IVIVC of inhibition of hepatocyte uptake of pitavastatin
| AUCR (Observed or Predicted) | AUCR with Pitavastatin as the Substrate Drug in the Presence of Inhibitor Drugs | |
|---|---|---|
| Rifampicin | Cyclosporine | |
| Observed in vivo AUCR | 5.8a | 4.6b |
| Predicted AUCRs | ||
| HUM4122D (SCHH) | 2.4 | 2.2 |
| HU1651 (SCHH) | 1.9 | 1.9 |
| HUM4122D (suspension) | 2.9 | 2.5 |
| HUP1001 (suspension) | 2.2 | 2 |
| Simulated AUCRs (the RAF of each transporter was multiplied by an SF) | ||
| SF = 10 | 5.3 | 4 |
| SF = 15 | 5.8 | 4.2 |
↵a The AUCR of pitavastatin in the presence of rifampicin is 5.1–6.7 based on data from three studies conducted across three different populations. The AUCR of 5.8 was observed in the Caucasian population and was considered to be the benchmark in this study (Prueksaritanont et al., 2014).
↵b The AUCR of pitavastatin in the presence of cyclosporine is based on data provided on the Livalo label (can be accessed on the U.S. Food and Drug Administration website at https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=022363).