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[DNA拓扑异构酶抑制剂作为化疗药物——临床视角]

[DNA topoisomerase inhibitor as chemotherapeutic drug--clinical point of view].

作者信息

Taguchi T

机构信息

Hospital Attached to Research Institute for Microbial Diseases, Osaka University, Japan.

出版信息

Gan To Kagaku Ryoho. 1991 Aug;18(10):1574-8.

PMID:1651685
Abstract

CPT-11 is a semisynthesized derivative of camptothecin that has a potent antitumor activity by inhibiting DNA topoisomerase I. Leukopenia (mainly neutropenia) is DLF (dose limiting factor) and MTD (maximum tolerated dose) is higher than 250 mg/m2 in CPT-11 from the results of clinical phase I study. Now we are going on phase II study of CPT-11. We are seeing the cases responded to the drug in cancer of the lung, ovary, uterus, stomach, colorectum, pancreas, breast, malignant lymphoma etc.

摘要

CPT-11是喜树碱的半合成衍生物,通过抑制DNA拓扑异构酶I具有强大的抗肿瘤活性。根据临床I期研究结果,白细胞减少(主要是中性粒细胞减少)是CPT-11的剂量限制因素,其最大耐受剂量(MTD)高于250mg/m²。目前我们正在进行CPT-11的II期研究。我们正在观察其在肺癌、卵巢癌、子宫癌、胃癌、结直肠癌、胰腺癌、乳腺癌、恶性淋巴瘤等癌症中对该药有反应的病例。

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