Preclinical research and ongoing clinical trials are validating epidermal growth factor receptor (EGFR) as a suitable molecular target in cancer therapy. Here we report the case of a 39-year-old non-smoking man with heavily pretreated stage IV bronchioloalveolar NSCLC who was treated with gefitinib ('Iressa', ZD1839) at the dose of 250 mg/day, orally. Symptomatic relief was already detectable after 2 weeks of gefitinib therapy, pulmonary function tests readily improved, performance status went from 2 to 0 within 8 weeks, CT scan performed after 10 weeks of treatment showed nearly complete resolution of the clinical picture, and clinical remission was maintained up to 32 weeks. This case-report illustrates the potential of EGFR tyrosine kinase inhibition to induce clinically meaningful responses in heavily pretreated, advanced NSCLC patients and suggests that participation of such patients into clinical trials of signal transduction inhibitors should be encouraged.