Compound Selectivity for SGLT2 vs. SGLT1 (Fold) UGE in humans at highest dose; mean value ± SDa (g/day) Reduction in HbA1c (%) ASP1941 255 [28] 90.8 ± 16.0 [29] 58.9 ± 14.6 [31] 50 [30] −0.8 [30] BI 10773 >2,500 [32] 72.6 ± 35.9 [33] 88 ± 20.3 [34] 90.8 [35] NR Canagliflozin 414 [36] 129.2 ± 20.8 SE [37] 113 [38] −0.92 [37] Dapagliflozin 1,200 [39] 70 [22] −0.61 to −0.89 [16-19] LX4211 20 [40] 80 [40] −1.25 [40] aSD unless otherwise indicated; SD/SE was not reported in some studies. HbA1c: Hemoglobin A1c; NR: Not Reported; SD: Standard Deviation; SE: Standard Error; UGE: Urinary Glucose Excretion. (Copyright 2011, American Society for Clinical Pharmacology and Therapeutics, Adapted with permission from: M Pfister et al. (2011) Inhibition of SGLT2: A Novel Strategy for Treatment of Type 2 Diabetes Mellitus, Clinical Pharmacology & Therapeutics 89: 4)

Table 1: Pharmacodynamic parameters of SGLT2 inhibitors currently in development.