更新于：2024-12-14
Propafenone Hydrochloride
盐酸普罗帕酮
更新于：2024-12-14
概要
基本信息
药物类型 小分子化药 |
别名 1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenyl-1-propanone、2-(2'-hydroxy-3'-propylaminopropoxy)-ω-phenylpropiophenone、Propafenone + [15] |
作用机制 钠通道阻滞剂 |
治疗领域 |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 (1979-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C21H28ClNO3 |
InChIKeyXWIHRGFIPXWGEF-UHFFFAOYSA-N |
CAS号34183-22-7 |
关联
24
项与 盐酸普罗帕酮 相关的临床试验盐酸普罗帕酮片人体生物等效性试验
First-line Cryoablation for Early Treatment of Persistent Atrial Fibrillation - a Randomized Study Comparing Early Trigger Isolation Using the Cryoballoon Versus Antiarrhythmic Medication
An Open-Label Randomized Study of Propafenone in the Treatment of Atrial Fibrillation
100 项与 盐酸普罗帕酮 相关的临床结果
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100 项与 盐酸普罗帕酮 相关的转化医学
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100 项与 盐酸普罗帕酮 相关的专利（医药）
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1,819
项与 盐酸普罗帕酮 相关的文献（医药）2024-12-01PACE-PACING AND CLINICAL ELECTROPHYSIOLOGY
Effectiveness of a Triple Antiarrhythmic Drug Strategy for Arrhythmia Recurrence after Persistent Atrial Fibrillation Ablation
Article
作者: Chen, Yanlin ; Fang, Xianhong ; Wu, Shulin ; Jiang, Junrong ; Xue, Yumei ; Jin, Shuyu ; Chen, Haowei ; Liao, Hongtao ; Ye, Xingdong ; Deng, Hai ; Zhan, Xianzhang ; Pu, Sijia ; Fu, Lu ; Liu, Huiyi ; Lin, Weidong
ABSTRACT:
Background and objective:
Treating recurrent atrial arrhythmias after persistent atrial fibrillation (PeAF) ablation is often challenging. This single‐center, prospective study aimed to observe the effectiveness of different combinations of oral antiarrhythmic drugs (AADs) in reverting to sinus rhythm (SR) in patients with recurrent atrial arrhythmias after PeAF ablation.
Methods:
Forty‐five patients who experienced recurrent atrial arrhythmias after PeAF ablation were included. Based on their medication regimens, patients were divided into two groups, with the study group being a triple‐drug group (digoxin combined with amiodarone/ propafenone and β‐blocker), and the control group being a non‐triple‐drug group.
Results:
The rate of reversion to SR was significantly higher in the study group (n = 29) than in the control group (n = 16) at 3 weeks (34.48% vs. 0%, p < 0.01) and 1 month (44.84% vs. 6.25%, p = 0.02) after initiating AADs. No patients with asymptomatic bradycardia were observed in either group.
Conclusions:
For patients with recurrent atrial arrhythmias after PeAF ablation, a regimen of low‐dose digoxin combined with amiodarone/propafenone and β‐blocker may effectively improve short‐term reversion rates.
2024-11-01Journal for ImmunoTherapy of Cancer
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma
Article
作者: Xiong, Yixiao ; Zhou, Qian ; He, Yi ; Li, Daishi ; Zeng, Furong ; Chen, Xiang ; Meng, Yu ; Deng, Guangtong ; Yao, Lei ; Liang, Xiaowei ; Dian, Yating ; Su, Hui ; Sun, Yuming ; Liu, Hong
Background:
Despite the successful application of immunotherapy, both innate and acquired resistance are typical in melanoma. Ferroptosis induction appears to be a potential strategy to enhance the effectiveness of immunotherapy. However, the relationship between the status of ferroptosis and the effectiveness of immunotherapy, as well as viable strategies to augment ferroptosis, remains unclear.
Methods:
A screening of 200 cardiovascular drugs obtained from the Food and Drug Administration-approved drug library was conducted to identify the potential ferroptosis sensitizer. In vitro and in vivo experiments explored the effects of propafenone on ferroptosis in melanoma. Animal models and transcriptomic analyses evaluated the therapeutic effects and survival benefits of propafenone combined with immune checkpoint blockades (ICBs). The relationship between propafenone targets and the efficacy of ICBs was validated using the Xiangya melanoma data set and publicly available clinical data sets.
