Induction parameters of esaxerenone and reference compounds on CYP2B6 and CYP3A4
Primary cultures of fresh human hepatocytes from three donors were used. Parameters were calculated using the fold induction of metabolic activity for CYP2B6 and mRNA for CYP3A4. Parameters for CYP1A2 were not calculated, because the induction potential of esaxerenone was not observed.
| No. 1 | No. 2 | No. 3 | Mean ± S.D. | |||
|---|---|---|---|---|---|---|
| CYP2B6 | Esaxerenone | Emax | 15.5 | 5.52 | 6.57 | 9.21 ± 5.51 |
| EC50 (μM) | 4.70 | 7.64 | 21.0 | 11.1 ± 8.7 | ||
| Phenobarbital | Emax | 215 | 8.98 | 51.4 | 91.8 ± 108.8 | |
| EC50 (μM) | 5170 | 968 | 12,700 | 6280 ± 5940 | ||
| CYP3A4 | Esaxerenone | Emax | 61.2 | 26.9 | 24.0 | 37.4 ± 20.7 |
| EC50 (μM) | 16.4 | 4.10 | 10.9 | 10.5 ± 6.1 | ||
| Rifampicin | Emax | 171.5 | 54.3 | 18.9 | 81.6 ± 79.9 | |
| EC50 (μM) | 8.57 | 0.566 | 0.709 | 3.28 ± 4.58 |