Table 3.
Pharmacokinetic characteristics of sodium–glucose cotransporter 2 inhibitors.
| Parameters | SGLT-2 Inhibitors | |||||
|---|---|---|---|---|---|---|
| Dapagliphlozin | Canagliphlozin | Empagliphlozin | Ipragliphlozin | Luseogliphlozin | Tofogliphlozin | |
| Molecular Weight [kDa] | 408.9 | 444.5 | 450.9 | 404.5 | 434.5 | 386.4 |
| Cmax | 2465 nmol/L for the 100 mg dose 7828 nmol/L for the 300 mg dose |
2465 nmol/L for the 100 mg dose 7828 nmol/L for the 300 mg dose |
259 nmol/L for the 10 mg dosxe 687 nmol/L for the 25 mg dose |
1277 ± 360a | NA | NA |
| The volume of distribution [L] | 118 | 119 | 74 | NA | 39 | 50 |
| Tmax [h] | 1.5 | 1.5 | 1 | 1.5 | 1.5 | 0.75 |
| Bioavailability [%] | 78% | 65% | 86% | 90.2% | NA | 97.5 |
| Ability to cross the BBB | YES | YES | YES | YES | YES | YES |
| Half-life | 12.9 h | 10.6 h for the 100 mg dose 13.1 h for the 300 mg dose |
12.4 h | 14.97 h | NA | NA |
| The primary route of elimination | feces/urine | |||||
| References | [210,211,212,213,214] | [120,210,214] | [210,211,214] | [210,214,215,216] | [210,214,217] | [210,214,218,219,220] |
Explanation of abbreviations: Cmax, maximum plasma concentration; Tmax, time to reach maximum concentration; NA, not available.