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Ertugliflozin for the treatment of type 2 diabetes

机译:Ertugliflozin用于治疗2型糖尿病

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摘要

Sodium/glucose cotransporter 2 (SGLT2) is exclusively expressed in the S1 and S2 segments of proximal convoluted tubules and accounts for similar to 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 similar to 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.
机译:钠/葡萄糖COTRANSPORTER 2(SGLT2)仅在近端复杂小管的S1和S2段中表达,并且占类似葡萄糖重吸收的90%。 Ertugliflozin,一种高选择性和可逆的SGLT2抑制剂,是用于治疗2型糖尿病(T2DM)的SGLT2抑制剂的Gliflozin类别的最新增加。 将于2017年12月获得美国食品和药物管理局(FDA)批准,以治疗T2DM作为单一疗法,以及与SITAGLIPTIN(STEGLUJAN)和二甲双胍(Seglurometer)的两种单独的固定剂量组合疗法的一部分。 耳朱替唑辛显示在单剂量为15mg后的100%生物利用度。 它还具有比目前可用的gliflozins的半衰期(16.6小时),它转化为单每日给药和剂量减少,允许患者遵守。 本综述将专注于临床前药理学,药代动力学,近利石的临床疗效和安全性。

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