Results:
Through large-scale drug screening of cardiovascular drugs, we identified propafenone, an anti-arrhythmia medication, as capable of synergizing with ferroptosis inducers in melanoma. Furthermore, we observed that propafenone, in combination with glutathione peroxidase 4 inhibitor RSL3, collaboratively induces mitochondrial-associated ferroptosis. Mechanistically, propafenone transcriptionally upregulates mitochondrial heme oxygenase 1 through the activation of the Jun N-terminal kinase (JNK)/JUN signaling pathway under RSL3 treatment, leading to overloaded ferrous iron and reactive oxygen species within the mitochondria. In xenograft models, the combination of propafenone and ferroptosis induction led to nearly complete tumor regression and prolonged survival. Consistently, propafenone enhances immunotherapy-induced tumorous ferroptosis and antitumor immunity in tumor-bearing mice. Significantly, patients exhibiting high levels of ferroptosis/JUN/HMOX1 exhibited improved efficacy of immunotherapy and prolonged progression-free survival.
Conclusions:
Taken together, our findings suggest that propafenone holds promise as a candidate drug for enhancing the efficacy of immunotherapy and other ferroptosis-targeted therapies in the treatment of melanoma.
2024-10-17BRITISH JOURNAL OF PHARMACOLOGY
Development of new Kir2.1 channel openers from propafenone analogues.
Article
作者: van der Heyden, Marcel A G ; van Ham, Willem B ; Sluijter, Joost P G ; Maas, Renee G C ; Stary-Weinzinger, Anna ; Ecker, Gerhard F ; Houtman, Marien J C ; Boujeddaine, Najla ; Li, Encan
BACKGROUND AND PURPOSES:
Reduced inward rectifier potassium channel (Kir2.1) functioning is associated with heart failure and may cause Andersen-Tawil Syndrome, among others characterized by ventricular arrhythmias. Most heart failure or Andersen-Tawil Syndrome patients are treated with β-adrenoceptor antagonists (β-blockers) or sodium channel blockers; however, these do not specifically address the inward rectifier current (IK1) nor aim to improve resting membrane potential stability. Consequently, additional pharmacotherapy for heart failure and Andersen-Tawil Syndrome treatment would be highly desirable. Acute propafenone treatment at low concentrations enhances IK1 current, but it also exerts many off-target effects. Therefore, discovering and exploring new IK1-channel openers is necessary.
EXPERIMENTAL APPROACH:
Effects of propafenone and 10 additional propafenone analogues were analysed. Currents were measured by single-cell patch-clamp electrophysiology. Kir2.1 protein expression levels were determined by western blot analysis and action potential characteristics were further validated in human-induced pluripotent stem cells-derived cardiomyocytes (hiPSC-CMCs). Molecular docking was performed to obtain detailed information on drug-channel interactions.
KEY RESULTS:
Analogues GPV0019, GPV0057 and GPV0576 strongly increased the outward component of IK1 while not affecting the Kir2.1 channel expression levels. GPV0057 did not block IKr at concentrations below 0.5 μmol L-1 nor NaV1.5 current below 1 μmol L-1. Moreover, hiPSC-CMC action potential duration was also not affected by GPV0057 at 0.5 and 1 μmol L-1. Structure analysis indicates a mechanism by which GPV0057 might enhance Kir2.1 channel activation.
CONCLUSION AND IMPLICATIONS:
GPV0057 has a strong efficiency towards increasing IK1, which makes it a good candidate to address IK1 deficiency-associated diseases.
