Canagliflozin is an orally-available, C-aryl glucoside inhibitor of hSGLT2, rSGLT2, and mSGLT2 cells at a potency of 4.4, 3.7, and 2.0 nM, respectively. [1] It inhibits AMG uptake in CHO-hSGLT1 cells with an IC50 of 684 nM. Canagliflozin lowers renal glucose resorptive capacity and increases urinary glucose excretion. Additionally, Canagliflozin has been shown to improve beta-cell function in ZDF rats, reduce body weight, increase fatty acid oxidation, and reduce de novo lipgenesisin rodent models of insulin resistance and Type II diabetes mellitus. [1]

In a twelve week study, Canagliflozin reduces HbA1c slightly more than sitagliptin (-0.21%) in a dose-dependent manner. [2] Reductions in blood pressure have also been observed in similar studies. Canagliflozin was approved by the FDA for the treatment of Type 2 diabetes in January, 2013.