TABLE 5

Summary of PF-06282999 pharmacokinetic parameters following daily PF-06282999 administrations for 14 days

The dosing intervals for τ are 12 hours for twice a day and 8 hours for three times a day.

ParameterThree Times a DayTwice a Day (500 mg)
10 mg30 mg100 mg250 mg
N87888
AUC0–τ (h/µg/ml)
 Geometric mean1.053.378.2619.735.6
 % CV231910136
Cmax (µg/ml)
 Geometric mean0.1980.6041.523.545.14
 % CV221817155
tmax (h)
 Median2.022.003.002.003.01
 Range2.00–3.001.00–3.982.00–4.022.00–4.003.00–4.00
Cav (µg/ml)
 Geometric mean0.1310.4221.032.472.97
 % CV231910136
Cmin (µg/ml)
 Geometric mean0.07140.2310.5841.361.15
 % CV2927112215
t1/2 (h)
 Arithmetic mean4.434.904.757.356.08
 S.D.0.880.620.203.211.14
Rac,AUC
 Geometric mean1.621.771.461.521.15
 % CV91812115
Rac,Cmax
 Geometric mean1.621.561.331.361.07
 % CV11168157
  • AUC0–τ, area under the plasma concentration-time curve over dosing interval τ; Cav, average concentration; Cmin, minimum or trough concentration; Rac,AUC, accumulation ratio over 14 days for AUC; Rac,Cmax, accumulation ratio over 14 days for Cmax; tmax, time-to-peak concentration.