a Atherothrombosis Research Unit, Cardiovascular Institute , Icahn School of Medicine at Mount Sinai , New York , NY , USA.
Expert Opin Drug Metab Toxicol. 2018 Dec;14(12):1287-1302. doi: 10.1080/17425255.2018.1551877. Epub 2018 Nov 29.
Type 2 diabetes mellitus (T2DM) is a complex metabolic disorder associated with high cardiovascular (CV) risk. Some of the therapeutic strategies are contraindicated in patients with concomitant heart disease. However, the newest antidiabetic medications, sodium-glucose cotransporter 2 (SGLT2) inhibitors, have shown to significantly reduce CV mortality and heart failure (HF) hospitalizations. The mechanism behind these surprising cardiac benefits remains unclear. Areas covered: This article reviews the pharmacokinetic, pharmacodynamics, efficacy, and safety data for the different SGLT2 inhibitors. Specific attention is devoted to the postulated mechanisms of action for their benefit. The therapeutic efficacy and potential use in different indications outside T2DM such as HF, T1DM, and renal disease are also discussed. Expert opinion: SGLT2 inhibitors have an excellent pharmacokinetic and pharmacodynamic profile. Importantly, SGLT2 inhibitors are a safe and efficacious treatment option for T2DM. Given their cardiac benefits (reduction in HF and death) and the low incidence of adverse events, SGLT2 inhibitors are being currently studied as a treatment for HF also in nondiabetic individuals. These agents seem to represent a shift in the treatment of HF patients regardless their glycemic profile.
2 型糖尿病（T2DM）是一种与心血管（CV）风险升高相关的复杂代谢紊乱。一些治疗策略在伴有心脏病的患者中是禁忌的。然而，最新的抗糖尿病药物，钠-葡萄糖共转运蛋白 2（SGLT2）抑制剂，已显示出可显著降低心血管死亡率和心力衰竭（HF）住院率。这些令人惊讶的心脏益处背后的机制尚不清楚。
本文综述了不同 SGLT2 抑制剂的药代动力学、药效学、疗效和安全性数据。特别关注了它们作用机制的推测。还讨论了它们在 T2DM 以外的不同适应症（如 HF、T1DM 和肾脏疾病）中的治疗效果和潜在用途。
SGLT2 抑制剂具有优异的药代动力学和药效学特性。重要的是，SGLT2 抑制剂是 T2DM 的一种安全有效的治疗选择。鉴于其心脏益处（减少 HF 和死亡）和不良事件发生率低，SGLT2 抑制剂目前正在作为非糖尿病个体的 HF 治疗方法进行研究。无论患者的血糖水平如何，这些药物似乎都代表了 HF 患者治疗方式的转变。
