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摘要: Mavacamten是一种小分子肌球蛋白抑制剂,在治疗人类肥厚型心肌病(HCM)的潜在药物的筛选中被发现。Mavacamten可逆地抑制肌球蛋白与肌动蛋白的结合,抑制肌节力的产生,降低心肌高收缩性。临床试验也进一步证明其可以降低左心室流出道压力,减轻临床症状。现就Mavacamten的作用机制、临床价值及最新发现作一综述。Abstract: Mavacamten is an allosteric inhibitor of sarcomeric myosins identified in a small-molecule screening of potential drugs for the treatment of human hypertrophic cardiomyopathy (HCM). Mavacamten reversibly inhibits the binding of myosin to actin, inhibits sarcomere force, and reduces myocardial hypercontractility. Clinical trials have further demonstrated that Mavacamten can reduce the left ventricular outflow tract (LOVT) pressure and alleviate the clinical symptoms of HCM. This paper reviews the mechanism of action, clinical application, and prospect of Mavacamten.
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Key words:
- hypertrophic cardiomyopathy /
- myosin modulator /
- myosin /
- pharmacological treatment
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