Bimagrumab:一种用于治疗肥胖症的针对活化素 II 型受体的在研人类单克隆抗体。

Q3 Pharmacology, Toxicology and Pharmaceutics
Manmeet Kaur, Saurav Misra
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引用次数: 0

摘要

Bimagrumab 是一种人类单克隆抗体,可阻止激活素 II 型受体(ActRII)发挥作用。这种抗体对肌肉活化素-2受体的亲和力高于活化素和肌节蛋白等天然配体,而后者是肌肉生长的负调节剂。用比马格鲁单抗阻断激活素受体可能是控制肥胖症和2型糖尿病(T2DM)患者的一种新的药物治疗方法。Bimagrumab 可阻止肌节蛋白结合和其他肌肉生长负调控因子,从而对骨骼肌质量产生同化作用。临床前动物模型还显示,ActRII 阻断作用可促进骨骼肌以外的作用,包括对棕色脂肪组织(BAT)分化和活性的影响。在一项 2 期随机临床试验中,使用 bimagrumab 阻断 ActRII 可使超重或肥胖的 2 型糖尿病患者在 48 周内显著减少全身脂肪量(FM)、增加瘦肉量(LM)并改善代谢。试验涉及[参与者人数],结果显示[具体发现]。目前,正在对 Bimagrumab 治疗肌肉萎缩、髋部骨折功能丧失、肌肉疏松症以及肥胖症的潜力进行评估。但必须指出的是,Bimagrumab 还能阻断其他 ActRII 配体的作用,这些配体在神经激素轴、垂体、性腺和肾上腺中发挥作用。这些观察结果表明,比马格鲁单抗可能是治疗肥胖症和相关代谢紊乱患者的一种新方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Bimagrumab: an investigational human monoclonal antibody against activin type II receptors for treating obesity.

Bimagrumab is a human monoclonal antibody that prevents activin type II receptors (ActRII) from functioning. This antibody has a higher affinity for muscle activin-2 receptors than natural ligands such as activin and myostatin, which act as negative muscle growth regulators. Blocking the activin receptor with bimagrumab could be a new pharmaceutical approach for managing patients with obesity and type 2 diabetes mellitus (T2DM). Bimagrumab has anabolic effects on skeletal muscle mass by preventing myostatin binding and other negative muscle growth regulators. Preclinical animal models have also shown that ActRII blockade promotes actions beyond skeletal muscle, including effects on brown adipose tissue (BAT) differentiation and activity. In a phase 2 randomized clinical trial, ActRII blockade with bimagrumab led to significant loss of total body fat mass (FM), lean mass (LM) gain, and metabolic improvements over 48 weeks in overweight or obese patients with type 2 diabetes. The trial involved [number of participants], and the results showed [specific findings]. Currently, Bimagrumab is being evaluated for its potential to treat muscle wasting, functional loss in hip fractures and sarcopenia, as well as obesity. However, it is essential to note that Bimagrumab also blocks the effects of other ActRII ligands, which play a role in the neurohormonal axes, pituitary, gonads, and adrenal glands. These observations suggest that bimagrumab might represent a new approach for treating patients with obesity and related metabolic disturbances.

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来源期刊
Journal of Basic and Clinical Physiology and Pharmacology
Journal of Basic and Clinical Physiology and Pharmacology Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
3.90
自引率
0.00%
发文量
53
期刊介绍: The Journal of Basic and Clinical Physiology and Pharmacology (JBCPP) is a peer-reviewed bi-monthly published journal in experimental medicine. JBCPP publishes novel research in the physiological and pharmacological sciences, including brain research; cardiovascular-pulmonary interactions; exercise; thermal control; haematology; immune response; inflammation; metabolism; oxidative stress; and phytotherapy. As the borders between physiology, pharmacology and biochemistry become increasingly blurred, we also welcome papers using cutting-edge techniques in cellular and/or molecular biology to link descriptive or behavioral studies with cellular and molecular mechanisms underlying the integrative processes. Topics: Behavior and Neuroprotection, Reproduction, Genotoxicity and Cytotoxicity, Vascular Conditions, Cardiovascular Function, Cardiovascular-Pulmonary Interactions, Oxidative Stress, Metabolism, Immune Response, Hematological Profile, Inflammation, Infection, Phytotherapy.
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