Percentage of administered dose as metabolites in excreta following a single oral dose of [14C]bicifadine to mice, rats, and monkeys
Metabolite | Mice (20 mg/kg) | Rats (20 mg/kg) | Monkeys (8 mg/kg) | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Male | Female | Male | Female | Male | Female | ||||
| Urine | |||||||||
| Bicifadine | 0.8 | — | 2.1 | 5.2 | — | — | |||
| M2 | — | — | 1.0 | — | — | — | |||
| M3 | 7.5 | 6.2 | 6.5 | 4.4 | 4.3 | 3.5 | |||
| M14A-F | — | 9.7 | 2.3 | 1.2 | 11.9 | 6.3 | |||
| M27 | 3.6 | 3.7 | — | — | — | — | |||
| M12 | 0.4 | 0.5 | 0.5 | 0.2 | — | — | |||
| M9 | 38.2 | 39.1 | 36.4 | 38.2 | 31.2 | 18.3 | |||
| M31A-F | — | — | — | — | 5.8 | 2.3 | |||
| M19 | 4.5 | 3.6 | 4.4 | 1.5 | 0.2 | ||||
| M5 | — | — | 0.8 | 0.3 | — | — | |||
| M17 | — | 0.5 | 0.5 | 0.5 | — | — | |||
| M15 | — | — | 1.1 | 0.5 | — | — | |||
| M16 | — | — | 0.5 | 0.4 | — | — | |||
| M18 | — | — | 0.4 | 0.2 | — | — | |||
| M22 | — | — | 0.5 | 0.3 | — | — | |||
| M28B | 0.4 | — | — | — | — | — | |||
| M26 | 0.4 | 1.0 | — | — | 0.6 | — | |||
| Feces | |||||||||
| M3 | 6.3 | 3.7 | 16.2 | 13.9 | 3.3 | 2.5 | |||
| M9 | 9.2 | 4.3 | 9.7 | 13.0 | 2.5 | 1.7 | |||
| M26 | — | — | — | — | 0.3 | 0.2 | |||
| Bile (BDC rats only) | |||||||||
| M3 | 10.7 | 5.6 | |||||||
| M14A-F | 12.6 | 12.5 | |||||||
| M9 | 4.1 | 9.8 | |||||||
| M25 | 0.9 | — | |||||||
| M26 | 1.3 | 1.5 | |||||||
| Cage rinse | |||||||||
| M3 | 3.7 | 7.8 | |||||||
| M14A and D-F | — | 5.0 | |||||||
| M9 |
|
|
|
| 15.6 | 29.1 | |||
—, not detected.