TABLE 1

Plasma pharmacokinetic parameter estimates for ISIS 104838 after i.v. bolus administration and compared across species

Standard error of the estimate values are shown in parentheses.


Parameter

Mouse (5 mg/kg)

Rata (5 mg/kg)

Dog (2 mg/kg)

Monkey (2 mg/kg)
A (μg/ml) 37.1 (13.0) 43.5 (3.12) 31.1 (1.1) 36.1 (6.3)
B (μg/ml) 0.9 (0.7) 3.5 (1.5)
C (μg/ml) 0.4 (0.3)
t1/2α (h) 0.097 (0.024) 0.25 (0.03) 0.37 (0.01) 0.37 (0.01)
t1/2β (h) 0.79 (0.47) 1.9 (1.2)
t1/2γ (h) 11.1 (8.8)
Co (μg/ml) 37.9 (13.2) 47.4 (3.4) 31.1 (1.1) 36.1 (2.6)
AUC (μg · h/ml) 6.2 (1.2) 32.1 (2.5) 16.7 (0.7) 20.7 (0.6)
CL (ml/h/kg) 809 (153) 93.6 (7.2) 121 (4.9) 97.1 (2.6)
Vss (ml/kg) 242 (103) 413 (243) 64.7 (2.4) 57.3 (3.0)
t1/2K10 (h)
0.11 (0.03)
0.47 (0.05)
0.37 (0.01)
0.37 (0.01)
  • Co, plasma concentration at time 0, immediately after i.v. bolus injection.

  • a Radiolabel data (uses μg-Eq of [3H]ISIS 104838).