Pharmacokinetic parameters of TRA, dasatinib, and metabolite M5 after a single p.o. solution dose of 100 mg (120 μCi) of [14C]dasatinib to healthy subjects
Cmax/Geometric Mean (CV %) | AUC(INF)/Geometric Mean (CV %) | AUC(0-T)/Geometric Mean (CV %) | Tmax/Median (Min, Max) | T-HALF/Mean (S.D.) | CLR/Mean (S.D.) | UR/Mean (S.D.) | |
|---|---|---|---|---|---|---|---|
| ng/ml | ng · h/ml | ng · h/ml | h | h | ml/h | % | |
| TRA (n = 7)a | 224.6a (23) | –b | 400.4 (41)c | 0.5 (0.25, 1.5) | –b | 3.58 (1.17) | |
| Dasatinib (n = 8) | 104.5 (29) | 313.9 (42) | 298.8 (44) | 0.5 (0.25, 1.5) | 3.6 (1.0) | 404.8 (168.7) | 0.12 (0.05) |
| M5 (n = 8) | 2.9 (55) | 15.3 (53) | 8.9 (74) | 1.5 (0.75, 3) | 3.2 (1.2) |
| 1.2 (0.49) |
↵ a n = 7 because one subject had no quantifiable levels of TRA in plasma. The limits of quantitation in plasma for radioactivity ranged from 132 to 152 ng-Eq/ml
↵ b The AUC(INF) and T-HALF for radioactivity was not calculated because radioactivity was measurable only up to 4 h
↵ c n = 6 because one subject had no quantifiable levels of TRA in plasma and the extrapolated AUC could not be estimated in a second subject