Figure 3

Intracellular drug accumulation in the absence (Kp) and presence (Kp_cyto) of chloroquine (a) and intracellular drug bioavailability (F_ic) and cytosolic bioavailability (F_cyto) (b) of the tested inhibitors in hepatocytes. The signs within brackets in (a) denote charge at physiological pH. Lipophilic cationic drugs showed higher Kp than Kp_cyto. The neutral drugs telithromycin and pazopanib had comparable Kp and Kp_cyto, while nilotinib displayed higher Kp than Kp_cyto, likely due to precipitation and accumulation in the lysosomes²⁶. The numbers in (b) refer to the inhibitors listed in (a). Results are given as geometrical means (a,b) ± standard deviation (a) of triplicate measurements.