Table 2

Pharmacokinetic parameters of afuresertib

Dose (mg)No. of patientsCmax (ng/mL)AUC0-24 (ng•h/mL)Accumulation ratioC0 (ng/mL)
Single doseRepeat doseSingle doseRepeat doseSingle doseRepeat doseDay 8Day 15
25 26.5, 39.7 57.3, 79.8 294, 413 891, 1393 — 3.0, 3.4 30.5, 36.7 42.3, 48.0 
75 101, 112 244, 252 1003, 1139 3022, 3193 — 3.2, 2.7 93.8, 155 96.9, 131 
100 244 ± 158 554 ± 198 2366 ± 992 6782 ± 2004 — 3.3 ± 1.6 249 ± 107 261 ± 162 
125 175 ± 82.7 531 ± 288 2378 ± 1004 7405 ± 3584 — 2.9 ± 0.7 259 ± 105 342 ± 172 
150 350 ± 162 949 ± 348 4379 ± 1288 13425 ± 3953 — 3.0 ± 1.3 624 ± 345 822 ± 576 
Dose (mg)No. of patientsCmax (ng/mL)AUC0-24 (ng•h/mL)Accumulation ratioC0 (ng/mL)
Single doseRepeat doseSingle doseRepeat doseSingle doseRepeat doseDay 8Day 15
25 26.5, 39.7 57.3, 79.8 294, 413 891, 1393 — 3.0, 3.4 30.5, 36.7 42.3, 48.0 
75 101, 112 244, 252 1003, 1139 3022, 3193 — 3.2, 2.7 93.8, 155 96.9, 131 
100 244 ± 158 554 ± 198 2366 ± 992 6782 ± 2004 — 3.3 ± 1.6 249 ± 107 261 ± 162 
125 175 ± 82.7 531 ± 288 2378 ± 1004 7405 ± 3584 — 2.9 ± 0.7 259 ± 105 342 ± 172 
150 350 ± 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.