TABLE 2

Plasma pharmacokinetic parameter estimates for ISIS 104838 after i.v. administration in monkey and compared across dose

Standard deviation of individual estimates (n = 3-6) are represented in parentheses.


Parameter

i.v. Bolus (mg/kg)

i.v. 1-h Infusion (mg/kg)
0.125
0.5
1
2
1
3
10
Co (μg/ml) 2.5 (0.3) 8.9 (1.6) 18.6 (1.9) 36.1 (6.3)
Cmax (μg/ml) 7.93 (1.17) 32.6 (4.35) 91.9 (14.7)
AUC (μg · h/ml) 0.49 (0.12) 2.98 (0.50) 7.27 (0.29) 20.7 (1.4) 7.87 (1.43) 45.5 (10.0) 149 (25.7)
CL (ml/h/kg) 266 (76.2) 172 (30.6) 138 (5.4) 97.1 (6.4) 131 (24.0) 68.4 (15.0) 69.0 (11.8)
Vss (ml/kg) 56.5 (1.9) 63.6 (12.1) 49.7 (1.7) 57.3 (7.3) 94.7 (16.7) 65.2 (9.4) 106 (28.9)
t½k10 (h)
0.17 (0.04)
0.33 (0.09)
0.23 (0.03)
0.37 (0.03)
0.34 (0.07)
0.55 (0.08)
0.79 (0.07)
  • Co, plasma concentration at time 0, immediately after i.v. bolus injection.