Table 2.
Pharmacokinetic parameters of afuresertib
| Dose (mg) | No. of patients | Cmax (ng/mL) | AUC0-24 (ng•h/mL) | Accumulation ratio | C0 (ng/mL) | ||||
|---|---|---|---|---|---|---|---|---|---|
| Single dose | Repeat dose | Single dose | Repeat dose | Single dose | Repeat dose | Day 8 | Day 15 | ||
| 25 | 2 | 26.5, 39.7 | 57.3, 79.8 | 294, 413 | 891, 1393 | — | 3.0, 3.4 | 30.5, 36.7 | 42.3, 48.0 |
| 75 | 2 | 101, 112 | 244, 252 | 1003, 1139 | 3022, 3193 | — | 3.2, 2.7 | 93.8, 155 | 96.9, 131 |
| 100 | 8 | 244 ± 158 | 554 ± 198 | 2366 ± 992 | 6782 ± 2004 | — | 3.3 ± 1.6 | 249 ± 107 | 261 ± 162 |
| 125 | 8 | 175 ± 82.7 | 531 ± 288 | 2378 ± 1004 | 7405 ± 3584 | — | 2.9 ± 0.7 | 259 ± 105 | 342 ± 172 |
| 150 | 6 | 350 ± 162 | 949 ± 348 | 4379 ± 1288 | 13425 ± 3953 | — | 3.0 ± 1.3 | 624 ± 345 | 822 ± 576 |
Single- and repeat-dose data are presented as mean ± standard deviation except for 25- and 75-mg doses, which are presented as individual values; the number of patients with repeat doses is the same as that for single dose, except for 125 mg (n = 6) and 150 mg (n = 5).
AUC0-24, area under the plasma concentration-time curve from time 0 to 24 hours; Cmax, maximum plasma concentration; C0, predose concentration on day 8 and day 15.