Skip to main content

Table 3 Pharmacokinetic parameters for ASP3026 (cycle 1, day 1)

From: First-in-human, open-label dose-escalation and dose-expansion study of the safety, pharmacokinetics, and antitumor effects of an oral ALK inhibitor ASP3026 in patients with advanced solid tumors

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)
  1. Calculated accumulation ratio (AUCd28, tau/AUC24h of cycle 1, day 1)
  2. AUC area under the concentration–time curve, C max maximum concentration observed, NA not applicable, t max time of maximum concentration observed
  3. aMedian (range); mean (standard deviation) for other parameters