Table 1.
Sorafenib | Sorafenib-glucuronide | |||||
---|---|---|---|---|---|---|
Strain | Genotype | Cmax (μg/mL) | AUC (μg×h/mL) | Cmax (μg/mL) | AUC (μg×h/mL) | S-glu:Sorafenib AUC Ratio |
DBA | WT | 6.70±0.27 | 24.0±2.20 | 1.10±0.40 | 4.20±1.00 | 0.17±0.02 |
DBA | Oatp1b2(-/-) | 5.10±0.50* | 18.0±2.00 | 6.00±1.60* | 23.0±5.60* | 1.36±0.39* |
FVB | WT | 5.10±0.75 | 23.0±4.40 | 0.19±0.12 | 0.83±0.42 | 0.03±0.01 |
FVB | Oatp1a/1b(-/-) | 5.60±0.53 | 18.0±2.00 | 4.70±0.63*** | 24.0±2.30*** | 1.35±0.15*** |
FVB | OATP1B1tg | 5.60±0.59 | 16.0±1.40 | 3.30±0.40*** | 14.0±1.30*** | 0.90±0.12*** |
FVB | OATP1B3tg | 5.70±0.32 | 19.0±1.60 | 2.70±0.12*** | 12.0±1.40*** | 0.61±0.08*** |
Values are mean ± SEM. Abbreviations: AUC, Area under the curve; Cmax, maximum plasma concentration; S-glu, sorafenib-glucuronide; WT, wildtype
P<0.05
P<0.001.