Table 3.
Pharmacokinetic parameters for ASP3026 (cycle 1, day 1)
| Dose (mg; once daily) | Number | C max (ng/mL) | t max (h)a | AUC24 (ng h/mL) |
|---|---|---|---|---|
| Dose-escalation cohort | ||||
| 25 | 4 | 32.0 (10.2) | 3.0 (0.5–4.0) | 378 (104) |
| 50 | 3 | 99.7 (56.6) | 3.0 (2.0–4.0) | 846 (225) |
| 75 | 3 | 87.6 (40.3) | 8.2 (2.0–24.2) | 1155 (442) |
| 125 | 4 | 261.7 (131.1) | 5.0 (1.0–8.0) | 3000 (860) |
| 200 | 4 | 490.5 (68.6) | 2.5 (2.0–3.0) | 4585 (1310) |
| 325 | 3 | 586.2 (109.7) | 3.0 (3.0–8.0) | 7950 (1957) |
| 525 | 6 | 1750 (1279) | 4.0 (3.0–4.2) | 18,543 (10,812) |
| 800 | 3 | 1633 (252.7) | 3.0 (2.0–8.0) | 21,796 (5990) |
| Dose-expansion cohort | ||||
| 525 | 16 | 961.0 (563.8) | 3.1 (2.0–8.0) | 11,746 (9063) |
Calculated accumulation ratio (AUCd28, tau/AUC24h of cycle 1, day 1)
AUC area under the concentration–time curve, C max maximum concentration observed, NA not applicable, t max time of maximum concentration observed
aMedian (range); mean (standard deviation) for other parameters