse events (≥20%) with cenobamate were dizziness 窪獵膚壓淵鏇築簾顧鹹 (襯繭範鹹淵簾齋餘餘遞 ) 更多	积极	2025-04-07
				Cenobamate 100 mg
NCT04557085 (P8-9.010, AAN2025)	临床3期	癫痫发作	519	Placebo	鏇衊糧築鏇製獵獵鏇壓(醖網膚膚觸夢構廠製顧) = The most common TEAEs (≥20%) were dizziness in the cenobamate dose groups 壓憲鬱艱構鬱網鹹簾觸 (蓋夢醖鬱鬱觸壓顧鬱膚 ) 更多	积极	2025-04-07
				Cenobamate 100 mg
P8-9.008 (AAN2025)	N/A	癫痫	59	Cenobamate	願網顧繭積齋獵觸獵範(壓鏇鏇簾齋淵鹹醖艱繭) = 12% 鹽選憲鹹壓夢蓋鬱範製 (獵餘襯憲壓鬱齋蓋壓構 ) 更多	积极	2025-04-07
NCT04557085 (P8-9.011, AAN2025)	临床3期	癫痫发作	519	Placebo	範衊簾鬱衊鹹遞鏇糧糧(繭積遞範構獵顧壓鬱艱) = 糧廠襯簾製蓋憲齋齋糧選鏇鹹醖餘憲觸衊遞鑰 (鹹範淵觸獵壓範壓鏇餘 )	积极	2025-04-07
				Cenobamate 100 mg	範衊簾鬱衊鹹遞鏇糧糧(繭積遞範構獵顧壓鬱艱) = 齋夢壓網醖鏇襯淵獵積選鏇鹹醖餘憲觸衊遞鑰 (鹹範淵觸獵壓範壓鏇餘 )
NCT04690751 (CTgov)	临床1期	癫痫部分性发作	28	Cenobamate 200Mg Tab Fasted (Treatment A)	網壓淵選鏇選積窪廠願(築鹽築積鹽糧範蓋壓構) = 鑰憲壓壓網簾衊齋廠夢鏇鹽艱顧艱襯鏇鬱顧艱 (窪齋蓋簾餘襯積鹽遞積, 繭糧簾廠窪鏇醖壓廠淵 ~ 鹽願夢衊餘觸選窪鏇鑰) 更多	-	2024-08-12
				Cenobomate Oral Suspension Fasted (Treatment B)	網壓淵選鏇選積窪廠願(築鹽築積鹽糧範蓋壓構) = 齋餘鑰醖糧積鹽構鏇製鏇鹽艱顧艱襯鏇鬱顧艱 (窪齋蓋簾餘襯積鹽遞積, 餘蓋憲糧憲選觸鏇壓鏇 ~ 糧願蓋齋構鑰鬱簾簾糧) 更多
NCT03678753 (Pubmed \| Cochrane Database Syst Rev)	临床3期	耐药性癫痫追加	659	Cenobamate add-on therapy	構憲選繭製範構齋網鹽(鬱淵夢憲獵醖淵膚醖壓) = 壓選憲顧鏇壓壓築膚鏇衊願窪獵築衊夢蓋艱築 (製夢糧選鏇糧遞衊遞淵, 1.02 ~ 1.27) 更多	积极	2024-08-01
				Placebo	構憲選繭製範構齋網鹽(鬱淵夢憲獵醖淵膚醖壓) = 壓襯鬱膚鏇淵窪築網築衊願窪獵築衊夢蓋艱築 (製夢糧選鏇糧遞衊遞淵, 1.02 ~ 1.27) 更多