Average levels of circulating dabrafenib and metabolites in humans after a single oral administration of 95 mg of [14C]dabrafenib
Data are the mean (n = 4).
| Metabolite | Plasma Radioactivity | |||
|---|---|---|---|---|
| 2 h | 6 h | 10 h | 24 h | |
| % | % | % | % | |
| Dabrafeniba | 64.6 | 22.8 | 7.8 | 1.4 |
| Hydroxy-dabrafenibb | 19.4 | 18.4 | 10.8 | 1.5 |
| Carboxy-dabrafenibc | 4.1 | 34.2 | 51.1 | 44.8 |
| Desmethyl-dabrafenib | N.D. | 6.6 | 11.6 | 13.0 |
| M26d | N.D. | N.D. | 0.5 | 2.5 |
| M28/M29 | N.D. | N.D. | N.D. | N.D./N.Q |
| M30 | N.D. | N.D. | N.D. | N.D./N.Q |
| M31e | N.D. | N.D. | 0.8 | 6.0 |
| Total quantified | 88.1 | 81.9 | 82.5 | 69.1 |
N.D., not detected; N.Q., below level of quantitation by radioprofiling.
↵a Dabrafenib was quantifiable by radioprofiling only in subjects 401 (3.4%) and 404 (2.2%) at 24 hours and was not quantifiable by radioprofiling in other subjects.
↵b Hydroxy-dabrafenib was quantifiable by radioprofiling only in subjects 401 (3.6%) and 404 (2.6%) at 24 hours and was not quantifiable by radioprofiling in other subjects.
↵c Carboxy-dabrafenib was quantifiable by radioprofiling only in subjects 403 (5.3%) and 406 (11.2%) at 2 hours and was not quantifiable by radioprofiling in other subjects.
↵d M26 was quantifiable by radioprofiling only in subject 406 at 10 (1.9%) and 24 hours (10.1%) and was not quantifiable by radioprofiling in other subjects.
↵e M31 was quantifiable by radioprofiling only in subject 406 at 10 hours (3.4%) and was not quantifiable by radioprofiling in other subjects.