Knop Filip K, Brønden Andreas, Vilsbøll Tina
a Center for Diabetes Research, Gentofte Hospital , University of Copenhagen , Hellerup , Denmark.
b Department of Clinical Medicine, Faculty of Health and Medical Sciences , University of Copenhagen , Copenhagen , Denmark.
Expert Opin Pharmacother. 2017 Apr;18(6):555-571. doi: 10.1080/14656566.2017.1282463. Epub 2017 Mar 22.
The first-in-class glucagon-like peptide-1 receptor agonist (GLP-1RA) exenatide, which was initially approved in 2005, is available in twice-daily (BID) and once-weekly (QW) formulations. Clinical trial data suggest both formulations are effective and safe for patients with type 2 diabetes (T2D), both as monotherapy and as part of combination therapy. Since exenatide was approved, several other GLP-1RAs have become available for clinical use. Areas covered: Many ongoing clinical trials involving exenatide BID and exenatide QW are investigating new indications (exenatide BID) and new end points and combination therapies (exenatide QW). This review provides an overview of the delivery and pharmacokinetics of both formulations of exenatide, reviews existing data in T2D, and summarizes ongoing investigations. Expert opinion: Exenatide BID and QW have substantial clinical benefits. Comparisons with other GLP-1RAs demonstrate some differences in efficacy and safety profiles that make assessment of benefit:risk ratios complex. Head-to-head comparisons of QW GLP-1RA formulations may assist in the ranking of GLP-1RAs according to efficacy and safety. Results on the impact of exenatide QW on cardiovascular outcomes are eagerly awaited. The potential clinical utility of exenatide BID in other indications will clarify whether exenatide holds clinical promise in diagnoses other than T2D.
首个同类胰高血糖素样肽-1受体激动剂（GLP-1RA）艾塞那肽于2005年首次获批，有每日两次（BID）和每周一次（QW）两种剂型。临床试验数据表明，这两种剂型对2型糖尿病（T2D）患者无论是单药治疗还是作为联合治疗的一部分，均有效且安全。自艾塞那肽获批以来，其他几种GLP-1RA也已可供临床使用。涵盖领域：许多正在进行的涉及艾塞那肽BID和艾塞那肽QW的临床试验正在研究新的适应症（艾塞那肽BID）、新的终点指标和联合治疗方案（艾塞那肽QW）。本综述概述了艾塞那肽两种剂型的给药方式和药代动力学，回顾了T2D的现有数据，并总结了正在进行的研究。专家观点：艾塞那肽BID和QW具有显著的临床益处。与其他GLP-1RA的比较表明，在疗效和安全性方面存在一些差异，这使得对获益-风险比的评估变得复杂。QW GLP-1RA剂型的直接比较可能有助于根据疗效和安全性对GLP-1RA进行排名。人们急切期待艾塞那肽QW对心血管结局影响的结果。艾塞那肽BID在其他适应症中的潜在临床应用将阐明艾塞那肽在T2D以外的诊断中是否具有临床前景。
