Table 2.
GSK2330811 plasma PK parameters determined with noncompartmental analysis (PK population)
| PK parameter | GSK2330811 | ||||
|---|---|---|---|---|---|
| 0.1 mg kg–1 N = 6 | 0.3 mg kg–1 N = 6 | 1 mg kg–1 N = 6 | 3 mg kg–1 N = 6 | 6 mg kg–1 N = 6 | |
| AUC0–t, h*μg ml–1 | 510 (31.3) | 1427 (16.3) | 5099 (41.7) | 14 321 (21.6) | 27 187 (22.7) |
| AUC0–inf, h*μg ml–1 | 615 (26.2) | 1605 (21.6) | 5316 (42.5) | 14 656 (21.6) | 27 681 (23.3) |
| Cmax, μg ml–1 | 0.6 (32.3) | 1.5 (42.7) | 5.7 (43.5) | 19.0 (42.7) | 36.4 (22.9) |
| Vss/F, ml kg–1 | 108.44 (22.8) | 164.30 (27.5) | 127.19 (33.4) | 136.46 (42.5) | 163.23 (24.0) |
| CL/f, ml h–1 kg–1 | 0.1625 (26.2) | 0.1870 (21.6) | 0.1881 (42.5) | 0.2047 (21.6) | 0.2168 (23.3) |
| tmax, h a | 264.18 (96.0, 650.0) | 216.28 (96.0, 482.0) | 178.56 (142.3, 337.7) | 180.66 (24.0, 309.8) | 119.77 (96.0, 213.2) |
| t½, h | 462.6 (15.2) | 609.2 (13.7)b | 468.6 (15.5) | 462.1 (43.5) | 522.0 (17.0) |
a
Median (range) for tmax only, all other PK parameters are geometric mean (%CVb);
b
n = 3, as t½ could not be identified unambiguously for three subjects
AUC0–inf, area under the concentration–time curve from zero to infinity; AUC0–t, area under the concentration–time curve from zero hours to time t; Cmax, maximum observed concentration; CL/f, apparent clearance; CVb, between‐subject coefficient of variation; PK, pharmacokinetic; t½, terminal phase half‐life; tmax, time to reach the maximum observed plasma concentration; Vss/F, steady‐state volume of distribution/bioavailability