Bunnell C A, Winer E P
Breast Oncology Center, Dana-Farber Cancer Institute, Boston, Massachusetts, USA.
Oncology (Williston Park). 1998 Oct;12(10 Suppl 7):39-43.
Three oral 5-fluorouracil (5-FU) therapies have been approved by the US Food and Drug Administration or are in development for the treatment of patients with breast cancer: capecitabine, UFT, and 5-FU/eniluracil. Capecitabine has been approved for breast cancer patients whose disease is paclitaxel-resistant, and either anthracycline-resistant or for whom further anthracycline use is not indicated. A response rate of 20% was observed in an open-label phase II trial of capecitabine in heavily pretreated patients with metastatic breast cancer. Diarrhea and hand-foot syndrome were the most frequently reported toxicities. In a randomized phase II study of capecitabine vs paclitaxel in breast cancer patients who had failed anthracyclines, response rates were 36% for capecitabine vs 21% for paclitaxel. Several phase II trials of 5-FU/eniluracil in breast cancer are ongoing. Preliminary response data from one of these trials on 31 patients with anthracycline- and taxane-resistant advanced breast cancer showed a 16% partial response rate. Grade 3-4 treatment-related toxicities included diarrhea (8%), nausea (3%), and granulocytopenia (3%). In Japan, UFT is widely used for the treatment of breast cancer in both the adjuvant and metastatic settings, though studies in the United States are just getting under way. A phase II trial conducted in Madrid, Spain evaluated the combination of UFT, methotrexate, and leucovorin as salvage therapy for breast cancer patients. The overall response rate was 38% among 21 patients, and diarrhea was the most common toxicity. Many questions remain unanswered about the optimal use of oral 5-FU agents in breast cancer. There seems little question that these agents have substantial activity and will find a place in the therapeutic armamentarium.
美国食品药品监督管理局已批准三种口服5-氟尿嘧啶（5-FU）疗法用于治疗乳腺癌患者或这些疗法正处于研发阶段：卡培他滨、优福定（UFT）和5-FU/依诺尿嘧啶。卡培他滨已被批准用于治疗对紫杉醇耐药且对蒽环类药物耐药或不适合进一步使用蒽环类药物的乳腺癌患者。在一项针对转移性乳腺癌的经大量预处理患者的卡培他滨开放标签II期试验中，观察到缓解率为20%。腹泻和手足综合征是最常报告的毒性反应。在一项针对蒽环类药物治疗失败的乳腺癌患者的卡培他滨与紫杉醇的随机II期研究中，卡培他滨的缓解率为36%，而紫杉醇为21%。多项关于5-FU/依诺尿嘧啶治疗乳腺癌的II期试验正在进行。其中一项针对31例对蒽环类药物和紫杉烷耐药的晚期乳腺癌患者的试验的初步缓解数据显示，部分缓解率为16%。3-4级与治疗相关的毒性反应包括腹泻（8%）、恶心（3%）和粒细胞减少（3%）。在日本，优福定广泛用于辅助和转移性乳腺癌的治疗，不过美国的相关研究才刚刚起步。在西班牙马德里进行的一项II期试验评估了优福定、甲氨蝶呤和亚叶酸联合作为乳腺癌患者的挽救治疗。21例患者的总体缓解率为38%，腹泻是最常见的毒性反应。关于口服5-FU药物在乳腺癌中的最佳使用，仍有许多问题未得到解答。毫无疑问，这些药物具有显著活性，并将在治疗药物中占有一席之地。
