Table 2.
Summary of amenamevir plasma pharmacokinetics after a single dose
| Study | Amenamevir dose (mg) | No. | AUCinf (ng h/mL) | C max (ng/mL) | t max (h)a | t ½ (h) | CL/F (L/h) |
|---|---|---|---|---|---|---|---|
| 15L-CL-001 | 5 | 6 | 474 ± 113 | 42.9 ± 3.99 | 1.75 (1.00–3.00) | 7.75 ± 1.58 | 11.1 ± 2.88 |
| 25 | 6 | 1980 ± 303 | 177 ± 21.9 | 2.50 (1.00–4.00) | 7.42 ± 0.59 | 12.9 ± 2.04 | |
| 100 | 6 | 5870 ± 1670 | 526 ± 76.9 | 2.00 (1.00–3.00) | 7.09 ± 1.40 | 18.4 ± 5.71 | |
| 300 | 6 | 11,700 ± 1920 | 1040 ± 264 | 3.00 (2.00–4.00) | 6.88 ± 0.56 | 26.2 ± 4.49 | |
| 600 | 6 | 18,700 ± 2960 | 1680 ± 218 | 3.00 (2.00–4.00) | 6.86 ± 0.62 | 32.7 ± 4.78 | |
| Dose proportionalityb | – | 0.766 (0.718–0.814) | 0.759 (0.720–0.799) | – | – | – | |
| 15-CL-002 part 1 | Dose proportionalityb | – | 0.750 (0.714–0.785) | 0.773 (0.740–0.806) | – | – | – |
| 15-CL-002 part 2 | 300 (fasting) | 8 | 11,200 ± 3420 | 937 ± 389 | 2.00 (1.5–5.0) | 8.20 ± 1.79 | 29.2 ± 9.8 |
| 300 (fed) | 8 | 20,700 ± 4130 | 1580 ± 257 | 5.00 (3.0–5.0) | 8.45 ± 1.25 | 15.0 ± 2.8 | |
| GMRc | – | 1.90 (1.55–2.32) | 1.82 (1.34–2.48) | – | – | – |
All values are presented as the mean ± standard deviation unless otherwise stated
AUC inf area under the plasma concentration versus time curve from time zero to infinity, CL/F apparent oral clearance, C max peak drug concentration, GMR geometric least squares mean ratio (fed/fasting), t ½ terminal half-life, t max time to peak drug concentration
aThe median is presented (with the range in parentheses)
bPower model assessment of dose proportionality. The values presented are the slope (with the 95% confidence interval in parentheses)
cFor the fed/fasting condition (with the 90% confidence interval in parentheses)