Eagan R T, Ames M M, Powis G, Kovach J S
Cancer Treat Rep. 1982 Feb;66(2):283-7.
Dianhydrogalactitol was administered as two 1-hr infusions separated by a 4-hr period once every 5 weeks to 21 patients with advanced solid tumors. Total doses ranged from 100 mg/m2 (50 mg/m2 twice on a single day) to 160 mg/m2 (80 mg/m2 twice on a single day). Peak concentrations of drug at the end of a 1-hr infusion ranged from 1.9 to 5.6 microgram/ml. Plasma elimination of dianhydrogalactitol was approximated best by a two-compartment open model. The alpha-half-life was 3.9 +/- 1.9 mins and the beta-half-life was 31.3 +/- 2.7 mins. Dose-limiting hematologic toxicity was encountered at a total dose of 160 mg/m2, with leukopenia occurring more frequently than thrombocytopenia. Other toxic effects included mild to moderate nausea in most patients and two instances of moderate alopecia. One patient with large cell cancer of the lung had a partial regression lasting 2 months and one patient with a carcinoid in the thymus had a partial regression lasting 7 1/2 months. A third patient with a mixed adenocarcinoma-squamous cell carcinoma of the lung had improvement (30% decrease) in his pulmonary tumor for greater than 2 months.
双脱水半乳糖醇以两个1小时输注的方式给药，中间间隔4小时，每5周进行一次，共治疗21例晚期实体瘤患者。总剂量范围为100mg/m²（单日两次，每次50mg/m²）至160mg/m²（单日两次，每次80mg/m²）。1小时输注结束时药物的峰值浓度范围为1.9至5.6微克/毫升。双脱水半乳糖醇的血浆消除情况以二室开放模型拟合最佳。α半衰期为3.9±1.9分钟，β半衰期为31.3±2.7分钟。在总剂量为160mg/m²时出现了剂量限制性血液学毒性，白细胞减少比血小板减少更常见。其他毒性作用包括大多数患者出现轻度至中度恶心以及两例中度脱发。一名肺大细胞癌患者出现了持续2个月的部分缓解，一名胸腺类癌患者出现了持续7个半月的部分缓解。第三名肺混合性腺癌-鳞状细胞癌患者肺部肿瘤改善（缩小30%）超过2个月。
