TABLE 4

Percentage of dose excreted (volanesorsen and volanesorsen equivalent) for mice, monkeys, humans, and rats

SpeciesDose LevelDoseStudy DayTime PointSum of OligonucleotideDose Excreted TotalDose Excreted Parent
µMµM%%
Mouse80 mg/kg0.27917624 h0.129a46.4a37.6a
0.285a101.9a84.2a
Mean0.20774.260.9
Mouse80 mg/kg0.27917748 h0.03110.93.65
0.06121.75.75
Mean0.04616.34.7
Monkey20 mg/kg6.97925324 h1.43820.61.60
0.4055.810.99
1.09515.75.39
Mean (S.D.)0.980 (0.526)14.0 (7.5)2.7 (2.4)
Monkey20 mg/kg6.97925448 h0.5397.720.89
0.0771.100.41
0.5427.763.08
Mean (S.D.)0.386 (0.267)5.5 (3.8)1.5 (1.4)
Human400 mg55.832124 h17.01630.50.52
8.54215.30.23
12.00921.50.13
4.7378.480.29
Mean (S.D.)10.58 (3.64)18.9 (6.5)0.3 (0.1)
Human400 mg55.8322224 h2.3564.220.78
15.55327.94.96
9.75217.53.95
Mean (S.D.)9.22 (6.61)16.5 (11.8)3.2 (2.2)
Rat5 mg/kg0.349124 h0.04312.50.33a
0.04512.9NA
0.04412.5NA
Mean (S.D.)0.044 (0.001)12.6 (0.2)NA
Rat25 mg/kg1.745124 h0.39922.92.09
0.34119.61.34
Mean0.37021.21.7
  • a Samples were a pool of three individuals.