Iepsen Eva Winning, Torekov Signe Sørensen, Holst Jens Juul
The NNF Center for Basic Metabolic Research and, Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2200 Copenhagen N, Denmark.
Expert Rev Cardiovasc Ther. 2015;13(7):753-67. doi: 10.1586/14779072.2015.1054810.
Subcutaneous liraglutide (Victoza(®), Novo Nordisk) was approved for the treatment of Type 2 diabetes mellitus (T2DM) in Europe in 2009 and in the USA in 2010. In December 2014, liraglutide 3.0 mg was approved by the Food and Drug Administration (FDA) and in March 2015 by the European Medicines Agency (EMA) for the treatment of chronic weight management under the brand name Saxenda(®) Novo Nordisk. Liraglutide causes a glucose-dependent increase in insulin secretion, decreases glucagon secretion and promotes weight loss by inhibiting appetite. Liraglutide probably induces satiety through activation of different areas in the hind brain and possibly by preserving free leptin levels. Recently, liraglutide has been suggested to protect against prediabetes and seems to prevent bone loss by increasing bone formation following diet-induced weight loss in obesity. This article not only covers the major clinical trials evaluating the effects of liraglutide in obesity and T2DM but also provides novel insights into the pharmacological mechanisms of liraglutide.
皮下注射利拉鲁肽(维达列汀,诺和诺德公司)于2009年在欧洲获批用于治疗2型糖尿病(T2DM),并于2010年在美国获批。2014年12月,3.0毫克利拉鲁肽获美国食品药品监督管理局(FDA)批准,2015年3月获欧洲药品管理局(EMA)批准,以司美格鲁肽(诺和诺德公司)为商品名用于慢性体重管理。利拉鲁肽可引起胰岛素分泌呈葡萄糖依赖性增加,减少胰高血糖素分泌,并通过抑制食欲促进体重减轻。利拉鲁肽可能通过激活后脑的不同区域并可能通过维持游离瘦素水平来诱导饱腹感。最近,有人提出利拉鲁肽可预防糖尿病前期,并且在肥胖症患者因饮食诱导体重减轻后,似乎通过增加骨形成来预防骨质流失。本文不仅涵盖了评估利拉鲁肽对肥胖症和T2DM影响的主要临床试验,还提供了有关利拉鲁肽药理机制的新见解。