In a phase 1 study conducted in healthy subjects (Study 1116), 240 mg oral doses of neratinib were administered as capsules with a standard meal for 14 days (n=25). The mean relative exposure (AUC) to parent at steady-state (Day 刀 was 15%, 33%, 22%, and 4% for M3, M6, M7, and Mil, respective!y. Steady state exposure at day 7 (mean AUCss) and potency data (inhibition of phosphorylation by ERBB2) for parent and active metabolites were used to calculate the contributions to total plasma pharmacological activity provided by neratinib and each metabolite according to the following formula: