Investigational Agents Targeting SGLT1 and SGLT2 in the Treatment of Type 2 Diabetes Mellitus

Targeting sodium-dependent glucose transporters (SGLT1 and SGLT2) represents a new class of pharmacotherapy for type 2 diabetes mellitus, a major global health issue with an increasing social and economic burden. Following recent successes in market approvals of SGLT2 inhibitors, the ongoing effort has paved the way for the discovery of novel agents via structure-activity relationship studies, preclinical and clinical testing, including SGLT2 inhibitors, SGLT1/2 dual inhibitors, and selective SGLT1 inhibitors. A growing understanding of the physiology of SGLTs allows drug developers to explore additional cardiovascular and renal protective benefits of these agents in T2DM patients at risk. This review provides an overview of the recent investigational compounds and discusses future perspectives of drug discovery in this area.