TABLE 2

Uptake, biliary clearance, and biliary excretion of BCRP substrates in sandwich-cultured cryopreserved human hepatocytes

All compounds were tested as described under Materials and Methods. Compounds were tested at 2 μM, except for mitoxantrone (1 μM). Results are presented as the average of two separate experiments, except for lot 130 rosuvastatin (mean ± S.D. of three separate experiments).


Hepatocyte Lot

Compound

Uptakeapp

CLbile,int,app

BEI
pmol/min/mg protein μl/min/mg protein %
130 Rosuvastatin 26 ± 17 8.1 ± 3.5 58 ± 17
Mitoxantrone 22 4.5 17
QKR Rosuvastatin 31 12 45
Mitoxantrone 23 2.9 11
FEP Rosuvastatin 15 4.0 43
Topotecan 2.8 1.1 33

SN-38
3.3
3.3
51