TABLE 2.
Summary of pharmacokinetic parameters of dacomitinib and Vizimpro® under fasting and fed conditions.
| PK parameter | Fasting condition | Fed condition | ||
|---|---|---|---|---|
| Test (n = 30) | Reference (N = 29) | Test (N = 29) | Reference (N = 30) | |
| T max (h) | 6.00 (4.5, 10) | 6.00 (4.5, 48) | 5.00 (4.5, 12) | 5.00 (4.5, 12) |
| Cmax (ng/mL) | 37.58 ± 11.03 | 35.01 ± 11.23 | 35.47 ± 8.79 | 35.50 ± 7.81 |
| AUC0–t (ng∙h/mL) | 1709.51 ± 387.14 | 1607.10 ± 452.92 | 1769.02 ± 388.25 | 1790.58 ± 377.98 |
| AUC0–∞ (ng∙h/mL) | 1851.27 ± 467.85 | 1762.55 ± 541.14 | 1901.05 ± 438.31 | 1927.24 ± 417.64 |
| λ z (h–1) | 0.0117 ± 0.0030 | 0.0114 ± 0.0036 | 0.0119 ± 0.0031 | 0.0115 ± 0.0030 |
| t 1/2 (h) | 62.95 ± 16.58 | 67.10 ± 22.57 | 61.70 ± 15.04 | 63.95 ± 16.82 |
| AUC_%Extrap (%) | 7.09 ± 4.38 | 8.14 ± 5.32 | 6.68 ± 3.41 | 6.90 ± 3.63 |
| Vz/F (L) (CV%) | 2206.28 (26.62) | 2465.86 (32.66) | 2097.34 (26.01) | 2134.01 (28.63) |
| CL/F (L/h) (CV%) | 25.09 (23.64) | 26.76 (34.59) | 24.26 (22.85) | 23.88 (21.76) |
Note: Vz/F and CL/F values are geometric mean (CV%); T max values are median (minimum, maximum); the remaining values are arithmetic mean ± standard deviation (SD).
Abbreviations: AUC0–t , area under the concentration–time curve from time 0 to the last observed non‐zero concentration calculated by the linear trapezoidal method; AUC0–∞, area under the concentration–time curve from time 0 extrapolated to infinity; AUC_%Extrap, the percentage of the AUC derived after extrapolation; Cmax, maximum plasma concentration; CL/F: apparent clearance; CV, coefficient of variation; λ z : the terminal elimination rate; PK, pharmacokinetic; t 1/2, terminal half‐life; T max, time to maximum plasma concentration; Vz/F: apparent volume of distribution.