PLATINUM COMPLEXES - NEW CLASS OF ANTINEOPLASTIC AGENTS

被引:117
作者
LEH, FKV
WOLF, W
机构
[1] UNIV SO CALIF, CANC HOSP & RES INST, LOS ANGELES, CA 90033 USA
[2] UNIV SO CALIF, SCH PHARM, RADIOPHARM PROGRAM, LOS ANGELES, CA 90033 USA
关键词
D O I
10.1002/jps.2600650303
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This review discussed the design of Pt compounds that show antitumor activity. The compounds should be neutral and contain a pair of cis-leaving groups. The carrier groups also play an important role in the determination of activity. They should be inert and neutral. The new derivatives should be synthesized with high tumor affinity and low renal toxicity, problems yet to be overcome. Although the Pt compounds showed a broad spectrum of action in various tumors, their immunosuppressive effect, prolonged retention, slow urinary elimination and severe renal toxicity pose a possible clinical danger. Drug treatments scheduled at too close intervals may lead to accumulation of a toxic body load of Pt. The choices of dose level and time schedule are important factors in treatment. Based on the preclinical studies of tumor inhibition and pharmacological data, a widely spaced treatment schedule is desired. No apparent and serious manifestation of toxicity was observed during treatment of patients with cis-dichlorodiammineplatinum (II) at weekly intervals and a low dose.
引用
收藏
页码:315 / 328
页数:14
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