Table 4.
Pharmacokinetic parameters for ASP3026 (cycle 1, day 28)
| Dose (mg; once daily) | Number | C max (ng/mL) | t max (h)a | AUC24 (ng h/mL) | t ½ (h) |
|---|---|---|---|---|---|
| Dose-escalation cohort | |||||
| 25 | 3 | 68.4 (42.3) | 3.0 (1.0–8.1) | 1038 (335) | 36.6 (15.7) |
| 50 | 3 | 143 (62.4) | 3.0 (2.0–4.0) | 2111 (541) | 35.2 (18.7) |
| 75 | 3 | 352.5 (147.5) | 3.0 (2.0–4.0) | 5627 (1791) | 84.7 (53.9) |
| 125 | 1 | 667.9 (NA) | 2.1 (NA) | 8967 (NA) | 36.7 (NA) |
| 200 | 3 | 681.8 (104.8) | 3.0 (2.1–3.0) | 7620 (1699) | 21.9 (1.4) |
| 325 | 3 | 1159 (856.9) | 4.0 (3.0–4.0) | 18,764 (17,647) | 26.3 (29.1) |
| 525 | 6 | 2819 (1681) | 3.5 (2.0–4.1) | 40,114 (24,479) | 27.3 (5.0) |
| 800 | 1 | 4854 (NA) | 4.0 (NA) | 78,081 (NA) | 37.9 (NA) |
| Dose-expansion cohort | |||||
| 525 | 15 | 1331 (813.7) | 4.0 (0–4.1) | 19,993 (10,552) | 24.9 (12.7) |
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