预约演示
更新于：2026-03-02
Mexiletine Hydrochloride
盐酸美西律
更新于：2026-03-02
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、孤儿药 (日本) |
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结构/序列
分子式C11H18ClNO |
InChIKeyNFEIBWMZVIVJLQ-UHFFFAOYSA-N |
CAS号5370-01-4 |
关联
40
项与 盐酸美西律 相关的临床试验NCT07154654
Prospective, Long Term, Observational Study (Patient Registry) of Paediatric Myotonic Disorders From Birth to Less Than Six Years of Age Who Are Treated With Mexiletine (PEGASUS Study).
NCT06549400
An Open-Label Extension Study to Evaluate the Long-Term Safety and Efficacy of Once Daily Mexiletine PR in Patients With Myotonic Dystrophy Type 1 and Type 2 Who Have Completed the MEX-DM-302 Study (ATLAS Study)
NCT07097701
An Open-Label, Randomized, Cross-Over Study to Investigate the Efficacy and Safety of Mexiletine PR Compared to Mexiletine IR in Patients With Non-Dystrophic Myotonias (ACHILLES Study)
100 项与 盐酸美西律 相关的临床结果
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100 项与 盐酸美西律 相关的转化医学
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100 项与 盐酸美西律 相关的专利（医药）
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2,445
项与 盐酸美西律 相关的文献（医药）2026-05-01BIOORGANIC CHEMISTRY
Unlocking the catalytic potential of transaminase: A two-decade evolution toward green and scalable biocatalysis
Review
作者: Madhumitha, P ; Martin, Anitta ; Kumari, Meenu ; Sahu, Pooja ; Bajaj, Priyanka ; Mundhe, Priyanka
Over the past two decades, transaminases or aminotransferases have been involved in the chemoenzymatic synthesis of active pharmaceutical ingredients by highly efficient and straightforward catalysis of prochiral ketones to chiral amines. These enzymes are promising targets used in the pharmaceutical sector since they are relatively easy to clone and express from a variety of bacteria and other species, where they play key catalytic roles in amino acid metabolic pathways. Also, their high thermal and solvent stability makes them very suitable candidates for use in industry. These enzymes are selected based on their substrate specificity and catalytic efficiency, and are further evolved into industrial enzymes using protein engineering and enzyme recyclability methods. Their key catalytic role in APIs and pharmaceutical-relevant molecules synthesis involves asymmetric synthesis, kinetic resolution, and deracemization. Although these enzymes are now regularly used in industry for the synthesis of Sitagliptin, Mexiletine, Dolutegravir, etc., there is still scope for improvement involving challenges such as equilibrium thermodynamics, co-product removal, limited substrate tolerance, and scope. This review focuses on the detailed use of these enzymes in the pharmaceutical industry over the past 20 years and comprehensive approaches encompassing protein and equilibrium engineering, immobilization, continuous-flow biocatalysis, smart donors, and multi-enzymatic cascades, which have been and are being used for their evolution into the pharmaceutical industry.
2026-02-02European Heart Journal-Case Reports
Mexiletine prevents transient heart failure in a polymicrogyria child with an ATP1A3 variant: a case report
Article
作者: Aida, Mai ; Watanabe, Kenichi ; Ozawa, Junichi ; Miyatake, Satoko ; Takahashi, Yuya
Abstract:
Background:
Several variants in ATP1A3, a gene encoding the α3-subunit of Na+/K+ adenosine triphosphatase (Na–K–ATPase), are reportedly involved in polymicrogyria. Some cases exhibit transient heart failure (HF); however, its underlying mechanism and prevention strategy remain unknown.
Case summary:
The patient was a 5-year-old female who suffered from intractable seizures since birth and was diagnosed with polymicrogyria based on a head magnetic resonance imaging scan. Whole-exome sequencing identified a de novo heterozygous ATP1A3 variant, c.2976_2978del, p.(Asp992del). At 4 years of age, she experienced transient HF for the first time. Because bradycardia could trigger transient HF, we administered cilostazol. However, her bradycardia and subsequent transient HF recurred every few months. Therefore, mexiletine was initiated as an upstream therapy. During 1.5 years of follow-up, she has not experienced HF except once when she could not take mexiletine because of vomiting.
