Table I.
Dose, mg | Panel | N | AuC0-∞, nM·ha
|
Cmax, nMa
|
Tmax, h
|
Apparent t1/2, h
|
||||
---|---|---|---|---|---|---|---|---|---|---|
GM | 95% CI | GM | 95% CI | Median | Minimum-Maximum | HM | Pseudo-SD | |||
10 | A | 6b | 147 | 96-224 | 91 | 61-135 | 0.75 | 0.50-1.50 | 1.05 | 0.63 |
20 | A | 6 | 244 | 162-368 | 163 | 110-241 | 0.50 | 0.25-1.00 | 1.36 | 0.93 |
40 | A | 6 | 396 | 263-597 | 287 | 193-426 | 0.75 | 0.50-1.00 | 1.31 | 0.53 |
40 | B | 6 | 716 | 465-1100 | 471 | 312-711 | 1.00 | 0.25-1.50 | 1.95 | 0.42 |
40, fed | B | 6 | 815 | 530-1260 | 282 | 187-426 | 2.50 | 0.25-4.00 | 2.06 | 0.56 |
80 | A | 6 | 1170 | 777-1760 | 738 | 497-1100 | 1.00 | 0.50-1.50 | 1.74 | 0.63 |
80, obese | C | 8 | 1860 | 1250-2760 | 836 | 574-1220 | 1.25 | 0.50-2.00 | 2.55 | 0.71 |
120 | B | 6 | 3370 | 2190-5170 | 1270 | 846-1920 | 1.25 | 0.50-2.00 | 2.28 | 0.66 |
120, obese | C | 6 | 3540 | 2330-5370 | 1250 | 835-1880 | 1.25 | 0.50-2.00 | 2.72 | 0.54 |
160 | A | 6 | 3000 | 1990-4520 | 1280 | 860-1900 | 0.75 | 0.50-1.00 | 2.21 | 0.65 |
160 | B | 6 | 4460 | 2900-6860 | 1830 | 1220-2770 | 1.00 | 1.00-1.50 | 2.22 | 0.57 |
GM, geometric mean; HM, harmonic mean.
Back-transformed least squares mean and 95% confidence interval (CI) from mixed-effects model performed on natural log-transformed values.
n = 5 for t1/2 and AUC0-∞ at this dose because one patient had concentrations below the limit of quantitation.