Saunders M I, Anderson P J, Bennett M H, Dische S, Minchinton A, Stratford M R, Tothill M
Int J Radiat Oncol Biol Phys. 1984 Sep;10(9):1759-63. doi: 10.1016/0360-3016(84)90544-3.
Ro 03-8799, a lipophilic nitroimidazole with a basic side chain, has now been administered intravenously to 69 patients. The elimination half-life in plasma was 5.1 hr and the plasma concentration at 30 min was 14.8 micrograms/ml standardized to a dose of 1 g per square meter of surface area. Immediate symptoms of malaise, heat, sweating and disorientation limit the amount of the drug which may be given on any one occasion. However, a dose of 750 mg per square meter of surface area may be given combined with daily radiotherapy. Our data suggest that when given with a 20 fraction course of radiotherapy, sensitization of hypoxic cells may be achieved equal to a 10-fold increase in the dose of misonidazole above that presently permitted.
Ro 03-8799是一种带有碱性侧链的亲脂性硝基咪唑，目前已对69名患者进行了静脉注射。血浆中的消除半衰期为5.1小时，按每平方米表面积1克的剂量标准化后，30分钟时的血浆浓度为14.8微克/毫升。不适、发热、出汗和定向障碍等即时症状限制了单次给药的剂量。然而，每平方米表面积750毫克的剂量可与每日放疗联合使用。我们的数据表明，在进行20次分割疗程的放疗时，给予该药可能使缺氧细胞增敏，效果相当于将米索硝唑的剂量增加至目前允许剂量的10倍。
