Table 3:
Pazopanib pharmacokinetics in the dose expansion cohort
Mean (SD) | Median | Range | Number of observations | |
---|---|---|---|---|
Cmax, steady state (μg/mL) | 51·0 (13·9) | 57·6 | 31·7–66·6 | 7 |
Tmax, steady state (h) | 3·3 (1·4) | 3·0 | 2·0–6·0 | 7 |
Cmin, steady state (μg/mL) | 35·9 (5·5) | 36·8 | 28·8–41·5 | 5 |
AUC0–24 h, steady state (h × mg/L) | 1080·7 (144·9) | 1114·2 | 877·6–1216·7 | 4 |
Ke (per h) | 0·02 (0·01) | 0·02 | 0·02–0·03 | 4 |
T1/2 (h) | 31·9 (6·4) | 33·0 | 23·1–38·5 | 4 |
Clearance steady state/bioavailability (L/h) | 0·74 (0·13) | 0·7 | 0·6–0·9 | 4 |
Vz, steady state bioavailability (L/kg) | 0·7 (0·1) | 0·7 | 0·6–0·8 | 4 |
Pharmacokinetics analyses were done in the nine patients recruited in the dose expansion phase who received the recommended phase 2 dose of combination therapy. All patients received pazopanib at the indicated doses plus weekly cetuximab. Cmax=maximum plasma concentration. Tmax=time to reach the maximum plasma concentration. Cmin=minimum concentration. AUC=area under the curve. Ke=elimination rate constant. T1/2=half-life. Vz=volume of distribution.