Dapagliflozin (BMS-512148) is an orally-available C-aryl glucoside diphenylmethanol inhibitor of SGLT2 (IC50 1.1 nM) for the treatment of Type 1 and Type 2 diabetes. It is the first approved SGLT2 inhibitor (European Union as Forxiga) for the treatment of diabetes. Its excellent selectivity over SGLT1 (IC50 1390 nM) ensures that it does not interfere with intestinal glucose absorption. Dapagliflozin minimally inhibits glucose transporters GLUT1 and GLUT2 and modestly inhibits GLUT4. [1]

Dapagliflozin removes excess glucose and its associated calories in urine, which in turn reduces blood sugar levels. Clinical studies have shown concurrent reductions in weight and blood pressure. [2] In combination with metformin, the weight loss was statistically significant, dose-dependent, and persisted for over two years. [3]