Sharma R, Razdan K, Kuhad A, Kuhad A
Pharmacology Research Laboratory, University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Study, Panjab University, Chandigarh, India.
Pharmaceutics Division, University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Study, Panjab University, Chandigarh, India.
Drugs Today (Barc). 2019 Mar;55(3):167-175. doi: 10.1358/dot.2019.55.3.2904972.
Sodium/glucose cotransporter 2 (SGLT2) is exclusively expressed in the S1 and S2 segments of proximal convoluted tubules and accounts for roughly 90% of glucose reabsorption. Ertugliflozin, a highly selective and reversible SGLT2 inhibitor, is the latest addition to the gliflozin class of SGLT2 inhibitors for the treatment of type 2 diabetes mellitus (T2DM). It was granted approval by the U.S. Food and Drug Administration (FDA) in December 2017 for treatment of T2DM as a monotherapy, and as part of two separate fixed-dose combination therapies with sitagliptin (Steglujan) and metformin (Segluromet). Ertugliflozin demonstrated roughly 100% bioavailability following a single dose of 15 mg. It also has a longer half-life (16.6 hours) than presently available gliflozins, which translates into single daily dosing and dose reduction allowing for patient compliance. This review will focus on the preclinical pharmacology, pharmacokinetics, clinical efficacy and safety of ertugliflozin.
钠-葡萄糖协同转运蛋白2（SGLT2）仅在近端曲管的S1和S2节段中表达，约占葡萄糖重吸收的90%。依格列净是一种高度选择性和可逆性的SGLT2抑制剂，是格列净类SGLT2抑制剂中最新用于治疗2型糖尿病（T2DM）的药物。2017年12月，它获得了美国食品药品监督管理局（FDA）的批准，可作为单一疗法治疗T2DM，也可作为与西格列汀（Steglujan）和二甲双胍（Segluromet）两种单独的固定剂量联合疗法的一部分。单剂量15 mg后，依格列净的生物利用度约为100%。它的半衰期（16.6小时）也比目前可用的格列净更长，这意味着每日只需给药一次且剂量减少，从而提高了患者的依从性。本综述将重点关注依格列净的临床前药理学、药代动力学、临床疗效和安全性。
