TABLE 1

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.