Table 2.
Pharmacokinetic parameters of regorafenib in plasma and total radioactivity in plasma and whole blood after oral administration of a single oral dose of 120 mg [14C]regorafenib solution (N = 4)
| Parameter geometric mean (%CV) | Total radioactivity | Regorafenib | |
|---|---|---|---|
| Plasma | Whole blood | ||
| AUCa | 84.2 (47) | 56.0 (39) | 39.0 (34.9) |
| C max a | 2.90 (31) | 1.95 (19) | 1.58 (36.2) |
| T max (h)b | 1.50 (1.00–4.00) | 1.50 (1.00–4.00) | 1.25 (0.500–1.50) |
| t 1/2 (h)c | 37.6 (11) | 30.4 (8) | 48.6 (23.6) |
| Vz/F (L) | 77.4 (48) | 94.0 (34) | 216 (16.3) |
| CL/F (L/h) | 1.43 (47) | 2.14 (39) | 3.08 (34.9) |
% of AUC(144–inf): total (2.6%), extrapolated portion
Percent of total AUC(0–144) of radioactivity in plasma based on HPLC–LSC: regorafenib (57.4%), M-2 (28.7%), M-5 (6.3%), and M-7 (3.1%)
amg-Eq·h/L for AUC and mg-Eq/L for C max for total radioactivity; mg·h/L for AUC and mg/L for C max for regorafenib; values obtained by LC–MS/MS
bMedian (range)
cDue to differences in the lowest limit of quantification (LLOQ) of regorafenib using LC–MS/MS and the lowest limit of detection (LOD) of total radioactivity using liquid scintillation counting (LSC), different intervals for determination of half-life (t 1/2) were applied