A 69-year-old female, who had been admitted to another hospital with a complaint of headache and there detected brain tumor, was referred to our hospital for further examination and therapy. The patient was diagnosed as having advanced lung cancer with multiple brain metastasis. She was treated with five courses of a combination of chemotherapy consisting of carboplatin and paclitaxel following gamma knife radiotherapy. She showed a remarkable response, however, she experienced the side effects of general fatigue and numbness in her extremities, which were intolerable. Then, therapy with gefitinib alone was chosen as second-line chemotherapy. After one month, this therapy was discontinued due to grade 3 skin trouble and rash. When her condition improved, every other day oral administration of gefitinib was resumed. She has been treated on an outpatient basis because of no severe adverse reactions. The patient is alive with good performance status (PS) 0 more than one year after taking gefitinib. Furthermore, the primary and metastatic tumors are not enlarged. Gefitinib orally administered every other day could be a promising regimen as second-line chemotherapy for patients with lung cancer and brain metastasis.