Table 3.
Pharmacokinetic parameters after a single IV infusion of BLZ-100.
| Cohort 1 |
Cohort 2 |
Cohort 3 |
Cohort 4 |
Cohort 5 |
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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 mg BLZ-100 (N = 3) |
3 mg BLZ-100 (N = 3) |
6 mg BLZ-100 (N = 6) |
12 mg BLZ-100 (N = 6) |
18 mg BLZ-100 (N = 3) |
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| Parameter, units | n | Mean | SD | na | Mean | SD | n | Mean | SD | n | Mean | SD | n | Mean | SD |
| t1/2, hours | 0 | NE | – | 1 | 0.33 | – | 6 | 0.36 | 0.07 | 6 | 0.50 | 0.12 | 2 | 1.75 | – |
| CL, mL/hour | 0 | NE | – | 1 | 10800 | – | 6 | 12100 | 4460 | 6 | 8830 | 3060 | 2 | 5260 | – |
| Vss, mL | 0 | NE | – | 1 | 4770 | – | 6 | 5710 | 1530 | 6 | 4740 | 1100 | 2 | 6110 | – |
| Cmax, ng/mL | 3 | 95.5 | 29.7 | 3 | 315 | 89.5 | 6 | 783 | 208 | 6 | 1900 | 529 | 3 | 3830 | 1230 |
| Tlast, hours | 3 | 1.00 | 0.00 | 3 | 1.34 | 0.57 | 6 | 2.17 | 0.41 | 6 | 3.34 | 0.82 | 3 | 8.02 | 3.98 |
| AUC0-t, hr*ng/mL | 0 | NE | – | 3 | 184 | 77.5 | 6 | 548 | 197 | 6 | 1470 | 450 | 3 | 4430 | 1790 |
a. n = number of subjects for whom data were sufficient for estimation of each parameter. AUC0-t = area under the curve from 0 to the last measurable time point; CL = apparent clearance; Cmax = maximum observed concentration; NE = not estimable; SD = standard deviation; t1/2 = half-life based on the terminal portion of the concentration vs time curve; Tlast = time of the last observed measurable concentration; Vss = apparent steady-state volume of distribution.