Examining the potential of CP-671,305 as a substrate for human biliary transport proteins
Data (mean ± S.D.) are from three independent determinations.
CP-671,305 | Papp × 10−6 A→B | Papp × 10−6 B→A | Efflux Ratio BA/AB | ||
|---|---|---|---|---|---|
| μM | cm/s | ||||
| Parental MDCK | 2.0 | 0.70 | 0.60 | 0.85 | |
| MDCK/MDR1* | 2.0 | 0.70 ± 0.03 | 0.40 ± 0.01 | 0.60 | |
| MDCK/ABCG2/BCRP* | 2.0 | 0.60 ± 0.02 | 5.70 ± 0.20 | 9.50 | |
| MDCK/ABCC2/MRP2* | 2.0 | 1.00 ± 0.04 | 7.00 ± 0.10 | 7.00 | |
↵* MDR1, BCRP, and MRP-2 substrate properties were examined in the MDCK II cell line stably transfected with MDR1, BCRP, or MRP-2 genes, respectively.