Table 5.
Plasma pharmacokinetic parameters of metabolites
| Dose (mg bid) | M‐2 (BAY 67‐3472) | M‐4 (BAY 43‐9007) | M‐5 (BAY 68‐7769) | ||||||
|---|---|---|---|---|---|---|---|---|---|
| AUC0–12 (mg h/L) | Ratio (%) | Cmax (mg/L) | AUC0–12 (mg h/L) | Ratio (%) | Cmax (mg/L) | AUC0–12 (mg h/L) | Ratio (%) | Cmax (mg/L) | |
| 100 (n = 3) | 0.63 | 6.07 | 0.07 | 0.16 | 1.54 | 0.02 | 0.21 † | 2.04 † | 0.02 † |
| (57) | (74) | (45) | (40) | (25) | (23) | (54) | (78) | (71) | |
| 200 (n = 10) | 2.47 | 10.01 | 0.31 | 0.70 | 2.83 | 0.11 | 0.83 ‡ | 3.13 ‡ | 0.10 ‡ |
| (79) | (55) | (71) | (179) | (124) | (95) | (50) | (63) | (55) | |
| 400 (n = 6) | 5.84 | 11.7 | 0.73 | 1.89 | 3.81 | 0.24 | 1.79 | 3.60 | 0.22 |
| (269) | (63) | (285) | (324) | (81) | (353) | (563) | (144) | (573) | |
| 600 (n = 6) | 5.44 | 12.2 | 0.66 | 1.81 | 4.09 | 0.23 | 1.48 | 3.34 | 0.18 |
| (140) | (58) | (150) | (139) | (61) | (153) | (185) | (84) | (205) | |
Data are expressed as geometric mean, and percent coefficient of variance is expressed in parentheses.
Ratio of each metabolite to the sum of AUC0–12 of sorafenib, M‐2, M‐4, and M‐5.
†
n = 2;
‡
n = 9.
AUC, area under the curve.