Table 1.
SGLTi | Human SGLT1 (IC50 nM) | Human SGLT2 (IC50 nM) | Protein Binding (%) |
t1/2 (h) |
F (%) |
fe (%) |
Refs. |
---|---|---|---|---|---|---|---|
canagliflozin | 684 | 4.4 | 98 | 11–13 | 65 | <1% | [4,5] |
dapagliflozin | 803 | 1.6 | 91 | 12.2 | 78 | <2% | [4] |
empagliflozin | 8300 | 3.1 | 86 | 11.4–12.4 | 60–78 | 11–29 | [4,6,7,8] |
ertugliflozin | 1960 | 0.9 | 94 | 11–18 | 100 | 1.5% | [9,10] |
ipragliflozin | 2329 | 8.9 | 96 | 10–13 | 90 | <1% | [4,11,12] |
tofogliflozin | 8444 | 2.9 | 83 | 6.8 | 97.5 | 76% | [4,13] |
Abbreviations: t1/2—terminal half-life in plasma; F—bioavailability; fe—fraction of dose that was excreted unchanged in urine; IC50—half maximal inhibitory concentration.