TABLE 1

Plasma concentration, brain concentration, and brain-to-plasma ratio after oral administration of GNE-317 (50 mg/kg) or pictilisib (150 mg/kg) to U87 tumor-bearing mice

Results reported as mean ± S.D. (n = 3).

CompoundTimePlasmaNormal Brain
BrainBrain-to-Plasma RatioFree Brain-to-Free Plasma Ratio
hµMµM
GNE-31712.01 ± 0.482.50 ± 0.241.32 ± 0.480.48 ± 0.17
61.86 ± 0.932.02 ± 1.131.10 ± 0.210.398 ± 0.075
Pictilisib17.77 ± 0.260.16 ± 0.110.021 ± 0.0140.0059 ± 0.0038
65.26 ± 0.330.0669 ± 0.00600.0127 ± 0.00110.00353 ± 0.00032