Table 3. The pharmacokinetic parameters of crizotinib and 2-keto crizotinib in rats (n = 5, mean ± S.D.).
| Compound | Crizotinib | 2-Keto crizotinib | ||
|---|---|---|---|---|
| Group | Crizotinib | Crizotinib + Tropifexor | Crizotinib | Crizotinib + Tropifexor |
| AUC(0−t)(ng/mL*h) | 4,098.16 ± 480.24 | 5,563.04 ± 1,112.56* | 603.21 ± 97.71 | 877.14 ± 268.34 |
| AUC(0−∞) (ng/mL*h) | 4,141.79 ± 490.95 | 5,669.41 ± 1,166.99* | 604.85 ± 99.06 | 879.58 ± 268.53 |
| t1/2 (h) | 6.83 ± 0.77 | 8.23 ± 1.65 | 4.82 ± 1.18 | 5.78 ± 1.79 |
| Tmax (h) | 8.80 ± 1.79 | 8.80 ± 1.79 | 8.00 ± 0.00 | 8.80 ± 1.79 |
| CLz/F (L/h/kg) | 6.10 ± 0.69 | 4.56 ± 0.90* | 42.25 ± 7.06 | 30.44 ± 8.32* |
| Cmax (ng/mL) | 236.97 ± 45.30 | 325.92 ± 40.95* | 51.05 ± 14.39 | 74.33 ± 26.83 |
Notes.
Significant differences from control group, *P < 0.05.