TABLE 2

Potency and incidence of human BSEP inhibition by 85 pharmaceuticals

Cholestatic/Mixed DILIHepatocellular DILINo DILI
No. with quantifiable hBSEP IC50 (%)26/42 (62)6/22 (27)8/21 (38)
Median hBSEP IC50, μM (interquartile range)35.5 (4.5–177.8)*158.5 (20.0–631.0)158.5 (100.0–354.8)
Number with hBSEP IC50 <300 μM (%)24/42 (57)4/22 (18)5/21 (24)
  • * P < 0.05 compared with the No DILI group, unpaired t test.