Table 2.
Summary of selected pharmacokinetic parameters for plasma dolutegravir, plasma radioactivity, and blood radioactivity in healthy male human subjects after a single oral 20-mg (80-μCi) dose of [14C]dolutegravir as a suspensiona
| Analyte | n | Cmax (μg/ml) | Tmaxb (h) | AUC0–t (μg · h/ml) | AUC0–∞ (μg · h/ml) | CL/F (liter/h) | Vz/F (liter) | t1/2 (h) |
|---|---|---|---|---|---|---|---|---|
| Plasma dolutegravir | 6 | 2.57 (24) | 0.50 (0.50–2.00) | 35.7 (12) | 35.9 (12) | 0.56 (12) | 12.5 (9) | 15.6 (16) |
| Plasma radioactivity | 6 | 2.46 (24) | 0.50 (0.50–1.50) | 35.9 (11) | 36.1 (11) | NR | NR | 15.7 (14) |
| Blood radioactivity | 6 | 1.13 (25) | 1.25 (0.50–2.00) | 17.7 (13) | 18.4 (13) | NR | NR | 14.6 (12) |
a
Values are geometric mean (percent coefficient of variation) unless otherwise stated; NR, not reported. CL/F, apparent oral clearance; Tmax, time to Cmax; Vz/F, apparent volume of distribution.
b
Median (range).