Potency and incidence of human BSEP inhibition by 85 pharmaceuticals
Cholestatic/Mixed DILI | Hepatocellular DILI | No 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.