Simon M S, Eckenrode J, Natale R B
Department of Internal Medicine, University of Michigan, Ann Arbor.
Invest New Drugs. 1990;8 Suppl 1:S79-81. doi: 10.1007/BF00171989.
Methylglyoxal bis-guanylhydrazone (MGBG), a potent inhibitor of polyamine synthesis, has demonstrated single agent activity against a number of tumor types including malignant lymphomas and head and neck, esophageal and non-small cell lung cancers. The growth of small cell lung cancer (SCLC) cell lines can be arrested by polyamine inhibition. Therefore a phase II trial was conducted in twenty-four patients with refractory SCLC. MGBG was administered by intravenous infusion at a dose of 500 mg/m2 per week for four cycles and then every two weeks thereafter. The dose was escalated by 100 mg/m2 every two weeks in the absence of toxicity greater than or equal to grade 2. One patient achieved a partial response of objectively measurable lung disease and supraclavicular adenopathy. Three patients had stable disease. Dose limiting toxicity consisted primarily of mild to moderate nausea, vomiting, stomatitis and/or diarrhea. Myelosuppression was uncommon and rarely dose limiting. We conclude that MGBG in the dose and schedule used does not have significant activity as a single agent in previously treated small cell lung cancer.
甲基乙二醛双脒腙（MGBG）是一种有效的多胺合成抑制剂，已显示出对多种肿瘤类型具有单药活性，包括恶性淋巴瘤以及头颈部、食管癌和非小细胞肺癌。多胺抑制可使小细胞肺癌（SCLC）细胞系的生长停滞。因此，对24例难治性SCLC患者进行了一项II期试验。MGBG通过静脉输注给药，剂量为每周500mg/m²，共四个周期，此后每两周一次。在无大于或等于2级毒性的情况下，每两周剂量递增100mg/m²。一名患者出现了可客观测量的肺部疾病和锁骨上淋巴结肿大的部分缓解。三名患者病情稳定。剂量限制性毒性主要包括轻度至中度恶心、呕吐、口腔炎和/或腹泻。骨髓抑制不常见，很少限制剂量。我们得出结论，在所使用的剂量和方案下，MGBG作为单药在先前治疗的小细胞肺癌中没有显著活性。
