Bexagliflozin: a comprehensive review of a recently approved SGLT2 inhibitor for the treatment of type 2 diabetes mellitus

Type 2 diabetes mellitus (T2DM) remains a major global health threat, claiming millions of lives annually. Despite recent advancements in managing T2DM, the need for innovative treatment options persists. Sodium-glucose cotransporter 2 (SGLT2) inhibition has proven to be an effective therapeutic strategy against T2DM, offering benefits in lowering hemoglobin A1c (HbA1c) and plasma glucose levels as well as treatment for patients with diabetes who develop chronic kidney disease (CKD). Bexagliflozin is a recently approved, orally administered SGLT2 inhibitor for treating T2DM and exhibits promise in combating CKD stages 3a and 3b. Structurally, bexagliflozin differs from other SGLT2 inhibitors in that it has a cyclopropyloxyethoxy group at the para position of the peripheral phenyl ring. This review article provides an overview of bexagliflozin’s discovery, mechanism of action, binding site interactions, metabolism, pharmacokinetics, and clinical applications. Emphasis is placed on the significant contribution of SGLT2 inhibitors, particularly bexagliflozin in glycemic control and treating associated comorbidities such as heart failure and chronic kidney disease in T2DM patients. (Figure presented.)