TABLE 4

Distribution of radioactive metabolites in urine and feces after an oral dose of [14C]apixaban to intact mice, rats, rabbits, dogs, and humans

Data are for human subjects without bile collection and for intact rats. Human data have been presented previously (Raghavan et al., 2009) and are included here for comparison.

Metabolite
Mouse
Rat
Rabbit
Dog
Human
Urine
Feces
Urine
Feces
Urine
Feces
Urine
Feces
Urine
Feces
%
Apixaban 13.6 73.2 12.1 65.9 0.04 39.4 7.2 58.6 21.5 34.0
M1 Trace N.D. Trace N.D. 0.1 0.4 Trace N.D. 1.6 1.2
M2 0.5 5.9 0.2 2.9 1.4 13.4 0.7 9.4 N.D. 12.2
M3 N.D. N.D. N.D. N.D. N.D. N.D. Trace 0.7 N.D. N.D.
M4 0.1 0.5 0.3 0.4 N.D. 0.2 0.1 0.7 N.D. 0.4
M7 0.1 3.5 0.2 2.2 N.D. 0.1 0.3 2.5 1.5 3.7
M8 N.D. N.D. Trace N.D. N.D. N.D. 0.2 0.2 N.D. N.D.
M9 Trace N.D. Trace 0.3 N.D. N.D. N.D. N.D. N.D. N.D.
M10 Trace N.D. N.D. N.D. N.D. N.D. N.D. N.D. N.D. 0.1
M13 0.5 N.D. N.D. N.D. N.D. N.D. N.D. N.D. N.D. 3.1
Othersa 0.3 0.8 0.2 0.1 0.7 0.1 0.1 0.2 N.D. 1.3
Totalb
15.2
83.9
13.0
71.8
1.8c
54.3
8.6
72.3
24.5
56.0

  • N.D., not detected; Trace, radioactive peak observed but <0.1%.

  • ↵ a Unidentified components.

  • ↵ b Total was <100% because of unidentified minor peaks, each representing <0.1%.

  • ↵ c Including M14 (0.22%) and M16 (0.03%).