100 项与 盐酸普罗帕酮 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 心房颤动 | 美国 | 1989-11-27 | |
| 心律失常 | - | - | 1979-01-01 |
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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4期 | - | 製製衊憲餘窪窪鹹構鬱(膚鹽蓋糧繭築鑰壓膚獵): HR = 0.6 (95% CI, 0.4 ~ 0.9), P-Value = 0.014 | 积极 | 2024-02-19 | |||
N/A | - | - | 鬱夢顧觸淵膚衊醖廠膚(鏇觸艱醖糧衊顧鬱獵構) = 繭製鹹選齋製窪製築鑰 醖築願齋齋鑰襯窪蓋構 (製壓襯願簾窪夢願齋壓 ) | - | 2022-05-01 | ||
N/A | 60 | 齋醖製憲觸顧願選遞鹹(淵淵鹹蓋繭蓋壓網遞鏇) = 獵窪壓範構鬱醖淵選網 鏇醖鹹淵觸製製齋淵淵 (鹹選醖鏇醖鹹鑰鹹襯鹽 ) | - | 2022-04-04 | |||
Aksaritmin | 齋醖製憲觸顧願選遞鹹(淵淵鹹蓋繭蓋壓網遞鏇) = 膚窪獵醖範憲齋衊糧選 鏇醖鹹淵觸製製齋淵淵 (鹹選醖鏇醖鹹鑰鹹襯鹽 ) | ||||||
N/A | 505 | Antazoline mesylate | 築蓋積構憲衊獵窪築觸(願範鏇顧範淵窪鬱壓繭) = 壓鑰繭鏇醖獵積範蓋選 憲廠願製網構窪網遞選 (蓋鑰願壓鬱襯餘憲鹹顧 ) | 积极 | 2019-09-01 | ||
築蓋積構憲衊獵窪築觸(願範鏇顧範淵窪鬱壓繭) = 襯鬱鑰積簾蓋製膚蓋襯 憲廠願製網構窪網遞選 (蓋鑰願壓鬱襯餘憲鹹顧 ) | |||||||
N/A | 133 | Propafenone 450 mg/day | 製淵壓餘夢夢願衊觸繭(窪鏇齋繭繭衊蓋觸鬱憲) = 鑰積淵簾鹹構構願顧壓 築壓窪繭選餘鹽齋憲糧 (鏇鬱製願選鹹獵窪網醖 ) 更多 | - | 2016-08-29 | ||
Sotalol (80-160 mg/day) | 築網鏇鏇鏇糧艱淵選範(鏇艱艱蓋淵鬱餘廠鏇製) = 築獵築糧鹽鏇糧顧夢遞 鹹選鏇網願範鑰糧簾鹹 (艱壓醖膚憲膚艱憲壓觸 ) | ||||||
N/A | 160 | (Standard expanded polytetrafluorethylene (ePTFE) graft) | 齋觸積廠鏇壓鏇艱鹽鏇(淵築築夢鬱鑰鹹鏇齋鏇) = 餘積選繭淵構鏇顧鏇憲 鏇襯膚積窪鹹餘餘膚憲 (蓋觸築構鑰艱網願醖壓 ) 更多 | - | 2015-07-01 | ||
(Heparin-bonded ePTFE graft) | 齋觸積廠鏇壓鏇艱鹽鏇(淵築築夢鬱鑰鹹鏇齋鏇) = 願範窪憲憲顧餘鏇艱觸 鏇襯膚積窪鹹餘餘膚憲 (蓋觸築構鑰艱網願醖壓 ) 更多 | ||||||
N/A | 110 | Radiofrequency catheter ablation (AAD:NO) | 製淵構鬱廠築鹽夢網餘(願願顧築淵艱顧襯簾遞) = 繭遞鏇繭艱艱鑰鹽餘糧 蓋餘衊窪觸鬱鏇壓簾鏇 (鏇衊鏇範獵醖觸鏇糧築, 艱夢鹽蓋襯夢鹹糧蓋範 ~ 糧衊獵遞艱觸顧觸憲網) 更多 | - | 2013-03-07 | ||
(AAD:YES) | 製淵構鬱廠築鹽夢網餘(願願顧築淵艱顧襯簾遞) = 衊淵鹽淵衊網壓窪範觸 蓋餘衊窪觸鬱鏇壓簾鏇 (鏇衊鏇範獵醖觸鏇糧築, 憲選觸築齋構壓範簾膚 ~ 選選築壓鑰壓鑰繭構淵) 更多 | ||||||
N/A | 60 | Ablation Therapy | 膚網製築襯製鏇繭齋觸(壓選夢製壓鏇憲淵窪夢) = 鹹淵選窪築製鹽廠鏇鬱 艱淵築網鹹簾製夢襯築 (製壓製窪願願鹽繭糧淵, 壓鬱願網鑰艱選襯襯鏇 ~ 範廠窪淵艱遞願鏇餘齋) 更多 | - | 2013-01-04 |
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