TABLE 2.
Pharmacokinetic parameters by cohort for BAL4815 estimated after once-daily intravenous 1-h constant-rate infusion of BAL8557a
| Cohortb and study day | Cmax (μ/ml) | AUC0-24 h (μ · h/ml) | AUC0-∞ (μ · h/ml) | t1/2 (h) | VSS (liters) | CLSS (liters/h) |
|---|---|---|---|---|---|---|
| Cohort 3 | ||||||
| Day 1 | 1.28 (±0.122) | 7.32 (±1.09) | — | — | — | — |
| Day 8 | 0.987 (±0.180) | 12.4 (±3.77) | — | — | — | — |
| Day 14c | 1.17 (±0.237) | 14.3 (±5.33) | 90.2 (±52.2) | 93.0 (±40.1) | 470 (±162) | 4.06 (±1.97) |
| Cohort 4 | ||||||
| Day 1 | 2.32 (±0.445) | 12.9 (±1.93) | — | — | — | — |
| Day 8 | 2.52 (±1.05) | 24.3 (±5.79) | — | — | — | — |
| Day 14 | 2.55 (±0.883) | 33.6 (±9.67) | 236 (±31.5)d | 117 (±17.6)d | 542 (±229)d | 3.19 (±0.901) |
a
Values are presented as arithmetic means plus or minus SD of six subjects except where indicated. —, values could not be reliably estimated as plasma samples could be collected during only a 24-h interval.
b
For cohort 3, loading doses of 100-mg equivalents of BAL4815 were followed by once-daily maintenance doses of 50-mg equivalents of BAL4815; for cohort 4, loading doses of 200-mg equivalents of BAL4815 were followed by once-daily maintenance doses of 100-mg equivalents of BAL4815.
c
n = 5.
d
n = 4.