Table 1.

Summary of PK and PD parameters estimated from WM-266-4 xenograft studies

PK parameterEstimate (%SE)a
 ka, h−11.08 (5.6)
Cl, L/h/kg3.13 (2.1)
Clpt, L/h/kg1.74 (4.5)
Cltp, L/h/kg0.040 (5.8)
 V/F, L/kg40.5 (1.5)
PD parameter for %pERK decreaseSingle dose estimate (%SE)aMultiple dose estimate (%SE)a
IC50, μmol/L0.78 (26.4)3.89 (7.7)
 Imax (%)97 (10.4)100 (fixed)
 h1 (fixed)1.85 (13.8)
  • aFitted parameters are expressed as estimate followed by the %SE in parentheses.