TABLE 2

Cmax values, IC20 values, and maximum tested concentrations of the 18 tested drugs

Cmax values are from the literature and refer to the maximum serum concentration of the drug (Regenthal et al., 1999; Chu et al., 2007; Xu et al., 2008; Dhillon and Keating, 2009; Keisu and Andersson, 2010; Dawson et al., 2012; Sharanek et al., 2014; Schadt et al., 2015). Cells were incubated for 24 hours with different concentrations of each drug. For cytotoxicity testing, the cells were treated with varying concentrations of each drug for 24 hours and then assayed with the MTT colorimetric test and IC20 values were calculated.

DrugCmaxIC20 (24 h)Maximum In Vitro Concentration Tested
µM
Group 1: drugs involved in clinical cholestasis
 BOS7.4120100
 CPZ0.25050
 CsA1.15>30050
 NEF4.265075
 TRO6.396550
Group 2: drugs involved in rare cases of clinical cholestasis
 CIM4.940004000
 DIC8375200
 ENT3.9250100
 MET7.7430003000
 PER22520
 TAC0.096050
 TOL2370100
Group 3: drugs not involved in clinical cholestasis
 AMI0.82020
 APAP13920,00025,000
 BUS0.01>300100
 FIA0.64>300100
 PIO4.2200100
 XIM0.3>300100