Kinetic parameters for active uptake of dabrafenib metabolites by OATPs
| Hydroxy-Dabrafenib | Carboxy-Dabrafenib | Desmethyl-Dabrafenib | |||||||
|---|---|---|---|---|---|---|---|---|---|
| Km | Vmax | Pdiff,u | Km | Vmax | Pdiff,u | Km | Vmax | Pdiff,u | |
| µM | pmol/min/106 cells | µl/min/106 cells | µM | pmol/min/106 cells | µl/min/106 cells | µM | pmol/min/106 cells | µl/min/106 cells | |
| Hepatocytes | 0.99 ± 0.26 | 11 ± 2.5 | 5.1 | 2.3 ± 0.40 | 9.4 ± 0.89 | 0.092 | 1.8 ± 0.56 | 62 ± 19 | 21 |
| OATP1B1 | Not a substrate | 15 ± 3.1 | 48 ± 10 | 0.19 | Not a substrate | ||||
| OATP1B3 | Not a substrate | 3.0 ± 0.96 | 12 ± 2.6 | 0.42 | Not a substrate | ||||
| OATP1A2 | Not a substrate | 2.0 ± 1.5 | 0.88 ± 0.46 | 0.28 | Not a substrate | ||||
Pdiff,u, unbound passive diffusion clearance.