TABLE 3

Brain-to-plasma ratios of sunitinib in all genotypes after a single oral dose (20 mg/kg), steady-state concentration ratios after a continuous intraperitoneal infusion (rate equal to 30 µg/h), at transient steady state (calculated as the maximum brain concentration to the corresponding plasma concentration in each genotype), and concentration ratios determined at 1 hour post oral dose (20 mg/kg) in each genotype

Data are presented as the mean ± S.D.

GenotypeAUC0, POCss Steady State i.p.Transient Steady StateRatio at 1 h
FVB wild type0.420.51 ± 0.260.66 ± 0.170.42 ± 0.09
Mdr1a/b(−/−)1.612.33 ± 0.562.42 ± 1.421.76 ± 0.65
Bcrp1(−/−)0.880.73 ± 0.441.09 ± 0.380.24 ± 0.20
Mdr1a/b(−/−)Bcrp1(−/−)20.5317.44 ± 5.0812.83 ± 1.268.14 ± 3.47
  • PO, orally.