TABLE 2

PK parameters for Q-1195 following intravenous and p.o. dosing in Sprague-Dawley rats

RouteDoseAUCinfCLVsst1/2%FAUCtAUCt/doseAUCt/AUCt low dose% of linear
mg/kgµM*hl/h/kgl/kgh
i.v.a1.042.30.0630.44.5
p.o.a5.01835.587
p.o.a15b4349.1
p.o.a15c5099.0
p.o.a458507.8
p.o.d5100194391.0100
p.o.d15100464312.480
p.o.d4558797184.146
  • AUCinf, area under the curve to infinity; AUCt, area under the curve to last time point; CL, clearance; %F, bioavailability; t1/2, half-life; Vss, volume of distribution at steady state.

  • a Pharmacokinetic parameters determined by noncompartment analysis.

  • b Day 1.

  • c Day 3.

  • d Pharmacokinetic parameters determined from a one-compartment model.