TABLE 2

GDC-0449 concentrations and exposures of GDC-0449 after an intravenous (25 mg/dog) or oral (25 mg/capsule) dose, with or without administration of activated charcoal to male dogs

TreatmentC24 hC96 hAUC0–168
μMμMμM · h
25 mg p.o.0.650 ± 0.2870.137 ± 0.09348.4 ± 20.1
25 mg p.o. with + charcoal0.847 ± 0.7330.004 ± 0.00525.9 ± 21.2
25 mg i.v.a5.07 ± 0.613.16 ± 0.52603 ± 57
25 mg i.v. with + charcoal4.49 ± 0.420.018 ± 0.016173 ± 24
  • AUC0–168, area under the plasma concentration-time profile from time 0 to 168 h postdose; C24 h, plasma concentration at 24 h postdose; C96 h, plasma concentration at 96 h postdose.

  • a Data from intact male dogs from bile duct-cannulated dog study. Data presented here for comparative purposes.