Table 7

AN3365 murine pharmacokinetic parameters

ParameteraValue
i.v. (30 mg/kg)b
    Cmax (μg/ml) at 5 min26.0
    CL (ml/h/kg)2914
    Vc (ml/kg)805
    Vss (ml/kg)3895
    MRT (h)1.34
    AUC (h · μg/ml)10.3
    α-t1/2 (h) (% AUC)0.12 (62)
    β-t1/2 (h) (% AUC)2.23 (38)
p.o. (30 mg/kg)c
    Cmax (μg/ml)0.90
    Tmax (h)0.5
    AUClast (h · μg/ml)2.2
    Terminal t1/2 (h)2.7
    % bioavailability21
    % plasma protein binding7.6
s.c. (30 mg/kg)c
    Cmax (μg/ml)8.4
    Tmax (h)0.25
    AUClast (h · μg/ml)12.1
    Terminal t1/2 (h)2.5
    % bioavailability100
  • a CL, clearance; Vc, volume of distribution of central compartment; Vss, volume of distribution at steady state; MRT, mean residence time; α-t1/2, alpha-phase half-life; β-t1/2, beta-phase phase half-life; Tmax, time to maximum drug concentration; Terminal t1/2, half-life of the drug after reaching pseudo-equilibrium.

  • b WinNonlin two-compartment analysis with 1/y2 weighting.

  • c WinNonlin noncompartment analysis with uniform weighing.