TABLE 5

Summary of pharmacokinetic parameters for MFM and PYR in cynomolgus monkeys (n = 2) after a single oral dose of MFM (8.6 mg/kg) with and without an oral PYR dose (2.5 mg/kg)

AnalyteVariableAnimal #1Animal #2Average
MFM AloneWith PYRMFM AloneWith PYRMFM AloneWith PYR
MFMCmax (µM)11.44.821.37.816.46.3
Tmax (hour)2.03.00.82.01.42.5
AUC0-24hour (µM·h)62.624.067.234.464.929.2
AUC0-inf (µM·h)63.925.667.635.665.730.6
% Urinary excretion of dose (0–24 hours)57.925.550.837.054.530.8
CLR (ml/min/kg)10.111.18.411.69.211.3
T1/2 (hour)4.05.53.14.53.65.0
PYRCmax (nM)227265246
Tmax (hour)4.04.04.0
AUC0-25hour (nM·h)338140333707
C25 hour (nM)122126124
T1/2 (hour)30.722.926.8
  • Data from individual animal are shown (n = 2 animals). The pharmacokinetic parameters were determined as indicated under Materials and Methods. PYR was orally dosed 60 min before MFM.