B-85-0040 is a new cisplatin analogue with dose limiting myelosuppression. 2. The maximum tolerated dose ranges between 300 and 525 mg/kg for single i.p. bolus injection in mice. 3. Its toxicity is circadian-stage dependent with optimal tolerance between 16 and 17 hours after lights on. 4. B-85-0040 is active in L1210 leukemia. Anti-tumor activity seems to be unrelated to the circadian stage of treatment. Optimal drug timing can therefore increase its therapeutic index.
摘要
B - 85 - 0040是一种新型顺铂类似物,具有剂量限制性骨髓抑制作用。2. 对于小鼠单次腹腔推注注射,其最大耐受剂量范围在300至525毫克/千克之间。3. 其毒性具有昼夜阶段依赖性,光照后16至17小时耐受性最佳。4. B - 85 - 0040对L1210白血病有活性。抗肿瘤活性似乎与治疗的昼夜阶段无关。因此,最佳给药时间可以提高其治疗指数。