Table 3.
Summary of PK parameters (mean ± SD, unless otherwise stated) at Cycle 1 Day 1 for blood AUY922 [28–70 mg/m2 (four highest doses)]
| AUY922 PK parameter | AUY922 dose (mg/m2) | |||
|---|---|---|---|---|
| 28 (n = 5) | 40 (n = 3) | 54 (n = 6) | 70 (n = 8) | |
| T max [median, h (range)] | 0.50 (0.48–1.07) | 1.05 (0.50–1.05) | 0.76 (0.48–1.17) | 1.02 (0.23–1.17) |
| C max (ng/ml) | 457 ± 101 | 710 ± 42 | 1,050 ± 118 | 1,100 ± 118 |
| AUC(0–last) (h·ng/ml) | 6,810 ± 1,090 | 6,960 ± 1,270 | 8,880 ± 1,710 | 8,540 ± 895 |
| AUC(0–inf) (h·ng/ml) | 9,550 ± 2,460 | 11,400 ± 3470a | 12,300 ± 2720a | 12,600 ± 1,720 |
| CL (l/h) | 4.79 ± 1.68 | 5.74 ± 1.16a | 7.24 ± 1.97a | 8.60 ± 1.30 |
| Vz (l) | 646 ± 111 | 980 ± 132a | 1,190 ± 151a | 1,570 ± 293 |
| T1/2 (h) | 98.7 ± 23.0 | 123.0 ± 40.8a | 120.0 ± 28.5a | 127.0 ± 18.8 |
PK pharmacokinetics, SD standard deviation
aData missing for one patient