In vitro parameter sets after sensitivity analyses
| Parameters | Units | Values | Sources |
|---|---|---|---|
| DDI conditions with CsA Ki_OATP1B1 of CsA | µM | 0.014 | Supplemental Fig. 4A |
| Ki_CYP3A4 of CsA | µM | 3.71 | Supplemental Fig. 4B |
| FaFg of CER | 0.791 (control)/1 (DDI) | Supplemental Fig. 4C | |
| ka of CER | /h | 0.789 (control)/2.5 (DDI) | Supplemental Fig. 4D |
| fm_CYP2C8 of CER | 0.85 | Supplemental Fig. 5D | |
| DDI conditions with GEM | |||
| Ki_OATP1B1 of GEM | µM | 4.00 | Supplemental Fig. 5A |
| Ki_OATP1B1(glu)/Ki_OATP1B1(GEM) | 0.371 | Ratio of geometric mean of in vitro Ki (Supplemental Table 5) | |
| Ki_OATP1B1 of GEM-glu | µM | 1.48 | |
| Ki,app_CYP2C8 of GEM-glu | µM | 26.7 | Supplemental Fig. 5B |
| kinact_CYP2C8 of GEM-glu | /h | 4.05 | Supplemental Fig. 5C |
| fm_CYP2C8 of CER | 0.85 | Supplemental Fig. 5D |
CsA, cyclosporine A; DDI, drug-drug interactions; GEM, gemfibrozil.