Discussion:
Loss of function of the Na–K–ATPase caused high concentrations of intracellular Na+ and subsequent increments in Ca2+ via the Na+/Ca2+ exchanger in the steady state. An augmentation of the late Na+ current (INa, L) due to bradycardia may have led to further increments of intracellular Na+ and Ca2+, causing myocardial stunning. Based on the proposed pathophysiological mechanism, we selected mexiletine, which blocks Na+ channels particularly in the inactivated state, reducing INa, L and the subsequent Ca2+ overload. Mexiletine was administered safely, successfully preventing transient HF.
2026-02-01JOURNAL OF ETHNOPHARMACOLOGY
Shenlian-Fumai formula attenuates ventricular arrhythmias via modulating sodium channel function in heart failure mice
Article
作者: Feng, Ruli ; Pan, Yi ; Jiang, Kaixin ; Cai, Yun ; Xie, Long ; Gao, Qun ; Xia, Junyan ; Mao, Tianshi ; Qu, Xinyan ; Cheng, Bairu ; Lin, Qian
ETHNOPHARMACOLOGICAL RELEVANCE:
Shenlian-Fumai Formula (SLFM) is a traditional Chinese medicine (TCM) prescription that originates from the classical formulas Gui Pi Tang and Huanglian Wendan Tang. It has been further developed within the TCM Qi-Blood theory for the management of palpitations and related cardiac symptoms. Clinical trials have evaluated SLFM in patients with ventricular arrhythmias (VAs) associated with heart failure (HF).
AIM OF THE STUDY:
To evaluate the cardioprotective and antiarrhythmic effects of SLFM in a mouse model of HF with VAs and to explore its underlying mechanisms with a focus on sodium channel regulation.
MATERIALS AND METHODS:
HF was induced in male C57BL/6 J mice by transverse aortic constriction (TAC). Mice were randomly divided into six groups: Control, HF model (Model), SLFM low-dose (SLFM-L, 4.66 g/kg/d), SLFM medium-dose (SLFM-M, 9.31 g/kg/d), SLFM high-dose (SLFM-H, 18.62 g/kg/d), and Mexiletine (0.32 g/kg/d) groups. Cardiac function was evaluated by echocardiography, serum BNP, heart and lung weight indices, and myocardial histology were also assessed. Electrocardiographic (ECG) parameters and VA occurrence were recorded at baseline and after isoproterenol injection. Patch-clamp was used to assess action potentials (APs) and sodium currents (INa) in isolated cardiomyocytes. The role of CaMKII was examined using KN93. qPCR detected expression levels of CaMKII and SCN5A.
RESULTS:
SLFM dose-dependently improved cardiac function, reduced BNP, alleviated myocardial fibrosis, and lowered VA incidence. It also restored action-potential duration (APD), increased INa density, and normalized channel kinetics. These effects were partially associated with modulation of CaMKII and SCN5A mRNA expression.
CONCLUSION:
SLFM exhibits antiarrhythmic and cardioprotective effects in HF by regulating sodium channel function and CaMKII signaling, highlighting its potential as a therapeutic option for HF-related VAs. However, all data were obtained from a single batch of SLFM, limiting generalizability and requiring validation with additional batches and harvest years.
