Table 4

Summary of pharmacokinetic parameters

Dose level (mg/kg)612182430
Css (μg/ml)2.88 ± 1.047.19 ± 3.129.89 ± 2.2113.38 ± 4.2419.11 ± 3.41
AUCinf (mg/h/ml)a67.0172 ± 79242 ± 43331 ± 109421 ± 138
Cl (ml/min/kg)1.491.32 ± 0.461.28 ± 0.251.35 ± 0.531.37 ± 0.70
t1/2 (min)69.679.7 ± 19.079.2 ± 16.2100 ± 19.0144 ± 22.2
% Intact at EOIb53.156.7 ± 3.056.0 ± 3.855.3 ± 3.658.2 ± 0.8
  • a EOI, end of infusion (24 h).

  • b % Intact, 100 × (ISIS 5132)/[(ISIS 5132) + (oligonucleotide metabolites)].