Values used for model simulations and resulting predicted steady-state rosuvastatin concentrations and partitioning

Clearance parameters were scaled from those determined in the in vitro model to represent those in the liver of a 5-kg monkey. Volumes for the extracellular and intracellular compartments were fixed to those of the plasma and liver, respectively, of a 5-kg monkey. Extracellular and intracellular fu were fixed to those measured in monkey plasma and liver, respectively. The initial condition for CEC and CIC was arbitrarily fixed to 1 and 0 µM, respectively.

Scaled in vitro model parameters8210100.
Corrected for transporter expression8211470.
Corrected for cell surface area1410100.120.120.0111.67474
Active uptake not limited by binding8210100.12a0.120.0151.6106106
  • EC = extracellular; IC = intracellular.

  • a Removed from Clup.