TABLE 3

In vitro parameter sets after sensitivity analyses

ParametersUnitsValuesSources
DDI conditions with CsA
 Ki_OATP1B1 of CsAµM0.014Supplemental Fig. 4A
Ki_CYP3A4 of CsAµM3.71Supplemental Fig. 4B
 FaFg of CER0.791 (control)/1 (DDI)Supplemental Fig. 4C
ka of CER/h0.789 (control)/2.5 (DDI)Supplemental Fig. 4D
 fm_CYP2C8 of CER0.85Supplemental Fig. 5D
DDI conditions with GEM
 Ki_OATP1B1 of GEMµM4.00Supplemental Fig. 5A
Ki_OATP1B1(glu)/Ki_OATP1B1(GEM)0.371Ratio of geometric mean of in vitro Ki (Supplemental Table 5)
Ki_OATP1B1 of GEM-gluµM1.48
Ki,app_CYP2C8 of GEM-gluµM26.7Supplemental Fig. 5B
kinact_CYP2C8 of GEM-glu/h4.05Supplemental Fig. 5C
fm_CYP2C8 of CER0.85Supplemental Fig. 5D
  • CsA, cyclosporine A; DDI, drug-drug interactions; GEM, gemfibrozil.