TABLE 2.
MEK Inhibitor | Dose mg/kg | Kp | Kp,uu | Reference |
---|---|---|---|---|
Trametinib | 5 (i.v.) | 0.15 | 0.15 | Vaidhyanathan et al. (2014) |
Gampa et al. (2018) | ||||
Cobimetiniba | 10 (p.o.) | 0.32 | 0.027 | Choo et al. (2014) |
E6201 | 40 (i.v.) | 2.66 | 0.14 | Gampa 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.
Kp and Kp,uu based on plasma and brain concentrations 6 hours postdose.