Ertugliflozin: A sodium-glucose cotransporter-2 (SGLT-2) inhibitor for glycemic control in type 2 diabetes

Abstract

Recently, a new class of anti-diabetic drugs has found its way into the market: sodium-glucose cotransporters (SGLT) inhibitors. Two major SGLT isoforms have been identified: SGLT-2, mainly expressed in proximal renal tubules, and SGLT-1, mainly expressed in the small intestine, the proximal renal tubule, and the myocardium. SGLT-2 inhibitors increase urinary glucose excretion, lowering glycemia without inducing excessive insulin secretion. Marketed SGLT-2 inhibitors actually include dapagliflozin, canagliflozin, and empagliflozin; a new SGLT-2 inhibitor is being studied: ertugliflozin. Ertugliflozin is a potent inhibitor of SGLT-2 and possesses a high selectivity over glucose transport via SGLT-1 and several other glucose transporters GLUT-1–4. Ertugliflozin inhibits renal glucose reabsorption resulting in urinary glucose excretion and thereby reduces plasma glucose and glycated hemoglobin in subjects with type 2 diabetes mellitus. Ertugliflozin is being developed as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. The aim of this review is to evaluate the preliminary published data about this new molecule.