Campbell Craig, McMillan Hugh J, Mah Jean K, Tarnopolsky Mark, Selby Kathryn, McClure Ty, Wilson Dawn M, Sherman Matthew L, Escolar Diana, Attie Kenneth M
Pediatrics, Epidemiology and Clinical Neurological Sciences, Western University, London, Ontario, Canada.
Children's Hospital of Eastern Ontario, University of Ottawa, Ottawa, Ontario, Canada.
Muscle Nerve. 2017 Apr;55(4):458-464. doi: 10.1002/mus.25268. Epub 2016 Dec 23.
ACE-031 is a fusion protein of activin receptor type IIB and IgG1-Fc, which binds myostatin and related ligands. It aims to disrupt the inhibitory effect on muscle development and provide potential therapy for myopathies like Duchenne muscular dystrophy (DMD).
ACE-031 was administered subcutaneously every 2-4 weeks to DMD boys in a randomized, double-blind, placebo-controlled, ascending-dose trial. The primary objective was safety evaluation. Secondary objectives included characterization of pharmacokinetics and pharmacodynamics.
ACE-031 was not associated with serious or severe adverse events. The study was stopped after the second dosing regimen due to potential safety concerns of epistaxis and telangiectasias. A trend for maintenance of the 6-minute walk test (6MWT) distance in the ACE-031 groups compared with a decline in the placebo group (not statistically significant) was noted, as was a trend for increased lean body mass and bone mineral density (BMD) and reduced fat mass.
ACE-031 use demonstrated trends for pharmacodynamic effects on lean mass, fat mass, BMD, and 6MWT. Non-muscle-related adverse events contributed to the decision to discontinue the study. Myostatin inhibition is a promising therapeutic approach for DMD. Muscle Nerve 55: 458-464, 2017.
ACE-031是一种IIB型激活素受体与IgG1-Fc的融合蛋白,可结合肌肉生长抑制素及相关配体。其目的是消除对肌肉发育的抑制作用,并为诸如杜氏肌营养不良症(DMD)等肌病提供潜在治疗方法。
在一项随机、双盲、安慰剂对照、剂量递增试验中,每2至4周给患DMD的男孩皮下注射ACE-031。主要目的是安全性评估。次要目的包括对药代动力学和药效学进行表征。
ACE-031与严重或重度不良事件无关。由于鼻出血和毛细血管扩张的潜在安全问题,在第二个给药方案后研究停止。与安慰剂组距离下降(无统计学意义)相比,ACE-031组在6分钟步行试验(6MWT)距离上有维持趋势,同时瘦体重、骨矿物质密度(BMD)增加和脂肪量减少也有趋势。
使用ACE-031在瘦体重、脂肪量、BMD和6MWT方面显示出药效学作用趋势。非肌肉相关不良事件促使做出停止研究的决定。抑制肌肉生长抑制素是治疗DMD的一种有前景的治疗方法。《肌肉与神经》55: 458 - 464, 2017年。