TABLE 2

Pharmacokinetics of SGX523 in cynomolgus monkeys and the urinary excretion of SGX523 and metabolite M11

Male cynomolgus monkeys (n = 2 for each route of administration) received a single intravenous or oral dose of SGX523 after an overnight fast using a parallel study design. SGX523 and M11 concentrations in plasma and urine samples were determined by LC/MS/MS analysis.

RouteDoseMatrixParameterValue
Intravenous1.6 mg/kgPlasmaCL (l/h/kg)0.22
PlasmaVdss (l/kg)0.65
PlasmaHalf-life (h)4.1
Urine% of dose excreted as intact SGX5230.2
Oral6.2 mg/kgPlasmaCmax (μM)4.8
Plasma%F39
UrineConcentration of SGX523 (μM)0.4
UrineConcentration of M11 (μM)29.2