Table 1.
Inhibition of P450 17A1 activities: steady-state IC50 values
| Inhibitor | IC50, nM (95% CI limits)a |
Predicted Kib (nM) |
||
|---|---|---|---|---|
| Progesterone 17α-hydroxylation | 17α-OH pregnenolone lyase | Progesterone 17α-hydroxylation | 17α-OH pregnenolone lyase | |
| Abiraterone | 3.2 (1.7, 6.2) | 4.2 (2.6, 6.9) | 1.3 | 3.4 |
| Orteronel | 417 (256, 680) | 1060 (810, 1400) | 160 | 870 |
| Seviteronel | 3500 (2870, 4250) | 3430 (2450, 4810) | 1370 | 2810 |
| Ketoconazole | 87 (63, 120) | 227 (145, 354) | 34 | 190 |
| Clotrimazole | 60 (37, 99) | 99 (55, 176) | 23 | 81 |