Saleh Danish, Eskandari Maeve, Choudhury Lubna
Department of Medicine, Division of Cardiology, Northwestern University, Feinberg School of Medicine, Chicago, IL, USA.
Bluhm Cardiovascular Institute, Northwestern University Feinberg School of Medicine, Chicago, IL, USA.
Future Cardiol. 2025 Jun 18:1-7. doi: 10.1080/14796678.2025.2521183.
Aficamten is a novel cardiac myosin inhibitor that has completed a Phase III trial for the treatment of obstructive hypertrophic cardiomyopathy (HCM). Aficamten was developed to optimize pharmacokinetic properties and clinical tolerability relative to its predecessor, mavacamten. Mechanistically, aficamten decreases myocardial contractility by way of reducing cardiac myosin ATPase activity and the number of active actin-myosin cross bridges during the cardiac cycle. Clinically, aficamten improves cardiac hemodynamics and biomarker profiles while promoting favorable cardiac remodeling, augmenting exercise tolerance and improving overall health status. Observed systolic dysfunction was infrequent, mild, reversible, and not associated with serious adverse events. Collectively, the available data suggests that aficamten is a well-tolerated drug that shows strong clinical efficacy across a wide array of clinical parameters. In this review, we provide a comprehensive description of the pharmacology, clinical efficacy, and tolerability of aficamten.
阿非卡坦是一种新型心肌肌球蛋白抑制剂,已完成治疗梗阻性肥厚型心肌病(HCM)的III期试验。相对于其前身马伐卡坦,阿非卡坦在研发过程中优化了药代动力学特性和临床耐受性。从机制上讲,阿非卡坦通过降低心肌肌球蛋白ATP酶活性以及心动周期中活性肌动蛋白-肌球蛋白交叉桥的数量来降低心肌收缩力。在临床上,阿非卡坦可改善心脏血流动力学和生物标志物谱,同时促进有利的心脏重塑,增强运动耐量并改善整体健康状况。观察到的收缩功能障碍并不常见,程度较轻,具有可逆性,且与严重不良事件无关。总体而言,现有数据表明阿非卡坦是一种耐受性良好的药物,在广泛的临床参数中显示出强大的临床疗效。在本综述中,我们对阿非卡坦的药理学、临床疗效和耐受性进行了全面描述。