TABLE 3

Comparison of initial rate of hepatocyte uptake in the presence or absence of Rif SV

Substrates were incubated in the presence or absence of the inhibitor Rif SV (100 μM) for passive and active uptake or in the buffer with or without Ca2+ for in vitro biliary clearance (CLbile). Data are presented from single studies run in duplicate or triplicate. A minimum of two experiments were performed on different days to verify coefficient of variation <15%.

SubstratesTransporters/Enzymes InvolvedControlRif SV (100 μM)Active Hepatic Uptake
PSuptakeCLbilePSpassiveCLbile
μl · min1 · mg protein1%
MidazolamCYP3A4280.029∼00.0
BuprenorphineUGT390.043∼00.0
TCNTCP4216.37.03.483.2
RosuvastatinOATP1B1, OATP1B39.32.51.20.693.0