TABLE 5

Comparison of brain distribution of vemurafenib and dabrafenib in FVB wild-type mice after an i.v. dose of 2.5 mg/kg

DabrafenibVemurafeniba
PlasmaBrainPlasmaBrain
Terminal rate constant (min−1)0.0310.0360.00510.0047
Half-life (min)23.719.1136148
Clearance (ml/min/kg)24.21.6
Volume of distribution (l/kg)0.830.316
AUC0 → t last (min · µg/ml)120.9 ± 15.82.8 ± 0.41663 ± 1406.5 ± 0.9
Kp0.0230.004
  • AUC, area under the concentration-time curve; FVB, Friend leukemia virus strain B; Kp, AUCbrain/AUCplasma.

  • a From previously published data (Mittapalli et al., 2012).