Table 6.
Pharmacokinetic parameters for mmBPU and amino-BPU in plasma
| Dose (mg) |
Week | Number of Patients |
Pharmacokinetic Parametersa |
|||||
|---|---|---|---|---|---|---|---|---|
| Tmax (h) |
Cmax (nM) |
t1/2,z (h) |
AUCb (μM*h) |
Metabolite:BPU AUC ratio |
||||
| mmBPU | 320 | 1 | 6 | 1.93 ± 0.21 | 2858 ± 742 | 279 ± 170 | 130 ± 73.0 | 3.5 ± 1.4 |
| mmBPU | 320 | 4 | 6 | 2.26 ± 0.88 | 3279 ± 996 | 483 ± 301 | 122 ± 56.2 | 3.2 ± 0.9 |
| mmBPU | 150 | 1 | 7 | 3.51 ± 2.63 | 517 ± 306 | 317 ± 89 | 29.2 ± 13.9 | 4.3 ± 2.2 |
| mmBPU | 150 | 4 | 7 | 2.51 ± 2.42 | 732 ± 338 | 283 ± 122 | 28.0 ± 16.0 | 4.1 ± 3.2 |
| mmBPU | 150 | 8 | 6 | 4.05 ± 1.81 | 349 ± 94 | 736 ± 420 | 29.8 ± 9.5 | 4.7 ± 3.9 |
| amino-BPU | 320 | 1 | 6 | 2.59 ± 1.10 | 251 ± 131 | 734 ± 101 | 15.7 ± 8.9 | 0.5 ± 0.2 |
| amino-BPU | 320 | 4 | 6 | 3.67 ± 1.50 | 582 ± 228 | 415 ± 158 | 54.3 ± 33.7 | 1.4 ± 0.6 |
| amino-BPU | 150 | 1 | 7 | 31.20 ± 67.88 | 46 ± 40 | 255 ± 276 | 2.6 ± 1.7 | 0.4 ± 0.4 |
| amino-BPU | 150 | 4 | 7 | 32.27 ± 62.41 | 87 ± 56 | 623 ± 283 | 9.0 ± 6.5 | 1.4 ± 1.4 |
| amino-BPU | 150 | 8 | 6 | 23.33 ± 23.40 | 71 ± 37 | 986 ± 504 | 10.4 ± 4.7 | 1.8 ± 1.8 |
a
Values are reported as the mean ± standard deviation for the 150 and 320 mg dose level.
b
AUCinf is reported for all dose levels for week 1; AUClast is reported for all dose levels for week 4; AUC0-168 h is reported for all dose levels for week 8.
Abbreviations: AUC, area under the concentration-time curve; Cmax, maximal plasma concentration;Tmax, time of the maximal plasma concentration; T1/2, z, terminal half-life.