Table 4.
Plasma pharmacokinetic parameters of sorafenib
| Dose (mg bid) | day 1 | day 14 | day 28 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| AUC (mg h/L) | AUC0‐12 (mg h/L) | Cmax (mg/L) | Tmax (h) | T1/2 (h) | CL/f (L/h) | AUC0–12 (mg h/L) | Cmax (mg/L) | Ctrough (mg/L) | AUC0–12 (mg h/L) | Cmax (mg/L) | |
| 100 (n = 3) | 9.4 | 3.3 | 0.43 | 4 | 27.1 | 10.6 | 9.4 | 1.04 | 0.70 | 12.3 | 1.42 |
| (39) | (42) | (41) | (3–8) † | (39) | (39) | (21) | (30) | (43) | (27) | (35) | |
| 200 (n = 15) | 24.3 | 5.1 | 0.74 | 4 | 24.4 | 8.2 | 20.2 ‡ | 2.64 ‡ | 1.38 § | 21.1 ¶ | 2.43 †† |
| (100) | (110) | (107) | (3–24) † | (58) | (100) | (37) | (49) | (588) | (49) | (52) | |
| 400 (n = 6) | 35.4 | 7.0 | 1.21 | 8 | 25.5 | 11.3 | 36.7 | 4.91 | 3.75 | n/a | n/a |
| (195) | (173) | (201) | (3–24)† | (40) | (195) | (73) | (76) | (104) | |||
| 600 (n = 7) | 40.5** | 9.7 | 1.41 | 6 | 30.4 ‡‡ | 14.8 ‡‡ | 33.8 ‡‡ | 4.42 ‡‡ | 4.29 ‡‡ | n/a | n/a |
| (67) | (81) | (70) | (4–23) | (34) | (67) | (43) | (55) | (62) | |||
Data are expressed as geometric mean or median, and percent coefficient of variance is expressed in parentheses.
†
range;
‡
n = 10,
§
n = 11,
¶
n = 8,
††
n = 9,
‡‡
n = 6 (Calculated by using the half of lower limit of quantification for one patient with Ctrough lower than the lower limit of quantification)
AUC, area under the curve; n/a, not available.