Table 2.
Pharmacokinetic parameters of luseogliflozin and its major metabolite (M2) after single (Day 1) and multiple (Day 7) doses of luseogliflozin
| Dose | Day | C max (ng/mL) | t max (h) | AUC (ng h/mL)a | AUC ratiob | t 1/2 (h) | Ae0–24 (% of dose) |
|---|---|---|---|---|---|---|---|
| Luseogliflozin | |||||||
| 0.5 mg (N = 7) | Day 1 | 21.9 ± 2.88 | 0.857 ± 0.556 | 171 ± 38.4 | – | 9.86 ± 1.57 | 3.76 ± 0.832 |
| Day 7 | 25.6 ± 4.25 | 0.643 ± 0.244 | 179 ± 32.6 | – | 10.5 ± 1.03 | 4.56 ± 1.04 | |
| 1 mg (N = 8) | Day 1 | 43.7 ± 10.8 | 0.688 ± 0.259 | 357 ± 53.9 | – | 9.61 ± 1.34 | 4.06 ± 0.497 |
| Day 7 | 52.3 ± 10.9 | 0.688 ± 0.259 | 370 ± 55.5 | – | 10.0 ± 1.37 | 4.30 ± 0.875 | |
| 2.5 mg (N = 8) | Day 1 | 119 ± 27.0 | 0.625 ± 0.354 | 864 ± 132 | – | 9.24 ± 0.928 | 4.51 ± 1.13 |
| Day 7 | 136 ± 42.0 | 1.00 ± 0.886 | 899 ± 148 | – | 9.20 ± 0.710 | 4.79 ± 1.09 | |
| 5 mg (N = 8) | Day 1 | 243 ± 45.7 | 0.625 ± 0.231 | 1690 ± 271 | – | 8.96 ± 1.11 | 4.11 ± 0.763 |
| Day 7 | 299 ± 50.3 | 0.688 ± 0.259 | 1880 ± 318 | – | 9.54 ± 1.26 | 4.56 ± 0.617 | |
| M2 | |||||||
| 0.5 mg (N = 7) | Day 1 | 0.726 ± 0.136 | 4.71 ± 3.04 | 28.6 ± 6.17 | – | 24.7 ± 8.12 | 5.22 ± 0.848 |
| Day 7 | 1.30 ± 0.196 | 2.07 ± 0.932 | 22.8 ± 3.03 | 0.138 ± 0.0172 | 18.6 ± 2.45 | 10.4 ± 1.65 | |
| 1 mg (N = 8) | Day 1 | 1.61 ± 0.383 | 4.75 ± 1.83 | 62.7 ± 10.5 | – | 24.0 ± 8.91 | 5.86 ± 0.674 |
| Day 7 | 2.95 ± 0.522 | 2.44 ± 1.32 | 50.4 ± 7.62 | 0.147 ± 0.0229 | 17.6 ± 4.28 | 11.1 ± 1.27 | |
| 2.5 mg (N = 8) | Day 1 | 4.13 ± 0.554 | 3.31 ± 2.53 | 140 ± 31.3 | – | 20.2 ± 4.39 | 6.72 ± 0.749 |
| Day 7 | 6.64 ± 0.776 | 2.75 ± 1.13 | 116 ± 15.3 | 0.140 ± 0.0244 | 16.6 ± 2.42 | 11.2 ± 2.13 | |
| 5 mg (N = 7) | Day 1 | 8.90 ± 1.22 | 5.86 ± 3.08 | 306 ± 63.8 | – | 19.5 ± 4.41 | 6.70 ± 1.18 |
| Day 7 | 15.3 ± 2.37 | 2.00 ± 1.12 | 259 ± 50.8 | 0.148 ± 0.0136 | 19.3 ± 3.63 | 11.6 ± 2.49 | |
Values are presented as the mean ± standard deviation
Ae 0–24 amount of unchanged drug excreted in urine from 0 to 24 h, AUC inf area under the plasma concentration–time curve extrapolated to infinity, AUC τ area under the plasma concentration–time curve during the dosing interval, C max maximum plasma concentration, M2 active metabolite of luseogliflozin (O-deethyl form), t max time to the maximum plasma concentration, t 1/2 elimination half-life
aDay 1: AUCinf, Day7: AUCτ
bCalculated as AUCτ (M2)/AUCτ (luseogliflozin)