Table 3.
Summary of key PK parameters of ODM-203 in expansion phase (tablet formulation)
| Day 1 | Day 15 | |||||
| 200 mg | 300 mg | 400 mg | 200 mg | 300 mg | 400 mg | |
| (n=3) | (n=3) | (n=25) | (n=3) | (n=3) | (n=24) | |
| Cmax, ng/mL | 1539 (9) | 2608 (46) | 1933 (49) | 3118 (28) | 4906 (148) | 9070 (81) |
| AUC0–last, h*ng/mL | 25 886 (7) | 36 708 (46) | 30 257 (59) | 58 612 (27) | 84 233 (213) | 170 304 (90) |
| Median (min, max) Tmax, h | 8.0 (7.7 to 11.1) | 6.0 (4.1 to 6.1) | 6.3 (3.1 to 24.7) | 8.0 (6.0 to 11.2) | 6.1 (3.1 to 8.7) | 6.0 (0.0 to 23.3) |
| Accumulation ratio* | – | – | – | 2.3 (23) | 2.3 (123) | 5.5 (76) |
| Mean (SD) metabolite to parent ratio† | 0.043 (0.022) | 0.061 (0.030) | 0.048 (0.034) | 0.085 (0.043) | 0.094 (0.004) | 0.117 (0.031) |
| Mean (SD) Caverage, ng/mL | – | – | – | 2560 (719) | 5652 (5460) | 8928 (5148) |
Values expressed as geometric mean (coefficient of variation (%)) unless otherwise stated.
*Calculated by dividing ODM-203 AUC0–last on day 15 by corresponding value on day 1.
†Calculated by dividing ORM-21444 AUC0–last by corresponding ODM-203 value.
AUC0–last, area under the concentration time-curve from time zero to last sample; Caverage, average concentration in plasma after multiple dosing; Cmax, maximum observed concentration of concentration-time curve; PK, pharmacokinetics.