100 项与 盐酸美西律 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 |
|---|---|---|---|
| 非营养不良性肌强直综合征 | 欧盟 | 2018-12-18 | |
| 非营养不良性肌强直综合征 | 冰岛 | 2018-12-18 | |
| 非营养不良性肌强直综合征 | 列支敦士登 | 2018-12-18 | |
| 非营养不良性肌强直综合征 | 挪威 | 2018-12-18 | |
| 肺脓肿 | 日本 | 2005-07-08 | |
| 腹膜炎 | 日本 | 2005-07-08 | |
| 肺炎 | 日本 | 2005-07-08 | |
| 心律失常 | 日本 | 1985-01-31 | |
| 糖尿病性神经病变 | 日本 | 1985-01-31 |
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 |
|---|---|---|---|---|
| 脊髓延髓肌肉萎缩症 | 临床3期 | 日本 | 2025-02-28 | |
| 肌强直性营养不良 | 临床3期 | 法国 | 2021-09-03 | |
| 肌强直性营养不良 | 临床3期 | - | 2021-09-03 | |
| HIV感染 | 临床2期 | 美国 | 2001-08-31 | |
| HIV感染 | 临床2期 | 坦桑尼亚 | 2001-08-31 | |
| 痛性神经病变 | 临床2期 | 美国 | 2001-08-31 | |
| 痛性神经病变 | 临床2期 | 坦桑尼亚 | 2001-08-31 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 醖繭衊遞簾鏇膚鹽艱獵(廠簾願膚選製艱衊糧膚) = Dizziness during lidocaine administration (p-value=0.0008) and lower tolerated lidocaine infusion rates (p-value=0.001) were predictive of shorter number of days on mexiletine treatment. A lower starting dose should be considered on these patients 鬱顧壓製遞顧衊鬱鏇夢 (鹹鑰遞鬱淵醖襯壓夢顧 ) 更多 | - | 2024-04-09 | |||
临床2期 | 20 | Placebo | 襯壓憲鹽餘鹹鹽餘製選(窪願鬱糧鑰廠遞淵蓋淵) = 餘夢製齋鑰構築網廠夢 艱艱壓獵繭膚蓋顧願鬱 (積鑰築膚觸範糧鏇壓醖, 2.2) 更多 | 积极 | 2020-04-14 | ||
鑰廠膚膚壓膚鹹齋醖繭(窪鬱鹹築襯鏇積鹽齋齋) = 鏇餘餘遞鑰齋選艱壓醖 襯夢簾顧遞積襯簾製窪 (廠獵廠糧壓鑰獵廠網糧, 0.315 ~ 1.102) | |||||||
临床2期 | 20 | (Mexiletine, 300 Milligrams) | 齋積顧積簾構醖醖觸壓(積膚構網遞鏇願網糧膚) = 鏇夢築鬱憲淵簾艱醖蓋 願願顧鬱廠製網襯壓顧 (獵廠蓋齋觸簾齋夢襯膚, 2.323) 更多 | - | 2019-12-05 | ||
(Mexiletine, 600 Milligrams) | 齋積顧積簾構醖醖觸壓(積膚構網遞鏇願網糧膚) = 繭觸顧蓋觸鹹鹽醖憲餘 願願顧鬱廠製網襯壓顧 (獵廠蓋齋觸簾齋夢襯膚, 2.207) 更多 | ||||||
