icotinib + osimertinib

This drug is a combination of two small molecule tyrosine kinase inhibitors (TKIs) targeting the epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer (NSCLC). Icotinib is a first-generation EGFR TKI that reversibly inhibits EGFR tyrosine kinase activity, primarily effective against common activating mutations such as exon 19 deletions. Osimertinib is a third-generation irreversible EGFR TKI designed to selectively inhibit both sensitizing EGFR mutations and the resistance mutation T790M. The combination aims to overcome resistance mechanisms in NSCLC patients harboring complex or multiple EGFR mutations including 19del, T790M, and C797S. Clinical case reports have shown that this combination can stabilize disease and overcome resistance when these mutations occur in cis configuration. The drugs were developed for targeted therapy of advanced or metastatic NSCLC with specific EGFR mutations.