Table 2.
Pharmacokinetic parameters for mifepristone and metabolites after administration of mifepristone plus ketoconazole (period 2, day 17) and mifepristone alone (period 1, day 12) (n = 13)
| Parameter | Mifepristone 600 mg daily + ketoconazole 200 mg twice daily | Mifepristone 600 mg alone | GMR % (90% CI) (combination/alone) |
|---|---|---|---|
| Mifepristone | |||
| C max (ng/mL) | |||
| Mean (SD) | 4325 (732) | 3448 (836) | |
| GLSM | 4265 | 3343 | 127.59 (116.66, 139.54) |
| AUC0–24 (h ng/mL) | |||
| Mean (SD) | 65,274 (15,686) | 47,473 (11,950) | |
| GLSM | 63,506 | 46,015 | 138.01 (127.12, 149.84) |
| t amax (h) | 4.25 (1.25–4.25) | 4.25 (2.25–4.25) | |
| RU 42633 | |||
| C max (ng/mL) | |||
| Mean (SD) | 2225 (947) | 2078 (714) | |
| GLSM | 2096 | 1983 | 105.73 (95.92, 116.54) |
| AUC0–24 (h ng/mL) | |||
| Mean (SD) | 45,855 (20,039) | 44,044 (15,789) | |
| GLSM | 43,081 | 42,098 | 102.33 (94.31, 111.03) |
| t amax (h) | 8.25 (0.50–11.92) | 4.25 (4.25–12.00) | |
| RU 42698 | |||
| C max (ng/mL) | |||
| Mean (SD) | 991 (285) | 596 (205) | |
| GLSM | 949 | 561 | 169.13 (156.36, 182.94) |
| AUC0–24 (h ng/mL) | |||
| Mean (SD) | 21,093 (6860) | 12,743 (4545) | |
| GLSM | 19,936 | 11,947 | 166.86 (155.06, 179.57) |
| t amax (h) | 8.25 (4.25–11.92) | 8.25 (4.25–12.00) | |
| RU 42848 | |||
| C max (ng/mL) | |||
| Mean (SD) | 1524 (389) | 1582 (353) | |
| GLSM | 1478 | 1548 | 95.48 (90.82, 100.38) |
| AUC0–24 (h ng/mL) | |||
| Mean (SD) | 33,362 (7876) | 34,840 (6537) | |
| GLSM | 32,511 | 34,266 | 94.88 (91.33, 98.56) |
| t amax (h) | 4.25 (0.00–11.92) | 12.00 (0.00–23.80) | |
GMRs and 90% CIs based on log-transformed values of AUC and C max
AUC 0–24 area under the curve from 0–24 h, CI confidence interval, C max maximum plasma concentration, GLSM geometric least squares mean, GMR geometric mean ratio, t max time to maximum plasma concentration
a t max is presented as median (range)