TABLE 2

High risk vs. low risk characteristics for moderate or large AUCi/AUC ratios for metabolized drugs in the presence of inhibitor


High Risk of Large AUCi/AUC Ratio

Low Risk of Large AUCi/AUC Ratio
Metabolized by single enzymea Metabolized by multiple enzymesa
High I/Ki ratioa Low I/Ki ratioa
High hepatic extractionb Low hepatic extractionb
Low Km (equal to, or greater than liver drug concentrations at therapeutic doses)c
High Km (much greater than liver drug concentrations at therapeutic doses)a