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. 2016 Feb 24;16:153. doi: 10.1186/s12885-016-2174-8

Table 3.

Pharmacokinetic parameters of selumetinib, by treatment combinations (75 mg bd)

Compound PK Parametersa Nb Sel + CisGem Selumetinib alone Sel vs Sel + CisGem Effect (90 % CI)e
Selumetinib AUC(0-t) (ng-hr/mL) 11 5304.37 4757.16 1.12 (0.95 to 1.30)
AUC(0-∞) (ng-hr/mL)c 11 6286.25 5653.31 1.11 (0.95 to 1.30)
Cmax (ng/mL) 11 1725.64 1331.33 1.30 (0.91 to 1.85)
Tmax (hours)d 11 1.50 1.55 0 (−1.09 to 0 .57)
N-desmethyl selumetinib AUC(0-t) (ng-hr/mL) 11 216.83 347.26 0.62 (0.43 to 0.91)
AUC(0-∞) (ng-hr/mL)c 11 277.55 452.88 0.61 (0.42 to 0.89)
Cmax (ng/mL) 11 48.41 77.16 0.63 (0.43 to 0.91)
Tmax (hours)d 11 1.62 2.00 0 (−1.13 to 0 .50)

aAnalysis used the actual time points when PK samples were collected. PK time point 0 corresponded to the time selumetinib was administered. Missing times of selumetinib dose administration were imputed from the non-missing time points. Missing concentrations for selumetinib and N-desmethyl selumetinib were estimated using linear interpolation

bOf 12 patients, 11 were evaluable for PK analysis. Patients evaluable for PK analysis included the patients for whom a PK parameter could be imputed

cLog linear models were used to extrapolate AUC (0-∞) using the last three measurements

dTmax is expressed in terms of medians

eRatio of geometric means between selumetinib and selumetinib + CisGem for AUC(0-t), AUC(0-∞) and Cmax. Rank-based difference in paired medians for Tmax