TABLE 3.
Summary of pharmacokinetic parameters of KAE609 following oral administration of multiple ascending doses (part 2)
| Pharmacokinetic parameter | Mean ±SD for dose group on indicated day |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| 10 mg |
30 mg |
60 mg |
100 mg |
150 mg |
||||||
| Day 1 | Day 3 | Day 1 | Day 3 | Day 1 | Day 3 | Day 1 | Day 3 | Day 1 | Day 3 | |
| AUC0–24 (μg · h/ml) | 1.24 ± 0.20 | 1.91 ± 0.4 | 4.08 ± 0.72 | 6.42 ± 1.22 | 6.99 ± 0.97 | 14.1 ± 3.48 | 12.2 ± 1.94 | 19.8 ± 3.56 | 15.1 ± 2.73 | 29.4 ± 4.12 |
| Cmax (ng/ml) | 120 ± 16.7 | 161 ± 29.3 | 364 ± 55.4 | 468 ± 69.2 | 641 ± 91.7 | 991 ± 216 | 921 ± 164 | 1,170 ± 206 | 1,170 ± 260 | 1,770 ± 232 |
| Tmaxa (h) | 2 (1.0–3.0) | 2 (1.0–2.0) | 2 (2.0–2.02) | 2 (1.0—2.0) | 2 (1.0–4.0) | 1.5 (1.0–2.0) | 3 (1.0–4.0) | 2 (2.0–4.0) | 2 (2.0–4.0) | 2.5 (2.0–8.15) |
| T1/2 (h) | NAb | 21.4 ± 4.4 | NA | 22.4 ± 5.0 | NA | 28.0 ± 4.5 | NA | 23.1 ± 6.1 | NA | 26.9 ± 8.3 |
| Racc | 1.54 | 1.57 | 2.01 | 1.67 | 1.98 | |||||
a
Values are means ± standard deviations, except for Tmax values, which are medians (with ranges shown in parentheses), and Racc values (for which only the means are reported). N = 6 to 7 subjects per cohort.
b
NA, not available; the T1/2 was determined on day 3 only.