Department of Medicine IV, Eberhard Karls University, 72076 Tübingen, Germany.
Drug Saf. 2010 Feb 1;33(2):87-100. doi: 10.2165/11319130-000000000-00000.
Exenatide is the first incretin mimetic, introduced into type 2 diabetes mellitus therapy in 2005, with first approval in the US. It is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used for treatment by twice-daily injection. A long-acting release formulation for once-weekly injection is in clinical development. Clinical studies and postmarketing experience with exenatide have shown a significant and sustained reduction in glycosylated haemoglobin (HbA(1c)) by approximately 1% together with other gylcaemic parameters without an intrinsic risk for hypoglycaemias, and a reduction in bodyweight by 5.3 kg in 82 weeks. Blood pressure and lipids are also favourably affected, but hard cardiovascular endpoints are not yet available. Animal studies show an improvement of beta-cell function and an increase in beta-cell mass after exenatide treatment. The most frequent adverse events associated with exenatide therapy are nausea and antibody formation (both approximately 40%). Nausea, mostly mild and transient, was responsible for a 6% dropout rate in clinical studies. A recent review on the association of acute pancreatitis with exenatide treatment showed no increased risk (relative risk 1.0; 95% CI 0.6, 1.7). This review gives a benefit-risk assessment of exenatide.
艾塞那肽是首个肠促胰岛素类似物，于 2005 年被引入 2 型糖尿病治疗领域，于美国首次获批。它是一种胰高血糖素样肽-1（GLP-1）受体激动剂，可通过每日两次注射进行治疗。一种每周一次注射的长效释放制剂正在临床开发中。艾塞那肽的临床研究和上市后经验表明，其可显著且持续地降低糖化血红蛋白（HbA1c）约 1%，同时改善其他血糖参数，且无低血糖固有风险，并在 82 周时减轻体重 5.3 公斤。血压和血脂也得到了有利影响，但尚无确切的心血管终点事件数据。动物研究显示，艾塞那肽治疗后可改善β细胞功能并增加β细胞量。与艾塞那肽治疗相关的最常见不良事件是恶心和抗体形成（两者均约为 40%）。恶心多为轻度和一过性，导致临床研究中 6%的患者停药。最近一项关于艾塞那肽治疗与急性胰腺炎关联的综述显示，其风险并未增加（相对风险 1.0；95%CI 0.6, 1.7）。本综述对艾塞那肽的获益-风险进行了评估。
