Transporter | Substrate | IC50 | Substrate | IC50 |
---|---|---|---|---|
µM | µM | |||
OATP1B1 | [3H]EG | 11 | Rosuvastatin | 26 |
OATP1B3 | [3H]EG | 60 | Rosuvastatin | 51 |
OATP1A2 | [3H]ES | 7.4 | Rosuvastatin | 1.8 |
OATP2B1 | [3H]ES | NCa | Rosuvastatin (pH 7.4) | 16 |
Rosuvastatin (pH 6.0) | 12 | |||
BCRP | [3H]ES | No inhibition | Rosuvastatin | NCb |
MRP3 | [3H]EG | No inhibition | Rosuvastatin | ND |
MRP4 | [3H]EG | NCc | Rosuvastatin | NCd |
NC, not calculated (data insufficient to determine IC50); ND, rosuvastatin uptake into MRP3 vesicles was not detected (IC50 not determined).
↵a Ronacaleret inhibited OATP2B1 transport of [3H]ES in vitro by 49% at a concentration of 100 µM.
↵b Ronacaleret inhibited human BCRP transport of rosuvastatin in vitro by 20% at the highest test concentration of 100 µM.
↵c Ronacaleret inhibited human MRP4 transport of [3H]EG in vitro by 25% at the highest test concentration of 100 µM.
↵d Ronacaleret inhibited human MRP4 transport of rosuvastatin in vitro by 31% at the highest test concentration of 100 µM.