TABLE 1

Study designs, experimental conditions, and measured endpoints for the in vivo studies

StudyDoseFormulationMouse StrainCollected SamplesMeasured Endpoints
mg/kg
Pharmacokinetics25MCTCD1, femalePlasma, brainGDC-0084 concentrations
PD modulation (pAkt, pS6)
MALDI imaging15MCTCD-1 Nude, female intracranial tumor-bearingBrainGDC-0084 brain distribution
Efficacy15MCTCD-1 Nude, female intracranial tumor-bearingPlasma, brain, tumorsTumor volumes
GS2 tumors: GDC-0084 plasma, brain and tumor concentrations, PD modulation
  • MCT, 0.5% methylcellulose/0.2% Tween 80; PD, pharmacodynamic.