Table 3.
Pharmacokinetic Parameters After a Single Dose of Efatutazone, Cycle 1 and Cycle 2
| Cycle | Efatutazone Dose Level, mg | ||||||
|---|---|---|---|---|---|---|---|
| 0.10 | 0.15 | 0.25 | 0.35 | 0.50 | 0.75 | 1.15 | |
| Cycle 1 | |||||||
| AUC0-t, ng/h/mL | 23.05 ±6.108(6) | 32.05 ± 7.753 (3) | 68.33 ±24.613(6) | 59.72 ± 32.582 (3) | 159.2 ±45.10(6) | 159.14 ± 126.314(3) | 256.3 ± 93.31 (4) |
| AUC0–12, ng/h/mL | 32.96 ± 6.904 (6) | 44.14 ± 12.152 (3) | 91.24 ±36.157(6) | 80.80 ± 40.739 (3) | 220.9 ± 74.42 (6) | 214.38 ± 163.811 (3) | 356.8 ± 127.69 (4) |
| Cmax, ng/mL | 4.213 ±0.9253(6) | 5.763 ± 1.5282 (3) | 12.193 ±3.0014(6) | 12.263 ±7.0980(3) | 26.92 ± 6.358 (6) | 27.637 ±21.4373(3) | 44.73 ± 15.050 (4) |
| aTmax, h | 3.000 [2.00–6.00] (6) | 2.000 [1.00–2.00] (3) | 1.584 [1.00–4.00] (6) | 3.000 [1.00–3.00] (3) | 2.000 [1.00–4.00] (6) | 3.000 [2.00–4.00] (3) | 2.500 [2.00–4.00] (4) |
| t1/2, h | 8.509 ±3.9178(5) | 13.782 ±6.9182 (3) | 11.481 ± 11.2970 (6) | 12.486 ±7.3517(2) | 5.743 ± 2.5637 (5) | 9.078 ± 2.7871 (3) | 11.659 ± 3.4494 (4) |
| Cycle 2 | |||||||
| AUC0-t, ng/h/mL | 44.03 ± 18.820(5) | 61.19 ±27.945 (3) | 88.64 ±25.019(5) | 81.09 ±23.117(3) | 289.9 ± 140.06(3) | 363.2 ± 105.39(3) | 342.3 ± 189.48 (4) |
| AUCtau, ng/h/mL | 61.14 ±24.901 (5) | 83.35 ± 42.444 (3) | 123.75 ±40.124(5) | 114.88 ±21.714(3) | 406.5 ± 195.76(3) | 526.8 ± 133.42 (3) | 525.9 ± 300.09 (4) |
| Cmax,ss, ng/mL | 6.878 ± 2.9560 (5) | 10.173 ±3.5419(3) | 15.30 ±4.491 (5) | 14.20 ±3.601 (3) | 44.07 ± 23.343 (3) | 57.03 ± 14.451 (3) | 58.33 ±30.173(4) |
| aTmax, h | 2.000 [0.917–3.00] (5) | 2.000 [1.00–3.00] (3) | 3.000 [2.00–4.00] (5) | 2.000 [2.00–3.00] (3) | 2.000 [2.00–4.00] (3) | 2.000 [2.00–3.00] (3) | 3.000 [3.00–3.00] (4) |
| t1/2, h | 11.631 ± 4.5931 (5) | 14.047 ± 14.7104(3) | 6.344 ± 1.9370 (4) | 7.560 ± 3.4744 (3) | 5.150(1) | 9.656 ± 2.4826 (3) | 12.58 ±0.276(2) |
| bAcc | 1.808 ± 0.4098 (5) | 1.825 ± 0.4439 (3) | 1.722 ± 0.8371 (5) | 1.613 ±0.5924(3) | 1.531 ±0.1826(3) | 6.452 ± 7.8442 (3) | 1.4981 ± 0.57875 (4) |
Abbreviations: AUC, area under the concentration versus time curve; Cmax, maximum plasma concentration; max, ss, maximum plasma concentration, steady state; Tmax, time of maximum plasma concentration; t1/2, plasma half-life.
Values are mean ± standard deviation (No.) or [range].
a
Tmax is presented as median [range] (No.).
b
Acc = AUC0-tau/AUC0–12.