TABLE 3

Bosentan stability, binding, induction parameter estimates, and induction predictions

Hepatocyte LotAverage % Remainingfu,mediumEmaxNominal EC50Measured EC50Nominal EC50,uMeasured EC50,u
CDP33.20.389.41.60.70.60.3
Hu162444.10.3811.63.01.01.10.4
Prediction method
 R3
  CDP34a29.1b46.9b50.4b67.0b
  Hu162434a21.8b44.6b41.6b65.7b
 AUCR
  CDP34a29.4b48.2b51.9b70.1b
  Hu162434a22.0b45.7b42.5b68.6b
  • a Observed % DDI.

  • b Predicted % DDI.