TABLE 1

Vemurafenib pharmacokinetic parameters after an intravenous dose of 2.5 mg/kg in FVB wild-type mice

Plasma and brain pharmacokinetic parameters were analyzed by using noncompartmental analysis after an intravenous dose of 2.5 mg/kg in FVB wild-type mice. The AUCbrain to AUCplasma ratio of 0.004 indicates the severely restricted brain distribution of vemurafenib.

PlasmaBrain
Terminal rate constant, min−10.00510.0047
Half-life, min136148
Clearance, ml/min0.04
Volume of distribution, ml7.9
AUC0→tlast, min · μg/ml1663 ± 140*6.5 ± 0.9*
AUCBrain/AUCPlasma0.004
  • * Mean ± S.E. (standard error of the estimate).