Bedikian A Y, Stroehlein J R, Karlin D A, Korinek J, Bodey G P
Am J Clin Oncol. 1982 Oct;5(5):535-7.
Thirty patients with measurable metastatic colorectal cancer refractory to 5-fluorouracil-containing regimens, received AZQ (1,4-cyclohexadiene-1,4-dicarbamic acid, 2,5-bis(1-aziridinyl)3,6,dioxo,diethylester, NSC 182986) on a 5-day intravenous schedule administered every 4 weeks. Good risk patients received AZQ at the starting daily dose of 8 mg/m2, while patients who had had therapy with radiation or myelosuppressive drugs such as mitomycin C or a nitrosourea compound received an initial daily dose of 6 mg/m2. There were no complete or partial remissions. Only one of 27 evaluable patients had objective tumor regression. Five additional patients had disease stabilization. The dose-limiting toxicity was myelosuppression, with thrombocytopenia being more severe than neutropenia. The myelosuppression occurred late in the treatment cycle (day 20), was more severe with repeated treatments, and was more severe in patients who had poor bone marrow reserves. AZQ administered by the 5-day dose schedule as used in this study is not effective against colorectal cancer.
30例对含5-氟尿嘧啶方案耐药的可测量转移性结直肠癌患者，接受了AZQ（1,4-环己二烯-1,4-二氨基甲酸2,5-双（1-氮丙啶基）3,6-二氧代二乙酯，NSC 182986）治疗，采用每4周一次的5天静脉给药方案。低风险患者起始每日剂量为8mg/m²接受AZQ治疗，而接受过放疗或使用过丝裂霉素C或亚硝基脲化合物等骨髓抑制药物治疗的患者起始每日剂量为6mg/m²。没有完全缓解或部分缓解病例。27例可评估患者中只有1例出现客观肿瘤消退。另有5例患者病情稳定。剂量限制性毒性为骨髓抑制，血小板减少比中性粒细胞减少更严重。骨髓抑制发生在治疗周期后期（第20天），重复治疗时更严重，且骨髓储备差的患者更严重。本研究中使用的5天给药方案给予的AZQ对结直肠癌无效。
