Table 4.
EMD 525797 PK data
| EMD 525797 | ||||||
|---|---|---|---|---|---|---|
| 35 mg | 100 mg | 250 mg | 500 mg | 1000 mg | 1500 mg | |
| N = 6 | N = 6 | N = 6 | N = 6 | N = 6 | N = 6 | |
| Cmax, μg/mL | ||||||
| Mean | 5.9 | 21.9 | 65.7 | 141 | 292 | 449 |
| (SD) | (0.76) | (1.75) | (7.48) | (15.2) | (42.0) | (58.7) |
| Range | 4.9–6.5 | 19.3–24.5 | 54.8–75.1 | 122–158 | 229–358 | 368–521 |
| Tmax, h | ||||||
| Median | 1.3 | 2.0 | 1.5 | 1.8 | 3.5 | 2.0 |
| Range | 1.0–4.0 | 1.5–3.0 | 1.0–2.0 | 1.0–4.0 | 1.5–8.0 | 1.0–6.0 |
| AUC0-∞, μg/mL•h | ||||||
| Mean | 169 | 1155 | 7350 | 21834 | 55811 | 112023 |
| (SD) | (20.2) | (212.6) | (1158) | (4936) | (9042) | (20183) |
| Range | 144–201 | 932–1513 | 6538–9421 | 17438–28809 | 43219–64439 | 81964–141859 |
| t1/2, h | ||||||
| Mean | 19.3 | 32.5 | 92.6 | 128.7 | 206.3 | 246.1 |
| (SD) | (3.5) | (6.8) | (24.4) | (35.1) | (24.8) | (79.1) |
| Range | 13.3–23.2 | 20.9–40.3 | 61.2–129.3 | 95.7–174.4 | 178.0–248.0 | 156.7–356.2 |
| CL, L/h | ||||||
| Mean | 0.209 | 0.089 | 0.035 | 0.024 | 0.018 | 0.014 |
| (SD) | (0.024) | (0.015) | (0.005) | (0.005) | (0.003) | (0.003) |
| Range | 0.18–0.24 | 0.07–0.11 | 0.03–0.04 | 0.02–0.03 | 0.02–0.02 | 0.01–0.02 |
| Vz, L | ||||||
| Mean | 5.9 | 4.1 | 4.5 | 4.3 | 5.4 | 4.7 |
| (SD) | (1.5) | (0.6) | (0.9) | (0.9) | (0.9) | (0.9) |
| Range | 4.2–8.1 | 3.1–4.8 | 3.4–5.8 | 3.2–5.8 | 4.4–6.5 | 3.5–5.7 |
AUC area under the concentration-time curve; CL clearance; C max maximum serum concentration; PK pharmacokinetic; SD standard deviation; t1/2, half-life; T max time to maximum serum concentration; V z volume of distribution