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正在进行临床试验的选择性雄激素受体调节剂 (SARMs) 作为肌肉减少症的药物治疗。

Selective androgen receptor modulators (SARMs) as pharmacological treatment for muscle wasting in ongoing clinical trials.

机构信息

Heart Institute (Incor), University of São Paulo Medical School , São Paulo, Brazil.

Department of Cardiology and Pneumology, University of Göttingen Medical Center , Göttingen, Germany.

出版信息

Expert Opin Investig Drugs. 2020 Aug;29(8):881-891. doi: 10.1080/13543784.2020.1777275. Epub 2020 Jun 18.

DOI:10.1080/13543784.2020.1777275
PMID:32476495
Abstract

INTRODUCTION

Skeletal muscle wasting is a frequent clinical problem encountered in patients with chronic diseases. Increased levels of inflammatory markers play a role in the imbalance between muscle protein synthesis and degradation. Although testosterone has long been proposed as a treatment for patients with muscle wasting, undesirable side effects have raised concerns about prostatic hypertrophy in men as well as virilization in women. Selective androgen receptor modulators (SARMs) have demonstrated similar results like testosterone at improving lean body mass (LBM) with less side effects on androgen-dependent tissue.

AREAS COVERED

This review outlines the ongoing clinical development in the field of SARMs and their effectiveness in improving body composition and physical function. The included articles were collected at pubmed.gov and analyzed integrally.

EXPERT OPINION

There is an unmet clinical need for safe and effective anabolic compounds such as SARMs. Despite the effect on LBM shown by SARMs in phase II clinical trials, results on improved physical function and muscle strength are still lacking and long-term outcomes have to be assessed in these patients. Moreover, there is a need to determine the effect of resistance exercise training and protein intake associated with SARMs in the treatment of patients with muscle wasting.

摘要

简介

骨骼肌减少症是慢性疾病患者中常见的临床问题。炎症标志物水平升高在肌肉蛋白合成和降解之间的失衡中起作用。尽管睾酮长期以来一直被提议作为治疗肌肉减少症患者的药物,但由于男性前列腺增生和女性男性化等不良副作用,人们对其产生了担忧。选择性雄激素受体调节剂(SARMs)已被证明具有与睾酮相似的效果,可改善瘦体重(LBM),而对雄激素依赖性组织的副作用较小。

涵盖领域

本综述概述了 SARMs 领域的临床开发进展及其在改善身体成分和身体功能方面的有效性。所纳入的文章均在 pubmed.gov 上收集,并进行了整体分析。

专家意见

对于安全有效的合成代谢化合物(如 SARMs)存在未满足的临床需求。尽管 SARMs 在 II 期临床试验中显示出对 LBM 的影响,但在改善身体功能和肌肉力量方面的结果仍然缺乏,并且需要在这些患者中评估长期结果。此外,需要确定与 SARMs 相关的阻力训练和蛋白质摄入对肌肉减少症患者治疗的影响。

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