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.
Keywords: Endocrine disorders; Ertugliflozin; SGLT2 inhibitors; Type 2 diabetes.
Copyright 2019 Clarivate Analytics.