Table 4.

Pharmacokinetic variables of ABT-751 and its metabolites on cycle 1, day 7 (mean ± SD)

AnalyteVariableq.d. Regimens
b.i.d. Regimens
200 mg (n = 3)250 mg (n = 6)300 mg (n = 4)125 mg Morning (n = 5)125 mg Evening (n = 6)150 mg (n = 9)175 mg (n = 8)
ABT-751Cmax (μg/mL)6.6 ± 1.712.7 ± 5.813.0 ± 2.69.0 ± 1.8*5.4 ± 1.85.8 ± 2.09.0 ± 3.3
Tmax (h)1.7 ± 0.62.0 ± 3.00.8 ± 0.31.9 ± 1.33.3 ± 2.91.8 ± 1.01.3 ± 1.2
Ctrough (μg/mL)0.4 ± 0.00.5 ± 0.30.5 ± 0.30.8 ± 0.51.0 ± 0.70.9 ± 0.51.3 ± 0.4
AUCτ (μg·h/mL)42.8 ± 1.960.5 ± 21.650.2 ± 21.3*33.5 ± 8.628.1 ± 9.531.4 ± 9.043.5 ± 8.1
CL/F (L/h)4.7 ± 0.24.6 ± 1.86.6 ± 2.04.0 ± 1.24.9 ± 1.65.1 ± 1.24.1 ± 0.8
ABT-751Cmax (μg/mL)4.3 ± 1.46.1 ± 0.68.9 ± 1.88.7 ± 5.57.6 ± 3.59.5 ± 5.38.8 ± 2.9
    GlucuronideTmax (h)4.7 ± 1.23.7 ± 2.33.5 ± 1.94.4 ± 2.24.7 ± 2.15.8 ± 1.64.0 ± 2.6
Ctrough (μg/mL)1.1 ± 0.41.5 ± 1.22.7 ± 2.45.1 ± 4.24.7 ± 3.46.5 ± 4.44.8 ± 3.0
AUCτ (μg·h/mL)60.2 ± 19.883.7 ± 19.1128.9 ± 49.381.6 ± 56.569.4 ± 38.992.4 ± 50.578.3 ± 29.2
ABT-751 SulfateCmax (μg/mL)6.9 ± 3.37.8 ± 1.214.7 ± 6.88.1 ± 3.27.1 ± 2.99.0 ± 4.17.8 ± 3.1
Tmax (h)5.3 ± 1.23.2 ± 2.62.5 ± 1.03.6 ± 2.24.7 ± 2.14.9 ± 2.33.1 ± 2.2
Ctrough (μg/mL)2.0 ± 1.61.9 ± 2.03.3 ± 3.14.0 ± 2.13.9 ± 2.05.5 ± 3.84.0 ± 3.2
AUCτ (μg·h/mL)102.9 ± 67.494.6 ± 40.1179.2 ± 82.771.1 ± 31.961.8 ± 30.286.6 ± 44.765.9 ± 32.2
  • * Dose-normalized pharmacokinetic variables were statistically significantly different from those in other groups in the same regimen (P < 0.05).

  • AUC0−24 for q.d. regimens: AUC0-12 for b.i.d. regimens.

  • The statistical test for this variable was equivalent to that for AUCτ.