Albiglutide: A once-weekly glucagon-like peptide-1 receptor agonist for type 2 diabetes mellitus.
Albiglutide: A once-weekly glucagon-like peptide-1 receptor agonist for type 2 diabetes mellitus.
复制标题
DOI：
10.2146/ajhp140260
复制
发表时间：
2015-07
期刊：
影响因子：
--
通讯作者：
P. Davis;U. Ndefo;A. Oliver;E. Payton
中科院分区：
文献类型：
--
作者：
P. Davis;U. Ndefo;A. Oliver;E. Payton
目的综述胰高血糖素样肽-1（GLP-1）受体激动剂阿必鲁肽的药理学、药代动力学、有效性、安全性、给药剂量和治疗地位。阿必鲁肽（Tanzeum，GlaxoSmithKline）是一种可注射的GLP-1激动剂，于2014年批准用作饮食调整和运动的辅助药物，以改善2型糖尿病成人的血糖控制。阿必鲁肽增加葡萄糖依赖性胰岛素分泌并减缓胃排空;其消除半衰期约为5天，允许每周给药一次。临床试验表明，阿必鲁肽连续治疗16周后，糖化血红蛋白（HbA 1c）值平均绝对降低0.78-1.55%。美国临床内分泌学家协会（AACE）和美国糖尿病协会（ADA）已经发布了关于阿必鲁肽使用的具体建议。研究表明，使用阿必鲁肽发生低血糖发作的可能性较低。在临床试验中，最常报告的不良事件是恶心和腹泻。有胰腺炎病史和有甲状腺癌个人或家族史的患者禁用阿必鲁肽。结论阿必鲁肽已被证明可有效治疗成人2型糖尿病，并被ADA推荐作为与二甲双胍联合使用的二线治疗，被AACE推荐作为治疗开始时HbA 1c浓度≤7.5%的患者的一线单药治疗。在临床试验中，患者对阿必鲁肽的耐受性通常良好，不良反应与其他GLP-1激动剂相当。
PURPOSE The pharmacology, pharmacokinetics, efficacy, safety, dosage and administration, and place in therapy of the glucagon-like peptide-1 (GLP-1) receptor agonist albiglutide are reviewed. SUMMARY Albiglutide (Tanzeum, GlaxoSmithKline) is an injectable GLP-1 agonist approved in 2014 for use as an adjunct to diet modification and exercise to improve glycemic control in adults with type 2 diabetes. Albiglutide augments glucose-dependent insulin secretion and slows gastric emptying; it has an elimination half-life of approximately five days, allowing for once-weekly administration. Clinical trials demonstrated mean absolute reductions in glycosylated hemoglobin (HbA1c) values of 0.78-1.55% after 16 weeks of adjunctive therapy with albiglutide. Specific recommendations on albiglutide use have been issued by the American Association of Clinical Endocrinologists (AACE) and the American Diabetes Association (ADA). Studies show that the potential for hypoglycemic episodes with albiglutide use is low. In clinical trials, the most frequently reported adverse events were nausea and diarrhea. The use of albiglutide is contraindicated in patients with a history of pancreatitis and patients with a personal or family history of thyroid cancer. CONCLUSION Albiglutide has been shown to be effective for the management of type 2 diabetes in adults and is recommended (by ADA) as second-line therapy when used in combination with metformin and (by AACE) as first-line monotherapy in patients with an HbA1c concentration of ≤7.5% at treatment initiation. In clinical trials, albiglutide was generally well tolerated by patients, with adverse effects comparable to those seen with other GLP-1 agonists.