Table 4.
Steady-state Pazopanib Pharmacokinetics Measured in All Patients at Week 3 (medians and ranges)
| Group | Dose (mg) |
N | Cmax (µg/mL) |
Tmax (hr) |
C(0)1 µg/mL |
AUC(0–6) (µg/mLxhr) |
AUC(0–24) (µg/mLxhr) |
CL/F2 (L/hr) |
|---|---|---|---|---|---|---|---|---|
| A | 800 | 18 | 52.0 (17.1–85.7) | 2.8 (1.(0–24).2) | 29.8 (10.3–750.) | 260.5 (92.0–475.9) | 888.2 (345.5–1482) | 0.9 (0.5–2.3) |
| B | 3003 | 1 | 32.9 | 3.0 | 17.3 | 170.5 | n/a | n/a |
| 400 | 5 | 22.7 (14.6–39.8) | 3.0 (2.0–4.1) | 19.3 (6.8–36.6) | 125.1 (78.3–205.8) | 467.6 | 0.9 | |
| 800 | 12 | 33.5 (11.3–104.2) | 3.0 (0.5–24.4) | 24.0 (8.3–74.6) | 176.5 (41.4–518.1) | 774.2 (214.7–2034.4) | 1.0 (0.4–3.7) | |
| C | 200 | 11 | 22.2 (4.2–32.9) | 2.0 (0.0–4.0) | 16.2 (3.1–24.2) | 122.2 (21.2–182.9) | 256.8 (65.7–487.7) | 0.8 (0.4–3.0) |
| 400 | 3 | 17.6 (13.0–42.5) | 4.0 (3.0–5.9) | 16.5 (11.8–28.9) | 94.1 (74.7–220.0) | n/a | n/a | |
| D | 100 | 5 | 2.3 (0.7–12.6) | 4.0 (1.1–6.0) | 4.2 (2.3–9.4) | 12.8 (3.0–69.1) | n/a | n/a |
| 200 | 14 | 9.4 (2.4–24.3) | 3.0 (1.0–8.0) | 5.7 (1.5–18.4) | 49.2 (9.5–134.5) | 130.6 (46.9–473.2) | 1.7(0.4–4.3) |
1
C(0) is the pre-dose plasma concentration and is equivalent to the trough level following the previous dose.
2
CL/F calculated as dose/AUC(0–24) at steady-state for the 24-hour dosing interval.
3
Patient was dose-reduced per protocol prior to week 3.