Compositions of imidafenacin and its metabolites in plasma, urine, and feces after a single p.o. administration of 0.25 mg of [14C]imidafenacin in healthy male subjects
Numbers in parentheses denote percentage of total radioactivity in samples.
Metabolites | Mass Transition | Retention Time | Plasma | Urine | Feces | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 2 h | 12 h | 0-4 h | 4-24 h | 0-48 h | 48-96 h | ||||||
| m/z | min | ng Eq/ml | % dose | ||||||||
| Imidafenacin | 322→240 | 21.3-21.7 | 1.19 (33.3) | 0.12 (10.7) | 2.9 (14.2) | 5.1 (13.9) | — | — | |||
| M-1 | 338→240 | 23.7 | — | — | 0.3 (1.4) | 0.2 (0.5) | — | — | |||
| M-2 | 354→240 | 26.9-27.0 | 0.34 (9.5) | 0.09 (7.6) | 2.6 (13.0) | 4.6 (12.4) | 1.8 (9.9) | 1.3 (10.9) | |||
| M-3 | 356→240 | 22.6-22.8 | 0.15 (4.1) | — | 0.3 (1.3) | 0.7 (1.9) | — | — | |||
| M-4 | 328→193 | 28.7-28.8 | 0.34 (9.4) | 0.21 (18.0) | 0.1 (0.5) | 1.3 (3.6) | — | — | |||
| M-5 | 329→193 | 24.6-24.7 | — | — | 0.5 (2.6) | 1.8 (5.0) | — | — | |||
| M-9 | 498→240 | 16.8-17.1 | 0.63 (17.6) | 0.11 (9.9) | 4.8 (23.6)a | 9.1 (24.9)a | — | — | |||
| M-10 | 298→240 | 18.7-19.4 | 0.28 (7.9)b | — | 0.7 (3.7) | 0.7 (1.9) | 1.0 (5.7) | 0.6 (4.7) | |||
| HU2, HF2 (M-11a) | 356→240 | 16.8-17.1 | — | — | 4.8 (23.6)a | 9.1 (24.9)a | 1.1 (6.2) | 0.3 (2.8) | |||
| HP1, HU3, HF3 (M-11b) | 356→240 | 18.3-18.9 | 0.28 (7.9)b | — | 4.6 (22.6) | 5.5 (14.9) | 3.9 (21.9) | 1.2 (9.7) | |||
| HU1 | 514→240 | 15.2-15.3 | — | — | 1.1 (5.6) | 2.0 (5.4) | — | — | |||
| HF1 | — | 14.7-15.0 | — | — | — | — | 0.6 (3.3) | 0.2 (1.4) | |||
| HF4 | — | 20.2-20.3 | — | — | — | — | 0.3 (1.7) | 0.8 (6.4) | |||
| HF5 | — | 21.5 | — | — | — | — | 0.6 (3.3) | 0.6 (4.8) | |||
| HF6 | — | 22.2 | — | — | — | — | 0.9 (5.1) | 0.2 (1.9) | |||
| HF7 | — | 22.7-22.9 | — | — | — | — | 0.2 (0.9) | 0.2 (1.5) | |||
| HF8 | — | 34.2-34.3 | — | — | — | — | 0.9 (4.8) | 1.2 (9.5) | |||
| Others | N.C. (2.7) | N.C. (27.3) | 2.3 (11.5) | 5.7 (15.6) | 6.6 (22.8) | 5.7 (30.8) | |||||
| Total |
|
| 3.57 (84.5) | 1.16 (73.5) | 20.2 (100) | 36.7 (100) | 17.9 (85.6) | 12.3 (84.4) | |||