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[抗肥胖药物:从以往的失望到新的希望]

[Anti-obesity drugs : from previous disappointments to new hopes].

作者信息

Scheen André, De Flines Jenny, Paquot Nicolas

机构信息

Service de Diabétologie, Nutrition et Maladies métaboliques, Département de Médecine, CHU Liège, Belgique.

出版信息

Rev Med Liege. 2023 Mar;78(3):147-152.

PMID:36924152
Abstract

Both physicians and patients dream of an efficacious and safe pharmacological approach to treat obesity. Unfortunately, most anti-obesity drugs prescribed since the fifties were associated with an unfavourable risk profile that led to numerous withdrawals. Medications issued from pharmaco-chemistry that mainly target brain amines to reduce appetite have been abandoned because of potential cardiovascular and neuropsychiatric toxicities. More recently, biological medications emerged, especially GLP-1 (Glucagon-Like Peptide-1) receptor agonists, well-known to manage type 2 diabetes and now recommended at higher doses for the treatment of obesity (liraglutide, semaglutide). A dual agonist that targets both GLP-1 and GIP (Glucose-dependent Insulinotropic Polypeptide) receptors (tirzepatide) appears to be even more potent as glucose-lowering agent and is currently tested as an anti-obesity agent. Many other pharmacological approaches are currently investigated but they should not mask the importance of life-style measurements.

摘要

医生和患者都梦想有一种有效且安全的药物治疗方法来治疗肥胖症。不幸的是,自五十年代以来开出的大多数抗肥胖药物都具有不良的风险特征,导致许多药物被撤市。主要针对脑胺以降低食欲的药物化学药物,由于潜在的心血管和神经精神毒性而被淘汰。最近,生物药物出现了,尤其是胰高血糖素样肽-1(GLP-1)受体激动剂,它以治疗2型糖尿病而闻名,现在推荐以更高剂量用于治疗肥胖症(利拉鲁肽、司美格鲁肽)。一种同时靶向GLP-1和葡萄糖依赖性促胰岛素多肽(GIP)受体的双重激动剂(替尔泊肽)似乎作为降糖剂更有效,目前正在作为抗肥胖剂进行测试。目前正在研究许多其他药物治疗方法,但它们不应掩盖生活方式干预的重要性。

相似文献

1
[Anti-obesity drugs : from previous disappointments to new hopes].[抗肥胖药物:从以往的失望到新的希望]
Rev Med Liege. 2023 Mar;78(3):147-152.
2
[A new era for glucagon-like peptide-1 receptor agonists].胰高血糖素样肽-1受体激动剂的新时代
Rev Med Liege. 2023 Jan;78(1):40-45.
3
The dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist tirzepatide: a novel cardiometabolic therapeutic prospect.双重葡萄糖依赖性胰岛素促胰岛素多肽(GIP)和胰高血糖素样肽-1(GLP-1)受体激动剂替西帕肽:一种新的代谢治疗前景。
Cardiovasc Diabetol. 2021 Nov 24;20(1):225. doi: 10.1186/s12933-021-01412-5.
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Glucagon-Like Peptide-1 Receptor Agonists and Dual Glucose-Dependent Insulinotropic Polypeptide/Glucagon-Like Peptide-1 Receptor Agonists in the Treatment of Obesity/Metabolic Syndrome, Prediabetes/Diabetes and Non-Alcoholic Fatty Liver Disease-Current Evidence.胰高血糖素样肽-1受体激动剂及双重葡萄糖依赖性促胰岛素多肽/胰高血糖素样肽-1受体激动剂在肥胖/代谢综合征、糖尿病前期/糖尿病及非酒精性脂肪性肝病治疗中的应用——当前证据
J Cardiovasc Pharmacol Ther. 2022 Jan-Dec;27:10742484221146371. doi: 10.1177/10742484221146371.
5
Dual-agonist incretin peptides from fish with potential for obesity-related Type 2 diabetes therapy - A review.鱼源双重激动剂肠降血糖素肽在肥胖相关性 2 型糖尿病治疗中的应用-综述。
Peptides. 2022 Jan;147:170706. doi: 10.1016/j.peptides.2021.170706. Epub 2021 Nov 30.
6
An update on peptide-based therapies for type 2 diabetes and obesity.关于 2 型糖尿病和肥胖症的基于肽的治疗方法的最新进展。
Peptides. 2023 Mar;161:170939. doi: 10.1016/j.peptides.2023.170939. Epub 2023 Jan 3.
7
Efficacy and safety of high-dose glucagon-like peptide-1, glucagon-like peptide-1/glucose-dependent insulinotropic peptide, and glucagon-like peptide-1/glucagon receptor agonists in type 2 diabetes.高剂量胰高血糖素样肽-1、胰高血糖素样肽-1/葡萄糖依赖性胰岛素释放肽和胰高血糖素样肽-1/胰高血糖素受体激动剂在 2 型糖尿病中的疗效和安全性。
Diabetes Obes Metab. 2022 May;24(5):788-805. doi: 10.1111/dom.14640. Epub 2022 Jan 21.
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A novel GIP analogue, ZP4165, enhances glucagon-like peptide-1-induced body weight loss and improves glycaemic control in rodents.一种新型的 GIP 类似物,ZP4165,可增强胰高血糖素样肽-1 诱导的体重减轻,并改善啮齿动物的血糖控制。
Diabetes Obes Metab. 2018 Jan;20(1):60-68. doi: 10.1111/dom.13034. Epub 2017 Jul 27.
9
GLP-1 Agonist to Treat Obesity and Prevent Cardiovascular Disease: What Have We Achieved so Far?GLP-1 激动剂治疗肥胖和预防心血管疾病:我们目前取得了哪些进展?
Curr Atheroscler Rep. 2022 Nov;24(11):867-884. doi: 10.1007/s11883-022-01062-2. Epub 2022 Aug 31.
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Dual GIP/GLP-1 receptor agonists: New advances for treating type-2 diabetes.双重 GIP/GLP-1 受体激动剂:治疗 2 型糖尿病的新进展。
Ann Endocrinol (Paris). 2023 Apr;84(2):316-321. doi: 10.1016/j.ando.2022.12.423. Epub 2023 Jan 10.

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