New drugs targeting the cardiac ultra-rapid delayed-rectifier Current(IKur):: Rationale, pharmacology and evidence for potential therapeutic value

被引：76

作者：

Ford, John W. ^{[1
]}

Milnes, James T. ^{[1
]}

机构：

[1] Xention Ltd, Cambridge CB22 3EG, England

来源：

JOURNAL OF CARDIOVASCULAR PHARMACOLOGY | 2008年 / 52卷 / 02期

关键词：

atrial fibrillation; atrial flutter; I-Kur; Kv1.5; ultra-rapid delayed rectifier; cardiac; heart; arrhythmia;

D O I：

10.1097/FJC.0b013e3181719b0c

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

There is a clear unmet medical need for new pharmacologic therapies for the treatment of atrial fibrillation (AF) with improved efficacy and safety. This article reviews the development of new and novel Kv1.5/ultra-rapid delayed-rectifier current (I-Kur) inhibitors and presents evidence that Kv1.5 modulation provides an atrial-selective mechanism for treating AF Academia and industry have invested heavily in Kv1.5 (> 500 scientific publications and > 50 patients published since 1993); however, to realize the full value of this therapeutic drug clinical efficacy and safety data are required for a selective Kv1.5 modulator. The reward for demonstrating clinical efficacy and safety in a pivotal Phase 3 trial, on regulatory approval, is "first in class" status.

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收藏

页码：105 / 120

页数：16

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