TABLE 3 

Mean oral pharmacokinetic parameters of GSK1278863 in the rat

Values are expressed as mean and S.D. of parameter, where appropriate (n = 3); serial sampling design in male Sprague-Dawley rats.

DoseCmaxTmaxaAUC0–24hAUC0–∞DNAUC0–24h
mg/kgμg/mlhμg.h/mlμg.h/mlμg.h/ml/mg/kg
1.6b2.86 ± 0.514.046.61 ± 8.95106.63 ± 19.9729.13
31.1c,d62.40 ± 3.782.0941.02 ± 68.91ND30.26
  • AUC0–24h, area under the plasma concentration-time curve within 0 to 24 hours; AUC0–∞, area under the plasma concentration-time curve from time 0 to infinity; DNAUC0-24h, dose-normalized area under the plasma concentration-time curve within 0 to 24 hours; ND, not determined since % extrapolated AUC0–∞ was high.

  • a Tmax expressed as median.

  • b Solution in 2% DMSO, 20% (w/v) Captisol in water, pH∼7.0.

  • c Suspension in 1% methylcellulose.

  • d Animals were not fasted overnight before dosing.