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Table 4 Pharmacokinetic parameters for ASP3026 (cycle 1, day 28)

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) 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)
  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