Blood and tissue concentrations in the liver of cyclosporine A after oral administration of doses of 10 and 50 mg/kg cyclosporine A in PXB mice and SCID mice
Data are presented as the mean from three or four animals.
| Dose | Systemic Exposure | Liver Tissue Exposure | Inlet to Liver | Reported IC50 | Reference | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Cmax | AUC | C8h | Iin,max,u | OATP1B1 | OATP1B3 | MRP2 | BCRP | MDR1 | |||
| mg/kg | μmol/l | μmol·h/l | μmol/kg tissue | μmol/l | μmol/l | ||||||
| PXB mice | 10 | 0.131 | 0.292 | 1.07 | 0.29–0.94 | ||||||
| 50 | 0.349 | 1.02 | 5.89 | 1.4–4.7 | 0.15 | 0.68 | 9.3 | 1.5 | 1.7 | ||
| SCID mice | 10 | 0.402 | 1.20 | 4.95 | 0.36–0.96 | ||||||
| 50 | 1.58 | 5.25 | 30.0 | 1.5–4.8 | Yoshida et al. (2012) | ||||||
C8h, corresponding to liver concentrations 8 hours after oral administration of rosuvastatin; MDR1, multidrug resistance protein 1.