TABLE 2

Percentage radioactivity of ruboxistaurin and its metabolites in plasma at 2, 4, 8, 16, 24, and 48 h postdose following a single oral administration of 10 mg/kg [14C]ruboxistaurin in female beagle dogs

Values represent mean ± S.E.


Metabolite

Mean Percentage Radioactivity
2 h
4 h
8 h
16 h
24 h
48 h
Ruboxistaurin 20.0 ± 1.4 9.9 ± 1.9 10.5 ± 1.8 15.0 ± 4.8 6.4 ± 1.3 3.4 ± 1.4
1 59.4 ± 3.8 45.9 ± 14.3 20.2 ± 5.0 39.1 ± 2.3 40.6 ± 14.3 15.4 ± 8.7
2 1.0 ± 0.1 1.1 ± 0.2 2.1 ± 0.9 1.6 ± 0.7 0.6 ± 0.4 1.5 ± 0.4
3 3.4 ± 0.3 2.3 ± 0.4 2.6 ± 0.6 1.6 ± 0.2 0.8 ± 0.5 1.5 ± 0.6
5 0.9 ± 0.1 1.4 ± 0.7 2.1 ± 0.7 1.4 ± 0.3 0.5 ± 0.4 1.3 ± 0.6
6
N.Q.
0.3 ± 0.3
2.4 ± 1.7
1.3 ± 1.1
4.2 ± 1.9
7.4 ± 4.6
  • N.Q., not quantifiable.