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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