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. 2012 May 23;75(1):118–128. doi: 10.1111/j.1365-2125.2012.04334.x

Table 2.

GSK679586 plasma pharmacokinetic parameters after single intravenous infusion of GSK679586 in healthy subjects

0.005 mg kg−1 0.05 mg kg−1 0.5 mg kg−1 2.5 mg kg−1 10 mg kg−1
(n = 3) (n = 3) (n = 6) (n = 6) (n = 6)
AUC(0,∞) (mg ml−1 h) 0.404 (6.4) 4.04 (10.5) 26.6 (10.9) 76.0 (28.6)
n = 2 n = 5 n = 6 n = 6
AUC(0,week 4) (mg ml−1 h) 0.232 (1.7) 2.56 (11.7) 16.4 (5.0) 43.0 (14.6)
n = 2 n = 6 n = 6 n = 6
Cmax (µg ml−1) 0.130 (7.6) 0.883 (0.9) 11.1 (14.4) 87.4 (15.1) 197 (22.1)
n = 2 n = 3 n = 6 n = 6 n = 6
tmax (h) 1.25 (0.50, 2.00) 4.00 (2.00, 4.00) 2.04 (1.00, 12.0) 3.00 (2.00, 12.0) 2.00 (1.00, 4.00)
n = 2 n = 3 n = 6 n = 6 n = 6
t1/2 (h) 540 (8.1) 467 (20.0) 591 (24.2) 578 (39.4)
n = 2 n = 5 n = 6 n = 6
CL (ml day−1 kg−1) 2.98 (6.3) 2.98 (10.5) 2.25 (10.9) 3.17 (28.6)
n = 2 n = 5 n = 6 n = 6
Vss (ml kg−1) 94.6 (1.2) 83.2 (9.7) 67.3 (13.9) 105 (19.3)
n = 2 n = 5 n = 6 n = 6

Values represent median (range) for tmax and geometric mean (between subject coefficient of variation, CVb%) for all other parameters.

For the 0.005 mg kg−1 dose group, AUC(0,∞), AUC(0,week 4), t1/2, CL, and Vss were not determined because none of the patients had sufficient plasma concentration data for calculation of these parameters. % AUC extrapolated was below 20% except in three subjects, two at the 0.05 mg kg−1 dose (20% and 26%) due to LLQ censoring and one subject at the 10 mg kg−1 dose (25%). AUC(0,∞), area under the plasma concentration–time curve (AUC) from time zero extrapolated to infinity; AUC(0,week 4), AUC from time zero to week 4; Cmax, maximum observed plasma concentration; tmax, time of maximum observed plasma concentration; t1/2, terminal phase half-life; CL = systemic clearance; Vss, volume of distribution at steady-state.