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 AUC_brain to AUC_plasma ratio of 0.004 indicates the severely restricted brain distribution of vemurafenib.

	Plasma	Brain
Terminal rate constant, min⁻¹	0.0051	0.0047
Half-life, min	136	148
Clearance, ml/min	0.04
Volume of distribution, ml	7.9
AUC_0→tlast, min · μg/ml	1663 ± 140^*	6.5 ± 0.9^*
AUC_Brain/AUC_Plasma	0.004

↵* Mean ± S.E. (standard error of the estimate).