Table 2.

Plasma PCI-24781 pharmacokinetic parameters following oral administration of PCI 24781 on day 1 by cohort (phase I pharmacokinetics evaluable population)

BID Dose levela (schedule)30 mg/m2 (days 1–5, 8–12, 15–19)45 mg/m2 (days 1–5, 8–12, 15–19)45 mg/m2 (days 1–7, 15–21)60 mg/m2 (days 1–7, 15–21)
Cohort1 (n = 5)2 (n = 7)3 (n = 3)4 (n = 9)
tmax (h) median (min–max)1.00 (0.917, 2.00)1.08 (1.00, 1.18)1.03 (1.00, 2.08)1.00 (0.667, 2.17)
Cmax (μmol/L) mean (SD)0.185 (0.075)0.339 (0.245)0.226 (0.088)0.295 (0.155)
AUC(0–4) (μmol/L/h) mean (SD)0.409 (0.085)b0.630 (0.424)0.440 (0.107)0.693 (0.427)
  • aAdministered within 28-day cycles.

  • bN = 4.