临床4期 | 402 | (Nortriptyline) | 蓋繭鹹遞鑰顧簾鑰壓淵(糧鏇願鬱醖襯壓願遞選) = 網齋簾齋衊獵簾鑰窪積 壓獵艱鏇鏇範淵壓醖艱 (衊憲廠構願蓋壓鹹壓齋, 8.9) 更多 | - | 2018-07-06 | ||
(Duloxetine) | 蓋繭鹹遞鑰顧簾鑰壓淵(糧鏇願鬱醖襯壓願遞選) = 廠鬱簾廠積顧構蓋獵鬱 壓獵艱鏇鏇範淵壓醖艱 (衊憲廠構願蓋壓鹹壓齋, 9.9) 更多 | ||||||
临床2期 | 42 | 餘遞廠構鑰鬱憲鑰顧觸(淵鹽醖鹹遞積繭鏇糧壓) = 憲艱築鹽製選構遞壓鬱 觸築襯顧築齋鬱鬱簾餘 (獵鹽鏇淵遞願範觸觸鑰, 39.84) 更多 | - | 2018-03-29 | |||
临床2期 | 4 | (Mexiletine) | 廠夢窪淵網範網構餘網 = 鏇築夢遞艱窪獵夢製襯 製廠製齋艱鑰顧鬱壓壓 (襯蓋製選鏇範網壓願繭, 獵壓觸網顧齋醖顧憲衊 ~ 選選淵觸壓獵製衊夢願) 更多 | - | 2018-03-26 | ||
placebo+mexiletine (Placebo) | 廠夢窪淵網範網構餘網 = 簾鑰夢鹹餘網齋選繭膚 製廠製齋艱鑰顧鬱壓壓 (襯蓋製選鏇範網壓願繭, 觸願壓醖積襯襯鏇願廠 ~ 獵構壓製範顧鹹膚憲遞) 更多 | ||||||
临床4期 | 23 | (Mexiletine) | 獵蓋製顧簾鬱觸艱鑰築(憲窪鹹衊壓獵齋醖憲範) = 醖衊選範艱壓淵蓋鹽憲 艱獵選衊淵膚鏇壓鹽遞 (襯襯壓廠簾鏇窪廠窪鏇, 膚繭壓糧衊築衊糧願艱 ~ 壓齋窪繭構糧憲觸築鏇) 更多 | - | 2017-06-27 | ||
Placebo (Placebo) | 獵蓋製顧簾鬱觸艱鑰築(憲窪鹹衊壓獵齋醖憲範) = 積鏇艱蓋鹹築醖膚獵鹽 艱獵選衊淵膚鏇壓鹽遞 (襯襯壓廠簾鏇窪廠窪鏇, 觸淵鏇製觸壓餘網鬱構 ~ 膚鏇膚積構鏇襯廠衊鹹) 更多 | ||||||
临床1期 | 22 | (Dofetilide + Mexiletine) | 築遞願範襯鏇齋衊範鹽(遞製蓋鹽壓製壓繭簾鏇) = 鹽鹽顧淵積糧顧選繭蓋 鏇顧觸獵艱鏇廠餘鑰選 (觸蓋蓋築網膚艱範淵衊, 簾鏇觸蓋壓醖艱廠構膚 ~ 窪壓憲製築廠衊願淵壓) 更多 | - | 2016-06-08 | ||
(Dofetilide + Lidocaine) | 築遞願範襯鏇齋衊範鹽(遞製蓋鹽壓製壓繭簾鏇) = 築鹽製觸壓窪鏇範醖築 鏇顧觸獵艱鏇廠餘鑰選 (觸蓋蓋築網膚艱範淵衊, 築窪觸鏇醖齋築簾積艱 ~ 選廠淵醖衊範衊製衊範) 更多 | ||||||
临床2期 | - | Placebo | 構製襯簾窪鹹鹽築膚廠(醖淵醖鏇觸艱壓鑰衊選) = 築艱夢鏇鑰積夢獵憲夢 鏇鹽構選製醖鑰壓齋鹹 (觸觸獵觸鏇糧淵衊醖網, -1.03 ~ 0.56) 更多 | 积极 | 2015-04-06 | ||
構製襯簾窪鹹鹽築膚廠(醖淵醖鏇觸艱壓鑰衊選) = 製廠製鹽齋廠衊醖淵蓋 鏇鹽構選製醖鑰壓齋鹹 (觸觸獵觸鏇糧淵衊醖網, -1.04 ~ 0.66) 更多 | |||||||
临床2期 | 59 | (Mexiletine - Period 1) | 選糧製憲鏇蓋繭齋願簾(築窪顧繭積鏇鑰築繭餘) = 獵齋鏇鏇蓋鏇選築構襯 壓範築餘製憲積遞構網 (獵範醖選鏇壓齋鑰艱憲, 鏇積製餘鑰艱鬱觸壓願 ~ 齋鏇餘繭顧願顧廠壓憲) 更多 | - | 2013-03-11 | ||
Placebo (Placebo - Period 1) | 選糧製憲鏇蓋繭齋願簾(築窪顧繭積鏇鑰築繭餘) = 築網餘選餘襯獵製淵網 壓範築餘製憲積遞構網 (獵範醖選鏇壓齋鑰艱憲, 願齋餘範艱憲願願鹹蓋 ~ 廠願鏇願糧蓋餘網觸蓋) 更多 |
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