Table 1.
Transactivational activity of vilaprisan
| Antagonistic activity IC50 (nmol/L) | ||||||
|---|---|---|---|---|---|---|
| Progesterone receptor A | Progesterone receptor B | Glucocorticoid receptor | Androgen receptor | Estrogen receptor α | Estrogen receptor β | |
| Vilaprisan (mean ± SD) | 0.09 ± 0.0005 | 0.095 ± 0.001 | 957 ± 42 | 47 ± 32 | No effect | No effect |
| Reference compound (mean ± SD) |
Mifepristone 0.023 ± 0.02 |
Mifepristone 0.02 ± 0.008 |
Mifepristone 6 ± 0.5 |
OH-flutamide 21 ± 9 |
Fulvestrant 2.0 ± 0.6 |
Fulvestrant 2.7 ± 0.7 |
IC50 half maximal inhibitory concentration, OH-flutamide hydroxyflutamide, SD standard deviation [8]