Tyrosine Kinase Inhibitor (TKI) Concentrations Used to Assess Bile Acid-dependent Hepatotoxicity.
| TKI | Cmaxa,b (μM) | Dose (mg) | Conc. 1 (μM, X-fold Cmax) | Conc. 2 (μM, X-fold Cmax) | Conc. 3 (μM, X-fold Cmax) |
|---|---|---|---|---|---|
| Dasatinib | 0.18 | 100 BID | 0.18 | 1.8 (10X) | 9.0 (50X) |
| Pazopanib | 132.80 | 800 QD | 0.66 (0.005X) | 6.6 (0.05X) | 66.4; 33.2 (0.5X; 0.25X) |
| Sorafenib | 4.30 | 400 BID | 0.43 (0.1X) | 4.3 | 43.0 (10X) |
a Cmax represents the highest mean or median steady-state total plasma concentration reported by the US FDA following chronic dosing.
b (Zhang et al., 2017).