Figure 4.

Effect of ensartinib on human CYP3A4-mediated metabolic activity in HepG2-CYP3A4 cells. Cells were pre-incubated with the tested drugs for 10 min, then the reaction was initiated by adding the substrate (luciferin-IPA). The reaction was stopped after 45 min and the samples’ luminescence was measured to assess the cells’ viability. Metabolic data were normalized to viability values to compensate for possible inaccuracies caused by non-uniformity in cell growth and/or false-positive results due to drug cytotoxicity. The viability values were then re-normalized as inhibition percentages. The plotted values are means ± SD based on three independent experiments. Statistical analysis was performed using background-subtracted luminescence data normalized to viability values using one-way ANOVA followed by Dunnett’s post hoc test (** p < 0.01; *** p < 0.001; **** p < 0.0001 compared to respective vehicle control).