Table 2.
Mean (coefficient of variation, %) urine pharmacokinetic parameters of BIA 9–1106 following the first (day 1) and the last (day 8) doses of an once-daily oral regimen of opicapone (n = 6 per dose group)
| Analyte | Dose | Day | Cmax-u | tmax-u | AURC(0,t) | AmtCUM | REC |
|---|---|---|---|---|---|---|---|
| (mg) | (nmol h−1) | (h) | (nmol) | (nmol) | (%) | ||
| Opicapone | 5 | 1 | 34 (24) | 2.0 (2.0–6.1) | 114 (32) | 160 (27) | 1.3 (27) |
| 8 | 52 (23) | 2.0 (2.0–2.0) | 205 (21) | 282 (25) | 2.3 (25) | ||
| 10 | 1 | 78 (19) | 2.0 (2.0–6.1) | 270 (22) | 426 (22) | 1.8 (22) | |
| 8 | 95 (10) | 2.0 (2.0–6.1) | 305 (29) | 461 (22) | 1.9 (22) | ||
| 20 | 1 | 151 (33) | 2.0 (2.0–6.1) | 728 (34) | 992 (24) | 2.1 (24) | |
| 8 | 184 (28) | 2.0 (2.0–6.0) | 772 (48) | 1014 (37) | 2.1 (37) | ||
| 30 | 1 | 255 (39) | 2.0 (2.0–6.1) | 1411 (22) | 1616 (17) | 2.2 (17) | |
| 8 | 234 (24) | 6.0 (2.0–6.1) | 1216 (17) | 1485 (16) | 2.1 (16) |
tmax-u values are median with range of values in parenthesis. Amtcum, cumulative amount of drug excreted in urine; AURC(0,t), area under the urine excretion curve from time 0 to last observed concentration; Cmax-u, maximum drug concentration in urine; REC, percent of drug recovered in urine; tmax-u, time to Cmax-u.