TABLE 2

Comparison of brain distribution of MEK inhibitors in wild-type mice (data are presented as means)

MEK InhibitorDose mg/kgKpKp,uuReference
Trametinib5 (i.v.)0.150.15Vaidhyanathan et al. (2014)
Gampa et al. (2018)
Cobimetiniba10 (p.o.)0.320.027Choo et al. (2014)
E620140 (i.v.)2.660.14Gampa et al. (2018)
  • MEK, mitogen-activated protein kinase enzyme; Kp (AUC ratio), the ratio of AUC(0-t,brain) to AUC(0-t,plasma) using total drug concentrations; Kp,uu (AUC ratio), the ratio of AUC(0-t,brain) to AUC(0-t,plasma) using free drug concentrations.

  • a Kp and Kp,uu based on plasma and brain concentrations 6 hours postdose.