Clinical phase I study of the hypoxic cell radiosensitizer RO-07-0582, a 2-nitroimidazole derivative.
Clinical phase I study of the hypoxic cell radiosensitizer RO-07-0582, a 2-nitroimidazole derivative.
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缺氧细胞放射增敏剂 RO-07-0582（一种 2-硝基咪唑衍生物）的临床 I 期研究。
作者：
R. Urtasun;P. Band;J. Chapman;H. Rabin;A. Wilson;C. Fryer
RO-07-0582 毒性研究在 12 名患者中进行，共进行了 16 次检测。使用单次和多次剂量方案，并确定实体瘤组织、脑脊液和血液（14至24小时）中的药物浓度。当总剂量达到 24 g 时，1 名接受分次治疗的患者出现严重周围神经病变。药物吸收和血液浓度与甲硝唑没有显着差异。 2至4小时达到最高血液水平，并且在施用后的几天内已稳定至仅略高于对照水平的水平。
RO-07-0582 toxicity studies were performed in 12 patients for a total of 16 assays. Single and multifraction dose schedules were used, and drug concentrations in solid tumor tissue, cerebrospinal fluid, and blood (at 14 to 24 hr.) were established. A severe peripheral neuropathy occurred in 1 patient on the multifraction regimen when the total dosage reached 24 g. Drug absorption and concentration in the blood do not significantly differ from that of metronidazole. Maximum blood levels were reached at from 2 to 4 hr., and several days subsequent to administration had stabilized to levels only slightly above control levels.