Theliatinib

Theliatinib is a potent epidermal growth factor receptor EGFR tyrosine kinase inhibitor with a Ki value of 0.05 nM and IC₅₀ of 3 nM. It exhibits strong antitumor activity in patient-derived estrogen cancer xenograft (PDECX) models with high EGFR expression, including remarkable tumor regression in two PDECX models with both EGFR gene amplification and protein overexpression in a dose-dependent manner (5 and 15 mg/kg/day). The efficacy of theliatinib is reduced in the models with PI3KCA mutations or FGFR1 overexpression in addition to high EGFR expression.