Epidermal growth factor receptor-targeted therapy and symptom improvement in non-small cell lung cancer are discussed. Non-small cell lung cancer (NSCLC) is a common and frequently incurable disease. Patients with advanced stage IIIB/IV disease, although not candidates for curative resection, can benefit from treatment that prolongs survival, alleviates symptoms, and reduces complications. While incremental advances have occurred with the use of chemotherapy and radiation therapy, the benefits have been largely palliative. Moreover, the adverse events associated with these therapies may undermine the treatment goal by replacing disease-related symptoms with treatment-related adverse events. Thus, novel, more targeted approaches are needed. Increased understanding of cellular and molecular biology has resulted in the development of treatments that selectively target key regulatory pathways and molecules involved in cell growth and metastasis. Gefitinib is one member of a new class of targeted anticancer agents known as tyrosine kinase inhibitors with activity against NSCLC. In clinical trials, gefitinib has produced responses in patients with relapsed or refractory NSCLC, reduced disease-related symptoms, and has been associated with improvements in quality of life. Such targeted therapy may have a significant impact on the treatment of patients with NSCLC.