Table 2.
Pharmacokinetic parameters (mean ± SD) of famitinib (M0) and N-desethylfamitinib (M3) following oral administration of 20 or 27 mg famitinib L-malate once daily for 28 days in patients
| tmax (h) | Cmax (ng·mL−1) | Cmin (ng·mL−1) | Cav (ng·mL−1) | AUC0–24h (ng·h·mL−1) | DF (%) | AR | ||
|---|---|---|---|---|---|---|---|---|
| Dose = 20 mg (n = 8) | ||||||||
| Day 1 | M0 | 6.75 ± 2.38 | 21.7 ± 7.78 | N.A. | N.A. | 333 ± 119 | N.A. | N.A. |
| M3 | 7.75 ± 2.71 | 0.963 ± 0.366 | N.A. | N.A. | 14.9 ± 5.85 | N.A. | N.A. | |
| Day 28 | M0 | 7.13 ± 3.36 | 44.2 ± 18.4 | 20.8 ± 8.32 | 33.5 ± 14.5 | 805 ± 348 | 71.0 ± 31.3 | 2.73 ± 1.29 |
| M3 | 12.8 ± 9.68 | 3.12 ± 1.22 | 1.70 ± 0.837 | 2.52 ± 1.18 | 60.5 ± 28.4 | 63.5 ± 31.5 | 6.03 ± 4.82 | |
| Dose = 27 mg (n = 7) | ||||||||
| Day 1 | M0 | 4.44 ± 1.24 | 47.7 ± 11.3 | N.A. | N.A. | 674 ± 221 | N.A. | N.A. |
| M3 | 5.33 ± 2.78 | 1.99 ± 0.490 | N.A. | N.A. | 31.2 ± 8.00 | N.A. | N.A. | |
| Day 28 | M0 | 5.14 ± 1.07 | 73.5 ± 15.9 | 28.2 ± 9.79 | 50.2 ± 14.7 | 1205 ± 352 | 97.5 ± 37.3 | 1.80 ± 0.375 |
| M3 | 6.14 ± 3.39 | 4.57 ± 1.58 | 2.63 ± 1.34 | 3.60 ± 1.57 | 86.5 ± 37.7 | 64.0 ± 40.8 | 2.68 ± 0.860 |
N.A., not applicable.