gefitinib, erlotinib, or icotinib

Gefitinib, erlotinib, and icotinib are first-generation small molecule tyrosine kinase inhibitors that selectively target the epidermal growth factor receptor (EGFR) tyrosine kinase domain. By competitively binding to the ATP-binding site of EGFR, these drugs inhibit EGFR phosphorylation and downstream signaling pathways involved in cell proliferation and survival. They are primarily indicated for the treatment of non-small cell lung cancer (NSCLC) with activating EGFR mutations. All three agents have demonstrated comparable clinical effectiveness as adjuvant therapy in early-stage EGFR-mutated NSCLC patients following radical resection[1][2][5]. While their efficacy is similar, toxicity profiles may differ slightly; for example, erlotinib tends to have higher rates of rash and gastrointestinal side effects compared to gefitinib or icotinib[3][5]. Gefitinib may offer better penetration into brain metastases than the other two agents[4].

Brand names

IressaTarcevaConmana

Other names

ZD1839ZD-1839ZD 1839OSI-774OSI774OSI 774