University of Copenhagen, Gentofte Hospital, Diabetes Research Division, Department of Internal Medicine F, Hellerup, Denmark.
Expert Opin Investig Drugs. 2011 Apr;20(4):549-57. doi: 10.1517/13543784.2011.562191. Epub 2011 Mar 11.
Type 2 diabetes mellitus (T2DM) is an increasing health problem worldwide. Glucagon-like peptide-1 (GLP-1) receptor agonists are an expanding drug class that target several of the pathophysiological traits of T2DM. Lixisenatide is a GLP-1 receptor agonist in development for once-daily treatment of T2DM.
Pharmacological, preclinical and clinical evidence demonstrating the applicability of lixisenatide for the treatment of T2DM are reviewed. Available data and pending clinical development are summarized, critically appraised and compared to competitor drugs. The most relevant papers and meeting abstracts published up to November 2010 are used as sources for this review.
Efficacy and safety in T2DM are demonstrated with lixisenatide in monotherapy and in combination with metformin. However, limited data with the intended once-daily 20 μg subcutaneous dosing necessitate further evaluation of lixisenatide as add-on to various antidiabetic treatments. It remains to be established whether the slightly differing chemical properties compared to other GLP-1 receptor agonists including a rather short duration of action will be a disadvantage or maybe even an advantage, for example, when combined with long-acting insulin.
2 型糖尿病(T2DM)是全球日益严重的健康问题。胰高血糖素样肽-1(GLP-1)受体激动剂是一种不断发展的药物类别,针对 T2DM 的多种病理生理特征。利西那肽是一种 GLP-1 受体激动剂,正在开发中,用于每日一次治疗 T2DM。
本文综述了证明利西那肽治疗 T2DM 的适用性的药理学、临床前和临床证据。总结了现有数据和正在进行的临床开发情况,并与竞争药物进行了批判性评估和比较。本综述的资料来源于截至 2010 年 11 月发表的最相关的论文和会议摘要。
在 T2DM 的单药治疗和与二甲双胍联合治疗中,利西那肽显示出疗效和安全性。然而,由于每日一次皮下给予 20μg 的预期剂量的数据有限,需要进一步评估利西那肽作为各种抗糖尿病治疗的附加治疗。与其他 GLP-1 受体激动剂相比,其化学性质略有不同,作用持续时间较短,这是否会成为劣势,或者可能成为优势,例如与长效胰岛素联合使用时,仍有待确定。