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. 2019 Oct;47(10):1122–1135. doi: 10.1124/dmd.119.086744

TABLE 2.

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

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.

a

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