Distribution of radioactive metabolites after a 1-h incubation of [14C]ticagrelor (20 μM) with microsomes from mouse, rat, dog, marmoset, cynomolgus monkey, and human
| Metabolites | Percentage of Total Radioactivity | |||||
|---|---|---|---|---|---|---|
| Mouse | Rat | Marmoset | Dog | Cyno Monkey | Human | |
| Ticagrelor | 55.2 | 95.8 | 81.5 | 88.0 | 39.9 | 88.4 |
| M1 and M2a | ND | ND | ND | ND | 1.1 | ND |
| M5 (AR-C133913) | 5.8 | 1.9 | 8.7 | 2.3 | 18.7 | 3.4 |
| M7a | 1.8 | ND | ND | ND | 0.7 | ND |
| M7b | 1.0 | ND | ND | ND | 0.7 | ND |
| M8 (AR-C124910) | 24.6 | 0.9 | 6.0 | 7.1 | 28.4 | 4.5 |
| M10b | 3.1 | ND | 0.4 | 0.2 | 0.2 | 0.1 |
| M12 | 0.6 | ND | 0.1 | ND | 2.2 | ND |
| M13 | 0.3 | 0.5 | 0.4 | 0.3 | 0.9 | 0.2 |
| Othersb | 7.6 | 0.9 | 2.9 | 2.1 | 7.2 | 3.4 |
ND, not detected.
a M1 and M2 coeluted together.
b Sum of total other minor metabolites.