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心房颤动药物研发中的新型钾离子通道靶点——我们进展如何?

Novel K+ Channel Targets in Atrial Fibrillation Drug Development--Where Are We?

作者信息

El-Haou Said, Ford John W, Milnes James T

机构信息

Xention Ltd, Cambridge, United Kingdom.

出版信息

J Cardiovasc Pharmacol. 2015 Nov;66(5):412-31. doi: 10.1097/FJC.0000000000000277.

Abstract

There is a clear unmet medical need for new pharmacologic therapies with improved efficacy and safety for the treatment of atrial fibrillation. Considerable research efforts have been undertaken to discover and develop new safe and effective antiarrhythmic drugs that specifically target atrial K(+) channels. To realize the full value of these novel atrial-specific therapeutic drug targets, demonstration of clinical efficacy and safety is required for a new breed of atrial-selective antiarrhythmic drugs. The reward for demonstrating this in a pivotal phase III trial, on regulatory approval, will be "first-in-class" status. This article reviews the development status of new and novel K channel inhibitors currently in drug development as atrial-selective antiarrhythmics for the treatment of atrial fibrillation.

摘要

对于治疗心房颤动,显然存在对具有更高疗效和安全性的新药物疗法的未满足医疗需求。人们已经付出了相当多的研究努力来发现和开发专门针对心房钾离子通道的新型安全有效的抗心律失常药物。为了实现这些新型心房特异性治疗药物靶点的全部价值,需要新一代心房选择性抗心律失常药物证明其临床疗效和安全性。在关键的III期试验中证明这一点并获得监管批准后,回报将是“同类首创”的地位。本文综述了目前正在研发的新型钾通道抑制剂作为治疗心房颤动的心房选择性抗心律失常药物的开发状况。

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