Distribution of radioactive metabolites in incubations of [14C]apixaban with hepatocytes from mouse, rat, dog, monkey, and human
Control incubations contained 0.3 to 0.7% of M7 and 2.7 to 4.4% of other unidentified peaks.
Metabolite | Mouse | Rat | Dog | Monkey | Human | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1 μM | 10 μM | 1 μM | 10 μM | 1 μM | 10 μM | 1 μM | 10 μM | 1 μM | 10 μM | ||||||||||
| % | |||||||||||||||||||
| Apixaban | 91.2 | 93.3 | 88.1 | 91.1 | 86.6 | 90.8 | 73.7 | 82.0 | 79.2 | 92.6 | |||||||||
| M1 | N.D. | N.D. | N.D. | 0.1 | N.D. | N.D. | 1.2 | 1.6 | 0.3 | 0.2 | |||||||||
| M2 | 0.7 | 0.5 | 0.5 | 0.6 | 1.4 | 1.3 | 1.4 | 1.4 | 0.8 | 0.8 | |||||||||
| M3 | 0.2 | 0.2 | N.D. | 0.3 | 0.4 | 0.2 | 0.2 | 0.4 | N.D. | 0.1 | |||||||||
| M4 | 0.1 | 0.2 | N.D. | 0.2 | 0.3 | 0.2 | 0.7 | 0.2 | N.D. | 0.1 | |||||||||
| M5 | 1.1 | 0.8 | N.D. | N.D. | 0.5 | 0.7 | 7.7 | 7.4 | N.D. | 0.4 | |||||||||
| M6 | 0.1 | 0.1 | 0.3 | 0.6 | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | |||||||||
| M7 | 0.4 | 0.4 | 0.6 | 0.6 | 0.7 | 0.6 | 1.4 | 1.7 | 0.3 | 0.6 | |||||||||
| Othersa | 6.2 | 4.5 | 10.5 | 6.5 | 10.1 | 6.2 | 13.7 | 5.3 | 19.4 | 5.2 | |||||||||
N.D., not detected.
↵ a Unidentified peaks.