Asbury R F, Boros L, Brower M, Woll J, Chang A, Bennett J
Am J Clin Oncol. 1987 Feb;10(1):47-9. doi: 10.1097/00000421-198702000-00011.
Twenty-two patients with metastatic colorectal cancer were treated with a regimen of 5-fluorouracil 600 mg/m2 (maximum, 1.0 g) i.v./week and folic acid 140 mg/m2 i.v. given 1 h prior to the 5-FU. This study was undertaken in an attempt to confirm the in vitro finding that inhibition of thymidylate synthetase by 5-fluorouracil is prolonged by the presence of folates. There were four partial responses (18%) with mean duration 4 months. Dose-limiting toxicity was enteritis, seen in 12 patients (58%), and causing hospitalization in seven patients. Enteritis was shown to be due to the folic acid in most patients. Two patients died from leukopenia, enteritis, and sepsis. Mean serum folate levels at the time of 5-FU injection were 36 microM. This regimen is no more effective than 5-FU alone and has significantly more serious toxicity. Further investigation of this regimen is not recommended.
22例转移性结直肠癌患者接受了如下治疗方案：5-氟尿嘧啶600 mg/m²（最大剂量1.0 g）静脉注射，每周1次，叶酸140 mg/m²静脉注射，在5-氟尿嘧啶给药前1小时给予。进行这项研究是为了证实体外研究结果，即叶酸的存在可延长5-氟尿嘧啶对胸苷酸合成酶的抑制作用。有4例部分缓解（18%），平均缓解持续时间为4个月。剂量限制性毒性为肠炎，12例患者（58%）出现肠炎，7例患者因肠炎住院。在大多数患者中，肠炎被证明是由叶酸引起的。2例患者死于白细胞减少、肠炎和败血症。5-氟尿嘧啶注射时的平均血清叶酸水平为36微摩尔。该方案并不比单用5-氟尿嘧啶更有效，且毒性明显更严重。不建议对该方案进行进一步研究。
