Table 2.
Estimated and derived sunitinib pharmacokinetic parameters in the final model
| Estimated parameters | Estimate | Standard error of estimate (RSE%) | Interindividual variability (IIV) (CV%) | Standard error of IIV (RSE%) |
|---|---|---|---|---|
| Cl/F (L/h) | 50.5 | 20.6 | 67.9 | 42.7 |
| Vd/F(L) | 3210 | 7.8 | nd | nd |
| ka (h−1) | 0.468 | 27.6 | 63.9 | 42.9 |
| Relative F | 1.11 | 70 | nd | nd |
| Absorption lag time (h) | 0.487 | 6.8 | nd | nd |
| Proportional residual error (%) | 16.3 | 22.9 | nd | nd |
| Derived parameters* | Sunitinib without grapefruit juice | Sunitinib with grapefruit juice when simultaneously taken |
|---|---|---|
| AUC0–24 h (ng h/mL) | 1122 (277–2399) | 1245 (308–2663) |
| Cmax (ng/mL) | 13.0 (10.0–14.6) | 14.4 (11.1–16.2) |
| t 1/2 (h) | 53 (12–107) | |
| T max (h) | 8.2 (2.8–12.4) | |
RSE relative standard error; Cl/F apparent clearance; Vd/F apparent volume of distribution; ka absorption rate constant; F bioavailability; nd not determined; AUC 0–24 h area under the plasma concentration–time curve over the dose interval 0–24 h at steady-state pharmacokinetics; t 1/2 elimination half-life; T max time to reach peak plasma concentration
Between-subject variability was assessed using exponential models
* Derived parameters are calculated from estimated parameters and are demonstrated as mean values (range)