Gefitinib is a targeted anticancer drug and an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) mainly used in non-small cell lung cancer (NSCLC) with specific EGFR mutations. It works by blocking the EGFR signaling pathway, inhibiting tumor cell growth and survival. Developed by AstraZeneca in the late 1990s, gefitinib emerged during the rise of targeted therapies and received accelerated approval in 2003 for NSCLC patients who had failed prior chemotherapy. Its use has since focused on patients with confirmed EGFR mutations, making it a key drug in personalized cancer treatment.