Table 1.

Pharmacokinetic variables for free and liposomal LAQ824 in rats

Formulationt1/2 (h)AUC (μg × h/mL)CL (mL/h)Vd (mL)MRT (h)
Free LAQ8240.213.6737.28081.1
Ls-LAQ824 (TEA8SOS)*10.82198.54.570.715.5
  • NOTE: The data used to calculate the pharmacokinetic variables for LAQ824 when formulated either in the free form or liposomal form refers to the actual drug concentrations measured in the blood that were then used to calculate the %ID values found in the corresponding curves for Fig. 3B.

    Abbreviations: AUC, area under the concentration versus time curve in plasma based on the sum of exponential terms; MRT, mean residence time calculated from exponential terms; CL, clearance calculated from exponential terms; Vd, volume of distribution.

  • * The liposomal LAQ824 formulation examined was prepared from DSPC/cholesterol/PEG-DSG (3:2:0.3, mol/mol/mol) and loaded with LAQ824 at a ratio of 200 g LAQ824/mol phospholipid using the TEA8SOS gradient loading method as described in Materials and Methods.