Table 5.
Pharmacokinetic parameters for BPU in plasma
| Dose (mg) |
Week | Number of Patients |
Pharmacokinetic Parametersa |
|||||
|---|---|---|---|---|---|---|---|---|
| Tmax (h) |
Cmax (nM) |
Vz/F (L) |
Cls/F (L/h) |
t1/2,z (h) |
AUCb (μM*h) |
|||
| 5 | 1 | 1 | 1.0 | 13.8 | 9667 | 121 | 56 | 0.09 |
| 5 | 4 | 1 | 1.0 | 9.6 | NR | 142 | NR | 0.08 |
| 10 | 1 | 1 | 4.2 | 9.1 | 16282 | 134 | 84 | 0.16 |
| 10 | 4 | 1 | 1.0 | 14.3 | NR | 101 | 27 | 0.21 |
| 20 | 1 | 1 | 1.5 | 115 | 4165 | 97 | 30 | 0.44 |
| 20 | 4 | 1 | 2.0 | 36.2 | NR | 160 | 26 | 0.27 |
| 40 | 1 | 1 | 1.0 | 192 | 11992 | 158 | 52 | 0.54 |
| 40 | 4 | 1 | 1.5 | 130 | NR | 114 | 27 | 0.75 |
| 80 | 1 | 1 | 6.0 | 579 | 1657 | 14 | 81 | 12.0 |
| 80 | 4 | 1 | 2.0 | 994 | NR | 15 | 111 | 11.3 |
| 160 | 1 | 1 | 1.0 | 2040 | 5802 | 22 | 182 | 15.4 |
| 160 | 4 | 1 | 1.5 | 838 | NR | 53 | 138 | 6.4 |
| 320 | 1 | 6 | 1.8 ± 0.4 | 3484 ± 799 | 3305 ± 2018 | 17 ± 6 | 161 ± 133 | 46.2 ± 22.6 |
| 320 | 4 | 6 | 1.7 ± 0.4 | 3129 ± 1366 | NR | 21 ± 9 | 123 ± 65 | 40.4 ± 24.1 |
| 150 | 1 | 7 | 2.7 ± 2.0 | 630 ± 349 | 6056 ± 2592 | 50 ± 19 | 95 ± 48 | 7.4 ± 3.0 |
| 150 | 4 | 7 | 2.0 ± 2.0 | 774 ± 278 | NR | 47 ± 28 | 186 ± 161 | 9.0 ± 5.1 |
| 150 | 8 | 6 | 3.3 ± 2.2 | 349 ± 173 | NR | 51 ± 35 | 198 ± 79 | 9.0 ± 6.1 |
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; NR = not reportable; Tmax, time of the maximal plasma concentration; T1/2, z, terminal half-life; Vz/F, apparent volume of distribution.