tegafur + gefitinib

Tegafur + gefitinib is an investigational oral combination therapy used in clinical trials primarily for the treatment of advanced non-small cell lung cancer (NSCLC), especially in patients with EGFR mutations. Tegafur is a prodrug of fluorouracil (5-FU), a pyrimidine analogue that inhibits thymidylate synthase, disrupting DNA synthesis and exerting cytotoxic effects on rapidly dividing tumor cells[2]. Gefitinib is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, blocking downstream signaling pathways involved in cell proliferation and survival[1]. The rationale behind combining these agents is to enhance antitumor efficacy by targeting both DNA synthesis and EGFR-driven signaling. Clinical studies have shown that adding tegafur/uracil to gefitinib improves progression-free survival compared to gefitinib alone in NSCLC patients with EGFR mutations[3][6].