氯脲霉素的I期试验：通过给予葡萄糖尝试改善骨髓毒性。
Phase I trial of chlorozotocin: attempted amelioration of myelotoxicity by glucose administration.
作者信息
Panasci L, Comis R, Ginsberg S, Kohn L, Fitzpatrick A, Rubert M, Scalzo T
出版信息
Cancer Treat Rep. 1981 Jul-Aug;65(7-8):647-50.
Chlorozotocin is a new anticancer agent with the chloroethylnitrosourea cytotoxic moiety attached to the carbon-2 position of glucose. Like other chloroethylnitrosoureas, this agent produces delayed myelotoxicity which is dose-limiting. A phase I trial of chlorozotocin with administration of glucose was done in an attempt to modify the myelotoxicity. The patients received the first course of chlorozotocin (200 mg/m2) in the fasting state and then the second course of chlorozotocin with boluses of a 50% glucose solution. With the second course of chlorozotocin administration, the glucose concentration remained threefold greater than after the first course for at least 1 hour. The plasma half-life and apparent volume of distribution of chlorozotocin were similar following either course. The wbc, neutrophil, and platelet count nadirs after the first course of this agent were not significantly different than the nadirs after the second course. We were unable to modify the myelotoxicity of chlorozotocin with boluses of a 50% glucose solution.
氯脲霉素是一种新型抗癌药，其氯乙基亚硝基脲细胞毒性部分连接在葡萄糖的2 - 碳位上。与其他氯乙基亚硝基脲一样，该药物会产生延迟性骨髓毒性，这是剂量限制性的。开展了一项氯脲霉素联合葡萄糖给药的I期试验，试图改变其骨髓毒性。患者在空腹状态下接受第一疗程的氯脲霉素（200 mg/m²），然后在第二疗程的氯脲霉素给药时静脉推注50%葡萄糖溶液。在第二疗程氯脲霉素给药期间，葡萄糖浓度至少1小时内比第一疗程后高三倍。两疗程后氯脲霉素的血浆半衰期和表观分布容积相似。该药物第一疗程后的白细胞、中性粒细胞和血小板计数最低点与第二疗程后的最低点无显著差异。我们无法通过静脉推注50%葡萄糖溶液来改变氯脲霉素的骨髓毒性。
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