TABLE 8.
Pharmacokinetic parameters of almonertinib in rats after oral administration alone and combined multiple doses of rivaroxaban or apixaban.
| Parameters (Unit) | Almonertinib (15 mg/kg) | |||
|---|---|---|---|---|
| Alone (group 3) | With multiple-doses rivaroxaban (group 9) | Alone (group 4) | With multiple-doses Apixaban(group 10) | |
| AUC0-t (μg/L*h) | 138.29 ± 31.29 | 299.48 ± 149.69* | 280.58 ± 43.26 | 266.75 ± 51.89 |
| AUC0-∞(μg/L*h) | 138.29 ± 31.29 | 299.48 ± 149.69* | 298.74 ± 46.78 | 292.64 ± 48.88 |
| Cmax (μg/L) | 22.77 ± 4.76 | 51.43 ± 24.91** | 39.82 ± 8.12 | 42.15 ± 5.99 |
| Tmax (h) | 2.17 ± 1.13 | 3.17 ± 0.41 | 1.83 ± 1.03 | 2.50 ± 1.18 |
| t1/2z (h) | 2.18 ± 1.05 | 2.70 ± 0.78 | 5.40 ± 4.96 | 6.79 ± 4.15 |
| CLz/F (L/h/kg) | 112.62 ± 22.42 | 62.17 ± 31.01** | 51.29 ± 8.37 | 52.59 ± 9.62 |
| Vz/F (L/kg) | 330.81 ± 125.45 | 243.80 ± 167.75 | 383.29 ± 315.50 | 522.18 ± 317.78 |
| MRT0-t (h) | 5.03 ± 0.73 | 5.15 ± 0.66 | 6.53 ± 0.97 | 6.49 ± 0.35 |
| MRT0-∞ (h) | 5.03 ± 0.74 | 5.15 ± 0.66 | 8.35 ± 3.38 | 9.31 ± 2.59 |
*p < 0.05, **p < 0.01, compared with 15 mg/kg almonertinib alone, demonstrating statistically significant difference. The main pharmacokinetic parameters are revealed as the mean ± standard deviation.