Department of Endocrinology and Metabolism, Graduate School of Medicine, Yokohama-City University , Yokohama, Japan.
Expert Opin Pharmacother. 2020 Dec;21(17):2101-2114. doi: 10.1080/14656566.2020.1803280. Epub 2020 Sep 29.
Saxagliptin, a member of the dipeptidyl peptidase-4 inhibitor (DPP-4i) class of drugs, was approved by the FDA for the treatment of type 2 diabetes (T2D) in 2009, and has been in clinical use for more than a decade. Since the drug was first launched, much real-world evidence has also been accumulated. The efficacy and safety of saxagliptin, especially its cardiovascular safety, are of particular interest.
This review provides an overview of the safety and efficacy of saxagliptin based on observational studies, pharmacovigilance, and meta-analyses. In addition, with the findings of recent cardiovascular outcome trials (CVOTs), the authors discuss, herein, the efficacious use of saxagliptin.
Saxagliptin exhibits a moderate glucose-lowering effect and is well tolerated by patients with T2D. SAVOR-TIMI 53, a CVOT of saxagliptin, reported neutral effects of saxagliptin in respect of the cardiovascular outcomes, but did raise a concern about the risk of heart failure. Conversely, recent CVOTs on sodium-glucose co-transporter-2 inhibitors (SGLT2i) have shown a favorably reduced risk of heart failure with these drugs. Also, DPP-4is decrease the serum glucagon level, whereas the SGLT2is increase it. Given the characteristics of the two classes of drugs, combined therapy with the two might be a promising option.
沙格列汀是二肽基肽酶-4 抑制剂(DPP-4i)类药物的一种,于 2009 年被 FDA 批准用于治疗 2 型糖尿病(T2D),并已在临床应用了十余年。自该药物首次推出以来,也积累了大量的真实世界证据。沙格列汀的疗效和安全性,尤其是其心血管安全性,尤其受到关注。
本篇综述基于观察性研究、药物警戒和荟萃分析,概述了沙格列汀的安全性和疗效。此外,结合最近心血管结局试验(CVOT)的结果,作者在此讨论了沙格列汀的有效应用。
沙格列汀具有适度的降糖作用,T2D 患者对其耐受性良好。SAVOR-TIMI 53 是一项沙格列汀的 CVOT,报告显示沙格列汀对心血管结局无影响,但引起了对心力衰竭风险的关注。相反,最近关于钠-葡萄糖共转运蛋白 2 抑制剂(SGLT2i)的 CVOT 表明,这些药物可降低心力衰竭风险。此外,DPP-4i 会降低血清胰高血糖素水平,而 SGLT2i 则会升高。鉴于这两类药物的特点,联合使用这两类药物可能是一个有前途的选择。