TABLE 5

Comparison of simulated human PK parameters and the parameters from human subjects after 20-mg oral dose

ParameterPredictedHealthy Male after 20-mg Oral DoseaAZD3783 Human PET Study at 20-mg Oral Doseb
Tmax, h1.42.5 (1.5, 3)2, 3, 3
T1/2, h1317 (12, 36)7.3, 10.7, 12.2
AUC0-inf, nM/h18531018 (224%)761, 977, 2684
Cmax, nM9079 (21%)54, 80, 182
Cmin, nM23N.D.N.D.
Vdss, l/kg6.4N.D.N.D.
CL, l/h/kgc0.390.60 (19%)N.D.
  • N.D., not determined.

  • a n = 6, values are presented as median (minimum, maximum) value for Tmax and t1/2, geometric mean (CV%) for AUC and Cmax.

  • b Data are from Varnäs et al. (2011).

  • c CL data from clinical observation are presented as geometric mean of oral clearance, CL/F (CV%).