Icotinib

Icotininb is a potent epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC₅₀ of 5 nM. It blocks EGFR-mediated intracellular tyrosine phosphorylation IC₅₀ of 45 nM in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation. Icotinib shows potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment.