Klaassen U, Wilke H, Pari C P, Strumberg D, Harstrick A, Eberhardt W, Becher R, Diergarten K, Seeber S
Department of Internal Medicine (Cancer Research), West German Cancer Center, University of Essen, Germany.
Semin Oncol. 1995 Dec;22(6 Suppl 14):7-11.
Phase II study results demonstrating high efficacy and low toxicity for a weekly schedule of high-dose 5-fluorouracil/folinic acid (5-FU/FA) in intensively pretreated metastatic breast cancer patients prompted the addition of paclitaxel (Taxol; Bristol-Myers Squibb Company, Princeton, NJ) to this regimen in a phase I/II trial in outpatients: high-dose 5-FU (24-hour infusion)/FA (2-hour infusion preceding 5-FU) is given for 6 weeks (days 1, 8, 15, 22, 29, and 36), with paclitaxel (3-hour infusion) administered on days 1 and 22; 2 weeks' rest follows. Folinic acid 500 mg/m2 was administered throughout; the respective 5-FU doses for dose levels 1 through 3 were 1.5, 1.8, and 2.0 g/m2 with paclitaxel 135 mg/m2. Dose level 4 (500 mg/m2 FA, 2.0 g/m2 5-FU, and 175 mg/m2 paclitaxel) was chosen for phase II evaluation. To date, 46 patients with bidimensionally measurable disease (four each at dose levels 1, 2, and 3, and 34 at dose level 4) have been entered. The 12 patients treated at dose levels 1 through 3 were titrated to level 4 doses when phase II began; 35 patients are evaluable for response. The median age is 46 years, and the median number of metastatic sites is 2.5. Fourteen patients had received adjuvant chemotherapy, nine chemotherapy for metastasis, and 23 chemotherapy both adjuvantly and for metastasis. Of 31 anthracycline-treated patients, 27 had anthracycline-resistant disease. No dose-limiting toxicity appeared until dose level 4, when grade 3 or 4 leukopenia and diarrhea occurred in 15 and eight, respectively, of 108 cycles. Mild to moderate mucositis, hand-foot syndrome, myalgia, and nausea/vomiting occurred in 20% to 40% of cycles. One (3%) of the 35 patients had a complete response, 18 (51%) had partial responses, 14 (40%) had stable disease, and two (6%) had disease progression. Eleven (55%) of 20 evaluable patients with anthracycline-resistant disease responded (95% confidence interval, 34% to 76%). Median time to maximum response was 2 months, and the remission duration was 8+ months. Median survival time has not been reached. Paclitaxel and weekly high-dose 5-FU/FA was well tolerated and highly effective, even in patients with anthracycline-resistant metastatic breast cancer. The regimen can be administered safely to outpatients.
II期研究结果表明,对于经过强化预处理的转移性乳腺癌患者,每周一次高剂量5-氟尿嘧啶/亚叶酸(5-FU/FA)方案具有高效和低毒的特点,这促使在一项针对门诊患者的I/II期试验中将紫杉醇(泰素;百时美施贵宝公司,新泽西州普林斯顿)加入该方案:高剂量5-FU(24小时输注)/FA(在5-FU之前2小时输注)持续给药6周(第1、8、15、22、29和36天),紫杉醇(3小时输注)在第1天和第22天给药;随后休息2周。全程给予亚叶酸500mg/m²;剂量水平1至3的5-FU相应剂量分别为1.5、1.8和2.0g/m²,紫杉醇为135mg/m²。选择剂量水平4(500mg/m² FA、2.0g/m² 5-FU和175mg/m²紫杉醇)进行II期评估。迄今为止,已纳入46例具有可二维测量病灶的患者(剂量水平1、2和3各4例,剂量水平4为34例)。在II期开始时,剂量水平1至3治疗的12例患者被滴定至剂量水平4;35例患者可评估疗效。中位年龄为46岁,转移部位的中位数为2.5个。14例患者接受过辅助化疗,9例接受过转移性化疗,23例既接受过辅助化疗也接受过转移性化疗。在31例接受过蒽环类药物治疗的患者中,27例患有蒽环类药物耐药性疾病。直到剂量水平4才出现剂量限制性毒性,在108个周期中,分别有15例和8例出现3级或4级白细胞减少和腹泻。20%至40%的周期出现轻度至中度粘膜炎、手足综合征、肌痛和恶心/呕吐。35例患者中有1例(3%)完全缓解,18例(51%)部分缓解,14例(40%)病情稳定,2例(6%)病情进展。20例可评估的蒽环类药物耐药性疾病患者中有11例(55%)有反应(95%置信区间,34%至76%)。达到最大反应的中位时间为2个月,缓解持续时间为8+个月。中位生存时间尚未达到。紫杉醇和每周一次高剂量5-FU/FA耐受性良好且高效,即使对于蒽环类药物耐药的转移性乳腺癌患者也是如此。该方案可安全地用于门诊患者。