Relative percent distribution of radioactive metabolites in pooled plasma, urine, and fecal samples after p.o. administration of [14C]dasatinib to humans
Metabolite ID | % Distribution | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Plasma (2 h) | Urine (0–168 h) | Feces (0–168 h) | |||||||
| % Radioactivity | % Radioactivity | % Dose | % Radioactivity | % Dose | |||||
| M3a,ba | 3.3 | 6.8 | 0.2 | N.D. | N.D. | ||||
| M4 | MS | 1.3 | 0.05 | 3.1 | 2.6 | ||||
| M5 | 4.5 | 39.8 | 1.4 | N.D. | N.D. | ||||
| M6 | 3.6 | 1.3 | 0.05 | 10.4 | 8.9 | ||||
| M7 | 3.3 | 2.1 | 0.08 | N.D. | N.D. | ||||
| M8a | 3.4 | 5.5 | 0.2 | N.D. | N.D. | ||||
| M8b, M23a,ba,b | 1.4 | N.D. | N.D. | N.D. | N.D. | ||||
| M9 | N.D. | N.D. | N.D. | 1.8 | 1.5 | ||||
| M20 | 12.5 | 4.1 | 0.2 | 36.6 | 31.2 | ||||
| M21 | 9.5 | 7.8 | 0.3 | N.D. | N.D. | ||||
| M23a,b | N.D. | N.D. | N.D. | 14.7 | 12.5 | ||||
| M24 | 3.1 | 6.0 | 0.2 | 4.7 | 4.0 | ||||
| M30 | 6.9 | N.D. | N.D. | N.D. | N.D. | ||||
| M31 | 3.6 | N.D. | N.D. | N.D. | N.D. | ||||
| M34 | 1.1 | 2.3 | 0.08 | N.D. | N.D. | ||||
| M35a | 3.6 | 4.2 | 0.2 | N.D. | N.D. | ||||
| M36 | N.D. | 4.4 | 0.2 | N.D. | N.D. | ||||
| M37a,ba | 4.1 | 2.5 | 0.1 | N.D. | N.D. | ||||
| Dasatinib | 25.5 | 3.6 | 0.1 | 22.4 | 19.1 | ||||
| Total | 89.4 | 91.7 | 3.4 | 93.7 | 79.8 | ||||
MS, mass spectrometry; N.D., not detected
↵ a Metabolites (M3a,b), (M23a,b), and (M37a,b) were pairs of positional isomers that were not well resolved on HPLC
↵ b Metabolites M8b and M23a,b were not well resolved on HPLC. The percentage of distribution is the total percentage of all three metabolites