Tofogliflozin: a highly selective SGLT2 inhibitor for the treatment of type 2 diabetes.

Abstract

Diabetes mellitus impacts a substantial number of people worldwide and despite numerous antidiabetic medications available, approximately half of the drugs do not attain their recommended target, glycated hemoglobin (HbA1c). Recently, the kidney and its role in glucose reabsorption through the sodium/glucose cotransporter 2 (SGLT2) has been the target for novel antidiabetic treatments. Pharmacologic inhibition of SGLT2 in patients with diabetes results in increased urinary glucose excretion and decreased blood glucose levels, decreasing HbA1c levels. Tofogliflozin is the most selective SGLT2 inhibitor, with HbA1c reductions ranging from -0.44% to -0.99% throughout clinical studies, and it is well tolerated with a low rate of drug-related adverse events. Tofogliflozin has demonstrated efficacy and safety as monotherapy or as add-on to various antidiabetic agents, and it is currently undergoing phase IV clinical studies in Japanese patients with diabetes on background insulin therapy. Tofogliflozin is currently approved in Japan for use in patients with type 2 diabetes at a dose of 20 mg orally once daily in the morning, either before or after breakfast.