Distribution of radioactive metabolites after a 4-h incubation of [14C]ticagrelor (20 μM) with hepatocytes from rat, dog, and human
| Metabolites | Percentage of Total Radioactivity | ||
|---|---|---|---|
| Rat | Dog | Human | |
| Ticagrelor | 69.0 | 37.8 | 42.0 |
| M5 (AR-C133913) | 4.8 | 6.4 | 18.1 |
| M7a | 1.7 | ND | ND |
| M7b | 0.5 | 0.2 | 0.5 |
| M8 (AR-C124910) | 10.1 | 1.9 | 20.3 |
| M6aa | ND | 6.2 | ND |
| M6ba | ND | NQ | 6.1 |
| M9a | 1.4 | 11.5 | 1.6 |
| M9bb | ND | 28.2 | ND |
| M10b | 3.5 | 0.2 | 0.4 |
| M12 | ND | ND | 0.5 |
| M13 | 2.1 | 3.3 | 5.4 |
| Othersc | 6.9 | 4.3 | 5.1 |
ND, not detected; NQ, detected by LC-MS/MS only, not quantifiable by radiodetector.
a Metabolites M6a and M6b were proposed as a glucuronide conjugate of AR-C124910 with a different retention time.
b Metabolite M9b was proposed as a glucuronide conjugate of parent with a different retention time as M9a.
c Sum of all other minor metabolites.