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. 2010 Nov 1;28(31):4762–4768. doi: 10.1200/JCO.2010.30.3545

Table 4.

Pharmacokinetic Parameters of Vandetanib After a Single Dose and at Steady-State

Parameter Dosage Level
1: 50 mg/m2(n = 3)
2: 65 mg/m2(n = 2)
3: 85 mg/m2(n = 2)
4: 110 mg/m2(n = 8)
5: 145 mg/m2 (n = 7)
Median Range Median Range Median Range Median Range Median Range
After single dose
    Cmax (ng/mL) 84.4 84-87.7 149.5 106-193 158 156-160 264 189-342 368 174-636
    Tmax (h) 8.3 7.9-12 8.1 8-8.1 12.2 12.1-12.4 7.6 2.1-12.4 8.5 6.3-12.2
    AUC0-24 (ng/mL·h) 1,276 1,193-1,310 2,320 1,638-3,002 2,740 2,530-2,950 4,192 3,179-5,234 6,468 3,060-8,297
Parameter n = 3 n = 3 n = 3 n = 15 n = 9
Steady-state
    Ctrough,SS (ng/mL) 413 334-609 579 567-690 857 442-872 748 418-996 888 433-2,367
    Accumulation factor* 9.6 8.5-20 9 7.6-16.6 8.3 4.8-10 6.5 4.1-10.2 5.5 2.2-13.8

Abbreviations: Cmax, maximum concentration; Tmax, time to maximum concentration; AUC0-24, area under concentration-time curve from 0 to 24 hours after a single dose; Ctrough, SS, mean trough concentration at steady-state; h, hour.

*

Accumulation factor stands for the ratio of mean Ctrough, SS/Ctrough after the first dose.

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