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肌球蛋白抑制剂 CK-586 可轻微降低收缩功能并改善猫肥厚型心肌病的梗阻。

Cardiac myosin inhibitor, CK-586, minimally reduces systolic function and ameliorates obstruction in feline hypertrophic cardiomyopathy.

机构信息

Department of Clinical Sciences, College of Veterinary Medicine, North Carolina State University, 1060 William Moore Dr, Raleigh, NC, 27607, USA.

Department of Medicine and Epidemiology, School of Veterinary Medicine, University of California-Davis, Davis, CA, USA.

出版信息

Sci Rep. 2024 May 27;14(1):12038. doi: 10.1038/s41598-024-62840-3.

Abstract

Hypertrophic cardiomyopathy (HCM) remains the most common cardiomyopathy in humans and cats with few preclinical pharmacologic interventional studies. Small-molecule sarcomere inhibitors are promising novel therapeutics for the management of obstructive HCM (oHCM) patients and have shown efficacy in left ventricular outflow tract obstruction (LVOTO) relief. The objective of this study was to explore the 6-, 24-, and 48-hour (h) pharmacodynamic effects of the cardiac myosin inhibitor, CK-586, in six purpose-bred cats with naturally occurring oHCM. A blinded, randomized, five-treatment group, crossover preclinical trial was conducted to assess the pharmacodynamic effects of CK-586 in this oHCM model. Dose assessments and select echocardiographic variables were assessed five times over a 48-h period. Treatment with oral CK-586 safely ameliorated LVOTO in oHCM cats. CK-586 treatment dose-dependently eliminated obstruction (reduced LVOTOmaxPG), increased measures of systolic chamber size (LVIDs Sx), and decreased select measures of heart function (LV FS% and LV EF%) in the absence of impact on heart rate. At all tested doses, a single oral CK-586 dose resulted in improved or resolved LVOTO with well-tolerated, dose-dependent, reductions in LV systolic function. The results from this study pave the way for the potential use of CK-586 in both the veterinary and human clinical setting.

摘要

肥厚型心肌病(HCM)仍然是人类和猫最常见的心肌病,很少有临床前药理学干预研究。小分子肌球蛋白抑制剂是治疗梗阻性肥厚型心肌病(oHCM)患者的有前途的新型治疗方法,已显示出在缓解左心室流出道梗阻(LVOTO)方面的疗效。本研究旨在探讨心脏肌球蛋白抑制剂 CK-586 在 6 只自然发生 oHCM 的专用bred 猫中的 6、24 和 48 小时(h)药效学作用。进行了一项盲法、随机、五治疗组交叉临床前试验,以评估 CK-586 在这种 oHCM 模型中的药效学作用。在 48 小时期间评估了 5 次剂量评估和选择超声心动图变量。口服 CK-586 治疗可安全改善 oHCM 猫的 LVOTO。CK-586 治疗剂量依赖性地消除了梗阻(减少 LVOTOmaxPG),增加了收缩室大小(LVIDs Sx)的指标,并降低了心脏功能的某些指标(LV FS%和 LV EF%),而对心率没有影响。在所有测试剂量下,单次口服 CK-586 剂量可改善或解决 LVOTO,并具有良好耐受的剂量依赖性降低 LV 收缩功能。本研究的结果为 CK-586 在兽医和人类临床环境中的潜在用途铺平了道路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd11/11130313/aabb8659b8fe/41598_2024_62840_Fig1_HTML.jpg

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