Table 3.

Pharmacokinetic parameters following 30 min intravenous infusion of GS-9219 at 0.82 mg/kg

Plasma
PBMC
t1/2 (h)Cmax (nmol/L)Tmax (h)AUC(0-∞) (nmol/L h)Total C24 (nmol/L)*
PMEGND<12.3NDND4,020 ± 4,400
cPrPMEDAP4.02 ± 0.30404 ± 912.00 ± 03,700 ± 1,140456 ± 736
GS-92190.33 ± 0.204,280 ± 1,5500.32 ± 0.162,910 ± 830NP
  • NOTE: Plasma and PBMC pharmacokinetic parameters are the mean ± SD based on n = 8 and 6 dogs, respectively. NP, not performed.

  • * Total concentration represents intracellular concentrations of parent nucleotide and all of its phosphorylated species measured following dephosphorylation.

  • ND, not determined, as plasma levels of PMEG were below level of detection.