Webmavacamten又称MYK-461,是选择性心肌β肌球蛋白三磷酸腺苷(ATP)酶变构抑制剂,特. 异性抑制肌球蛋白MYH7突变导致的ATP酶过度激活,可逆性抑制心肌肌球蛋白与肌动蛋白耦. 联反应,减缓横桥周期,还能降低心肌肌球蛋白钙离子敏感性,从而引起肌节收缩分数减 WebMYK-461 is a small molecular chemical that reduces contractility by decreasing the adenosine triphosphatase activity of the cardiac myosin heavy chain. MYK-461 reduced ATPase activity in a dose-dependent manner with IC50 value of 0.3 mM after treatment of mouse cardiac myofibrils. MYK-461 (>10 mM) decreased the maximal ATPase rate by …
Evaluation of Mavacamten in Symptomatic Patients With
Web28 jun. 2024 · The PIONEER-HCM (A Phase 2 Open-label Pilot Study Evaluating MYK-461 in Subjects With Symptomatic Hypertrophic Cardiomyopathy and Left Ventricular Outflow Tract Obstruction) trial was a phase II, non-randomized, open-label study of mavacamten in 21 symptomatic patients (NYHA Class II-III) with oHCM in which mavacamten was … Web5 okt. 2024 · Mavacamten (MYK-461) is an oral, allosteric modulator of cardiac myosin being developed initially for symptomatic, obstructive hypertrophic cardiomyopathy (HCM). BMS said it planned to submit an... naruto characters that use swords
Targeting the sarcomere in inherited cardiomyopathies - Nature
Web8 apr. 2024 · PIONEER-HCM (Pilot Study Evaluating MYK‐461 in Subjects with Symptomatic Hypertrophic Cardiomyopathy and Left Ventricular Outflow Tract Obstruction) was a phase 2 open-label study whose primary endpoint was reduction in post-exercise LVOT gradient in obstructive HCM. 13 The investigators divided the 21 patients into … WebThe objectives of this randomized, placebo-controlled trial are to assess safety, tolerability, preliminary pharmacokinetics and pharmacodynamics of MYK-491. ... MyoKardia’s most advanced product candidate is mavacamten (formerly MYK-461). Mavacamten is a novel, oral, allosteric modulator of cardiac myosin that reduced hypercontractility in ... Web11 aug. 2024 · 该研究首次提出:MYK-461(Mavacamten化学名)作为肌节收缩蛋白的小分子抑制剂有望成为HCM治疗的一种有效尝试。 在基础实验中,研究人员首先筛选鉴定出一些能够降低心肌收缩力的特定化合物,然后对这些化合物进行分析,结果发现MYK-461可以通过降低心肌肌球蛋白重链的ATP酶活性来降低心肌收缩力。 naruto characters shisui