Table 3.

Pazopanib Pharmacokinetic Parameters After Single and Repeated Daily Doses

Dose	No. of Patients*	Tmax (hours)		Cmax (μg/mL)		AUC0-8 h (μg/mL · h)		AUC0-24 h (μg/mL · h)		Css† (μg/mL)
		Mean	SD	Mean	SD	Mean	SD	Mean	SD	Mean	SD
Tablet (part 1)
275 mg/m2
Day 1	5	7.6	8.4	36.5	16.5	184	88	484	244	33.0	16.2
Day 15/22	5	2.2	1.1	48.9	13.2	309	58
350 mg/m2
Day 1	2	3.5		34.7		199		511		30.8	19.2
Day 15/22	1	2.0		11.6		61.4
450 mg/m2
Day 1	2	4.0		66.7		354		999		23.9	13.5
Day 15/22	2	3.5		59.8		394
600 mg/m2
Day 1	3	6.1	2.0	23.0	8.4	314	253	832	496	42.8	18.8
Day 15/22	3	4.8	2.4	86.5	21.3	601	151
Suspension (part 2a)
160 mg/m2
Day 1	12	3.8	3.0	22.9	13.8	128	69	401	264	24.4	8.5
Day 15/22	10	3.4	2.6	40.0	13.5	262	94
225 mg/m2
Day 1	4	3.0	2.0	30.8	14.1	181	80	419	200	28.4	11.5
Day 15/22	2	2.0		46.0		295
Imaging (part 2b)
450 mg/m2
Day 1	3	5.4	4.2	21.4	7.6	119	34	375	166	45.9	15.9
Day 15/22	3	2.0	1.7	45.9	20.0	331	144

NOTE. Participation in extended pharmacokinetic studies was optional on parts 1 and 2b but required for part 2a. Participation in steady-state studies was mandatory for all patients.

Abbreviations: AUC_{0-8 h}, area under the curve from 0 to 8 hours; AUC_{0-24 h}, area under the curve from 0 to 24 hours; C_max, maximum serum concentration; C_ss, steady-state plasma trough concentration; SD, standard deviation; T_max, time to maximum serum concentration.

^*Number of patients who participated in extended pharmacokinetic sampling.

^†The C_ss column shows the mean and SD values of the trough concentrations across days 15 to 27 at each dose level. At least one trough value on day 15, 22, and/or 27 was available for 43 patients (31 patients had all three values). Specifically for C_ss, the numbers of patients were as follows: tablet 275 mg/m² (n = 6), 350 mg/m² (n = 6), 450 mg/m² (n = 5), and 600 mg/m² (n = 5); suspension 160 mg/m² (n = 11) and 225 mg/m² (n = 3); and imaging 450 mg/m² (n = 7).