Table 1.
Pharmacokinetic parameters of etamicastat, its metabolites and total radioactivity in plasma following a single 600 mg oral dose of unlabelled etamicastat and 0.623 mg [14C]-etamicastat
| Parameters | Total radioactivity [14C] | Etamicastat | BIA 5-961 | BIA 5-998 |
|---|---|---|---|---|
| AUC0–∞ (h μg ml−1)† | 97.4 (86.2–154.2) | 6.5 (5.1–8.9) | 4.2 (1.5–14.1) | 0.6* |
| %AUC (%)† | 20.5 (15.6–31.1) | 4.0 (2.1–5.4) | 3.8 (1.9–5.7) | 0.07* |
| AUC0–t (h μg ml−1)† | 75.5 (62.4–130.1) | 6.2 (4.8–8.7) | 4.1 (1.4–13.9) | 0.03 (0.003–0.05) |
| Cmax† | 2.6 (1.8–4.9) | 0.6 (0.4–0.7) | 0.5 (0.1–1.4) | 0.006 (0.005–0.04) |
| t1/2 (h) | 136.9 (113.7–169.8) | 22.9 (14.7–35.1) | 13.6 (8.3–24.0) | 0.001* |
| tmax (h) | 3.5 (3.0–4.0) | 2.0 (1.5–3.0) | 3.0 (3.0–6.0) | 4.5 (3.0–8.0) |
Data are medians (range) obtained from four healthy subjects. Abbreviations are as follows: %AUC, percentage of extrapolated plasma AUC; AUC0–∞, area under the plasma concentration–time curve from time zero to infinity; AUC0–t, area under the plasma concentration–time curve from time zero to the last sampling time at which the concentration was above the limit of quantification; Cmax, maximal plasma concentration; t1/2, terminal half-life; and tmax, time to maximal plasma concentration.
Data available for a single subject.
For total radioactivity, the units for Cmax and AUC were microgram-equivalents per millilitre and microgram-equivalents hour per millilitre, respectively.