Table 1. PK parameters of naloxegol and radioactivity in plasma and whole blood (n = 6).
| Parametera | Plasma naloxegol | Plasma radioactivity | Whole blood radioactivity |
|---|---|---|---|
| AUC0–∞, ng×h/mL | 233 (61.9) | 710 (49.2) | 392 (44.2) |
| Cmax, ng/mL | 51.1 (38.3) | 84.8 (40.3) | 57.5 (40.8) |
| tmax, hb | 1.74 (0.25 – 3.02) | 2.23 (0.50 – 4.02) | 2.20 (0.50 – 4.02) |
| t1/2, h | 7.88 (46.4) | 7.28 (41.4) | 3.66 (27.5) |
| λz, h–1 | 0.0880 (46.5) | 0.0952 (41.4) | 0.190 (27.5) |
| Vz/F, L | 1,320 (54.6) | 399 (25.2) | 364 (22.6) |
| CL/F, L/h | 116 (61.9) | 38.0 (49.3) | 69.0 (44.3) |
λz = terminal elimination rate constant; AUC0–∞ = area under the curve from time zero extrapolated to infinity; CL/F = apparent oral clearance; Cmax = maximum concentration; PK = pharmacokinetic; tmax = time to maximum plasma concentration; t1/2 = apparent elimination half-life; Vz/F = apparent volume of distribution. aValues are geometric mean (geometric coefficient of variation in percent) unless otherwise noted. bValues are median (min, max).