Sorafenib and regorafenib uptake by (A, C) HepG2 and (B, D) HuH7 cells and their (E, F) viability, as determined in cells transduced with empty lentiviral vectors (Mock) or containing the ORF of hOCT1 (hOCT1). Sorafenib and regorafenib were measured by HPLC‐MS/MS in the cells after incubating them with these compounds at 5 μM for 1 h. To determine cytotoxicity, cells were incubated with 5 μM sorafenib (with and without 250 μM quinine) or regorafenib for 6 h, and (E, F) cell viability was measured by MTT test 66 h later. Values are shown as mean ± SEM from five experiments performed in triplicate. *P < 0.05 on comparing hOCT1 versus Mock cells.