TABLE 2

Summary of pevonedistat uptake in plated human hepatocytes

InhibitorUptake Rate
(pmol/min/mg protein) (mean±SD)
Percent Control
(%) (mean±SD)
Lot 8317Lot 8339Lot 8350Lot 8317Lot 8339Lot 8350
KHB, 37°C262.5 ± 29.9657.1 ± 13.3432.5 ± 42.5NANANA
KHB, 4°C137.2 ± 8.7158.5 ± 27.2180.8. ± 22.0NANANA
Rifamycin SV (20µM)301.7 ± 25.1436.3 ± 12.9422.9 ± 77.3131.3 ± 20.055.7 ± 2.696.2 ± 30.7
CsA (20 µM)306.8 ± 38.5443.1 ± 27.5454.6 ± 9.8135.3 ± 30.757.1 ± 5.5108.8 ± 3.9
Verapamil (300 µM)414.2 ± 24.0528.5 ± 8.6680.8 ± 47.4221.1 ± 19.174.2 ± 1.7198.7 ± 18.8
Ketoprofen (300 µM)368.9 ± 49.7470.6 ± 11.5733.2 ± 90.2184.9 ± 39.762.6 ± 2.3219.5 ± 35.9
NBMPR (10 µM)358.4 ± 33.5484.0 ± 22.5538.4 ± 39.4176.6 ± 26.765.3 ± 4.5142.1 ± 15.7
Rifamycin SV (1 mM)260.5 ± 5.2265.9 ± 10.7346.6 ± 21.698.4 ± 4.221.5 ± 2.165.9 ± 8.6
Choline330.0 ± 30.2582.7 ± 33.2449.9 ± 25.6153.9 ± 24.185.1 ± 6.7106.9 ± 10.2