Summary of human pharmacokinetic parameters of GSK2251052, M3, and total radioactivity after a single i.v. infusion dose of [14C]GSK2251052 (1500 mg)
| Matrix | Analyte | AUC(0-t)a | AUC(0-∞)a | Cmaxa | CLa | Vssa | T1/2b | Tmaxb |
|---|---|---|---|---|---|---|---|---|
| µg ⋅ h/ml | µg.h/ml | µg/ml | l/h | l | h | h | ||
| Plasma | GSK2251052 | 72.3 (7.34) | 72.5 (7.41) | 24.6 (14.5) | 20.7 (7.41) | 197 (8.87) | 11.6 (9.96–12.1) | 0.917 (0.50–0.92) |
| M3 | 101 (12.1) | 103 (12.1) | 1.77 (9.77) | NA | NA | 77.3 (68.1–78.5) | 7.00 (5.00–24.0) | |
| Radioactivity | 191 (10.0) | 195 (9.90) | 24.3 (16.1) | 7.70 (9.90) | 348 (12.6) | 96.0 (86.2–117) | 0.917 (0.92–0.92) | |
| Whole blood | Radioactivity | 141 (20.8) | 193 (21.1) | 43.7 (10.2) | 7.79 (21.1) | 116 (17.8) | 14.3 (7.28–16.1) | 0.917 (0.92–0.92) |