Amount of midostaurin and metabolites in urine (0–72 hours) and feces (0–144 hours) after a single oral dose of 50 mg [14C]midostaurin (mean ± S.D.; n = 6)
Fraction of dose metabolized after recovery correction was > 90% in both rats and dogs after an intravenous dose (Supplement Material). This correction assumes that the disposition of the unrecovered radioactivity was similar to that of the recovered activity.
| % of Dose [recovery corrected] | |
|---|---|
| Feces | |
| P15.5 | 1.67 ± 0.50 |
| P21.2 | 1.64 ± 0.34 |
| P22.6B | 0.78 ± 0.28 |
| P23.3 | 0.95 ± 0.29 |
| P25.5 | 2.17 ± 0.81 |
| P27.9 | 5.75 ± 0.97 |
| P28.8B | 4.83 ± 1.61 |
| P29.6B | 26.7 ± 4.04 [37.5] |
| P33 | 4.15 ± 0.53 |
| P33.6 | 4.94 ± 0.49 |
| P34.5 | 1.34 ± 0.46 |
| P35.3 | 2.44 ± 0.96 |
| P37.7; CGP52421 epimer 1 | 2.85 ± 0.45 [4.0] |
| P38.7; CGP62221 | 3.65 ± 0.61[5.2] |
| P39.8; CGP52421 epimer 2 | —a |
| Midostaurin | 3.43 ± 1.63 [4.8] |
| Feces | |
| Sum of metabolites (144 hours) | 63.8 [89.6] |
| Total radioactivity (144 hours) | 67.2 [94.5] |
| Total radioactivity (20 days) | 77.6 |
| Urine | |
| P6, P6B (72 hours) | 2.62 ± 0.73 |
| Midostaurin (72 hours) | 0 |
| Total radioactivity (144 hours) | 3.9 [5.4] |
| Excreta | |
| Sum of metabolites (144 hours) | 67.7b [95.2] |
| Total radioactivity (144 hours) | 71.1 [100] |
| Fraction of dose metabolized (144 hours) | 95.2 |
| Total radioactivity (20 days) | 81.6 |