Mass balance results in mice, rats, rabbits, dogs, and humans after a single oral dose of [14C]apixaban
Species | Dosea | No. of Subjects | Matrix | Sampling Time | Recovery |
---|---|---|---|---|---|
h | % dose | ||||
Mouse | 30 mg/kg | 5 | Urine | 0-48 | 15.2 |
Feces | 0-48 | 83.9 | |||
Total | 0-48 | 99.1 | |||
Rat | 30 mg/kg | Intact 3 | Urine | 0-168 | 13.4 |
Feces | 0-168 | 74.0 | |||
Total | 0-168 | 87.4 | |||
BDC 3 | Bile | 0-48 | 2.6 | ||
Urine | 0-48 | 10.5 | |||
Feces | 0-48 | 69.8 | |||
Total | 0-48 | 82.9 | |||
Rabbit | 30 mg/kg | 3 | Urine | 0-48 | 1.8 |
Feces | 0-48 | 54.3 | |||
Total | 0-48 | 56.1 | |||
Dog | 5 mg/kg | 3 | Urine | 0-168 | 8.8 |
Feces | 0-168 | 73.7 | |||
Total | 0-168 | 82.5 | |||
Human | 20 mg | No bile collection 6 | Urine | 0-292 | 25.1 |
Feces | 0-292 | 56.0 | |||
Total | 0-292 | 80.5 | |||
Bile collection 4 | Bile | 3-8 | 2.4 | ||
Urine | 0-216 | 28.8 | |||
Feces | 0-216 | 46.7 | |||
|
|
| Total | 0-216 | 77.9 |
↵ a Radiospecific activities of [14C]apixaban used were 5 μCi/mg for mice, 5 μCi/mg for rats (oral), 1.5 μCi/mg for rabbits, 5 μCi/mg for dogs, and 5.4 μCi/mg for humans. Human data have been presented previously (Raghavan et al., 2009) and were included here for comparison only.