Arbuck S G, Takimoto C H
Division of Cancer Treatment, Diagnosis, and Centers, National Cancer Institute, Bethesda Naval Hospital, MD 20892, USA.
Semin Hematol. 1998 Jul;35(3 Suppl 4):3-12.
The camptothecins are a new class of antitumor agents that target topoisomerase I. Irinotecan and topotecan are the most widely used camptothecin analogs in clinical practice, with documented clinical activity in colorectal and ovarian cancer. Ongoing clinical trials with these agents are further characterizing their spectra of clinical activity and determining their optimal schedule of administration in combination with other anticancer agents. Newer camptothecin analogs in clinical development, such as 9-aminocamptothecin, 9-nitrocamptothecin, GI1147211, and DX-8951f, are also being studied to determine if they have improved toxicity and efficacy profiles compared with existing analogs. The successful development of the camptothecins as antitumor agents demonstrates the importance of topoisomerase 1 as a target for cancer chemotherapy.
喜树碱类是一类新型的靶向拓扑异构酶I的抗肿瘤药物。伊立替康和拓扑替康是临床实践中使用最广泛的喜树碱类似物，在结直肠癌和卵巢癌中具有已记录的临床活性。对这些药物正在进行的临床试验正在进一步明确其临床活性谱，并确定它们与其他抗癌药物联合使用的最佳给药方案。正在临床开发中的新型喜树碱类似物，如9-氨基喜树碱、9-硝基喜树碱、GI1147211和DX-8951f，也正在进行研究，以确定与现有类似物相比，它们是否具有改善的毒性和疗效特征。喜树碱类作为抗肿瘤药物的成功开发证明了拓扑异构酶1作为癌症化疗靶点的重要性。
