TABLE 4

Prediction of efavirenz mean CLpo from in vitro data generated in genotyped HLMs and expressed CYP2B6 by PBPK modeling

Simcyp ISEF values are Simcyp default ISEF values. RMSE, MRS, and average fold error were calculated by comparing the predicted efavirenz mean CLpo by PBPK modeling to observed mean values.

Predicted Mean CLpoObserved Mean CLpoRMSEMRSAverage Fold Error
HLMs3.0−2.52.3
 CYP2B6*1/*18.58.5
 CYP2B6*1/*64.78.3
 CYP2B6*6/*62.15.9
Expressed cytochrome P450s (Simcyp ISEF)3.8−3.83.2
 CYP2B6*1/*14.18.5
 CYP2B6*6/*62.85.9
Expressed cytochrome P450s (VISEF)1.01.00.55
 CYP2B6*1/*19.88.5
 CYP2B6*6/*66.65.9
Expressed cytochrome P450s (CLISEF)11.27.11.5
 CYP2B6*1/*124.38.5
 CYP2B6*6/*64.25.9