Bedikian A Y, Stroehlein J, Korinek J, Karlin D, Bodey G P
Am J Clin Oncol. 1983 Apr;6(2):181-6. doi: 10.1097/00000421-198304000-00007.
A randomized study was conducted in patients who had measurable metastatic colorectal cancer to compare the relative efficacy and toxicities of oral tegafur (1 gm/m2/days 1-21) with those of 5-fluorouracil (5-Fu, 500 mg/m2/days 1-4, then 250 mg/m2 on days 6, 8, 10, 12). The treatment courses were repeated every 4 weeks. Patients not responding to 5-Fu treatment were switched to tegafur. Randomization was stratified for presence or absence of liver metastasis and performance status. Partial responses were observed with 5-Fu, 6/32 (19%), tegafur, 7/35 (20%), and in patients who had been switched to tegafur after failing on 5-Fu, 1/20 (5%) with patients evaluable for response. Neutropenia was more common with 5-Fu (32% vs. 1% of treatment courses). Nausea occurred in about half the treatment courses; vomiting occurred in only 22%. Mucositis and diarrhea were more common with 5-Fu and severe in patients with liver function impairment. Neurologic toxicities due to tegafur were mild and occurred in less than 10% of the treatment courses. Oral tegafur and I.V. 5-Fu were equally effective against colorectal cancer, but tegafur was associated with minimal myelosuppression, which makes it suitable for use in combination with myelosuppressive antitumor agents.
对患有可测量转移性结直肠癌的患者进行了一项随机研究，以比较口服替加氟（1克/平方米，第1 - 21天）与5-氟尿嘧啶（5-Fu，500毫克/平方米，第1 - 4天，然后在第6、8、10、12天为250毫克/平方米）的相对疗效和毒性。治疗疗程每4周重复一次。对5-Fu治疗无反应的患者改用替加氟。随机分组根据有无肝转移和体能状态进行分层。5-Fu组观察到部分缓解的有6/32例（19%），替加氟组有7/35例（20%），在5-Fu治疗失败后改用替加氟的患者中，可评估反应的患者有1/20例（5%）。5-Fu组中性粒细胞减少更常见（占治疗疗程的32% vs. 1%）。约一半的治疗疗程出现恶心；呕吐仅发生在22%的疗程中。5-Fu组黏膜炎和腹泻更常见，且在肝功能损害的患者中严重。替加氟引起的神经毒性较轻，发生在不到10%的治疗疗程中。口服替加氟和静脉注射5-Fu对结直肠癌同样有效，但替加氟的骨髓抑制作用最小，这使其适合与骨髓抑制性抗肿瘤药物联合使用。
