Interaction of degarelix with human efflux and uptake transporters
Values presented are averages of two independent experiments.
| Transporter | Assay | Activation Values EC50/Compound’s Maximal Efficiency | Inhibition Values IC50/Compound’s Maximal Efficiency |
|---|---|---|---|
| µM/% | µM/% | ||
| MDR1 | ATPase | — | 19/76 |
| Calcein | — | ||
| MRP2 | ATPase | — | 76/56 |
| VT | >100/8 | ||
| BCRP | ATPase | — | 13/135a |
| VT | 48/63 | ||
| Hoechst | — | ||
| BSEP | VT | — | |
| OATP1B1 | Uptake | — | |
| OATP1B3 | Uptake | 10/68 | |
| OATP2B1 | Uptake | — |
EC50, the concentration of the compound tested to reach 50% of the compound’s own maximal efficacy; IC50, the concentration required for inhibiting the transport of the reporter substrate by 50%.
↵a Mean of duplicate determinations.