TABLE 4

Comparison of half-maximal inhibitory concentrations, IC50, determined in vitro using either atorvastatin or an endogenous substrate

CompoundOATP1B1OATP1B3OATP2B1
IC50
AtorvastatinIC50
E17βGaIC50
AtorvastatinIC50
E17βGaIC50
AtorvastatinIC50
E3Sa
µM
Atazanavir0.96 ± 1.21.4 ± 1.017 ± 1.30.40 ± 1.2>405.2 ± 1.2
Cyclosporine1.5 ± 1.21.4 ± 1.23.1 ± 1.41.3 ± 1.0>1837 ± 1.6
Rifampicin5.0 ± 1.21.2 ± 1.2190 ± 1.71.5 ± 1.1>63065 ± 1.2
  • E17βG, estradiol-17β-glucuronide; E3S, estrone-3-sulfate.

  • a IC50 values reprinted with permission from Karlgren et al. (2012b). Copyright 2012 American Chemical Society.