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一种新型抗肿瘤药物,梭布佐生(MST-16)

[A novel antitumor agent, sobuzoxane (MST-16)].

作者信息

Tsukagoshi S

机构信息

Cancer Chemotherapy Center, Japanese Foundation for Cancer Research.

出版信息

Gan To Kagaku Ryoho. 1994 Jun;21(7):1089-97.

PMID:8002628
Abstract

Sobuzoxane (MST-16) is an analogue of ICRF-159 which was once evaluated on the clinical efficacies in England. Zenyaku Pharm. Ind. in Japan synthesized many derivatives of bis (2,6-dioxopiperazine) and sobuzoxane was selected from the antitumor efficacies, the results of the toxicity tests and pharmacological profiles from these derivative. The compound was a new type topoisomerase II inhibitor, and G2M phase of the cell cycle was most sensitive. The clinical phase studies proved that sobuzoxane was quite effective for the treatment of malignant lymphoma (overall response rate in phase II study 29.7%) and adult T cell leukemia (response rate for acute type: 46.2%). The dose-limiting factor was leukopenia.

摘要

索布佐生(MST - 16)是ICRF - 159的类似物,ICRF - 159曾在英国进行过临床疗效评估。日本善光寺制药工业公司合成了许多双(2,6 - 二氧代哌嗪)衍生物,并根据这些衍生物的抗肿瘤疗效、毒性试验结果和药理学特征选择了索布佐生。该化合物是一种新型拓扑异构酶II抑制剂,细胞周期的G2M期最为敏感。临床阶段研究证明,索布佐生对恶性淋巴瘤的治疗相当有效(II期研究的总缓解率为29.7%),对成人T细胞白血病也有效(急性型的缓解率为46.2%)。剂量限制因素是白细胞减少。

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