PURPOSE: This study was performed to evaluate the efficacy and toxicity of vinorelbine in combination with epirubicin as a first-line chemotherapy in patients with advanced breast cancer as well as a second-line chemotherapy in refractory patients after failing to first-line chemotherapy. MATERIALS AND METHODS: Between March 1997 and July 1999, thirty-seven patients were enrolled. Vinorelbine 25 mg/m2 intravenously (IV) on days 1 and 8, and epirubicin 50 mg/m2 IV on day 1 were given every 3 weeks. Among the evaluable 34 patients, 25 patients received VE chemotherapy as a ""first-line chemotherapy"". 4 patients had initially systemic metastasis, 2 patients relapsed after operation and 19 patients relapsed after adjuvant chemotherapy. Nine patients had progressive diseases after one or more palliative regimens. Among the 9 patients, 1 patient showed the progression during the adjuvant chemotherapy. The median age of the patients was 49 years (range; 31~64), and 68% of patients were premenopausal. Dominant sites of metastasis were viscera in 82% and non-viscera (soft tissue, lymph nodes and bone) in 18%. RESULTS: Overall response rates (RR) were 64% in first-line group. There was no responder in second-line group. Six patients without any prior chemotherapy obtained 2 CR and 3 PR (RR; 83%), while pre-treated 28 patients showed 1 CR and 10 PR (RR; 39%). Among the second-line group, 6 patients had been exposed to anthracycline. Median number of chemotherapy cycle was 3.5 (2~7). Total 135 cycles of therapy were evaluable for toxicity. The most common dose-limiting toxicity was myelosuppression, mainly leukopenia in 58 cycles (43%). Grade 3 or 4 leukopenia were observed in 10 cycles (7%), of which 3 cycles were associated with infection requiring hospitalization. Anemia were observed in 42 cycles (31%), mostly grade 1 or 2 (28%). The most common non-hematologic toxicity was alopecia (91%) followed by phlebitis (41%). There was no therapy-related mortality. CONCLUSION: Vinorelbine and epirubicin combination showed significant activity as a first-line regimen in advanced breast cancer. The combinaton showed no activity in patients pretreated with other palliative regimen.