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去甲柔红霉素的临床活性:一种新的蒽环类衍生物。

Clinical activity of detorubicin: a new anthracycline derivative.

作者信息

Jacquillat C, Auclerc M F, Weil M, Maral J, Degos L, Auclerc G, Tobelem G, Schaison G, Bernard J

出版信息

Cancer Treat Rep. 1979 May;63(5):889-93.

PMID:455330
Abstract

The anthracycline derivatives are intercalating drugs which are of major importance in the treatment of leukemias and in the management of solid tumors. Structural analogs have been prepared by semisynthetic modifications in an attempt to extend the spectrum of antitumor activity and to reduce toxicity (acute myelosuppression and cardiotoxicity). This report concerns our preliminary clinical experience in 111 patients who received detorubicin. Two dose schedules were used in acute leukemia patients. Sequential doses were active in acute leukemia relapses but the mucous membrane toxicity was excessive; more recently, intermittent doses proved active in acute leukemia relapses (one 6-mg/kg dose) and in a patient with resistant Burkitt's lymphoma. In non-Hodgkin's lymphomas, a complete response rate of 71% was achieved with an intermittent schedule (3 mg/kg/day X 3 weeks). A remarkable shrinkage of skin involvement was also observed. Detorubicin showed a high activity in mycosis fungoides (five regressions among six patients) and some activity in soft tissue sarcomas, osteosarcomas, and various solid tumors.

摘要

蒽环类衍生物是嵌入性药物,在白血病治疗和实体瘤管理中具有重要意义。人们通过半合成修饰制备了结构类似物,试图扩大抗肿瘤活性谱并降低毒性(急性骨髓抑制和心脏毒性)。本报告涉及我们对111例接受去甲柔红霉素治疗患者的初步临床经验。急性白血病患者采用了两种给药方案。序贯给药对急性白血病复发有效,但黏膜毒性过大;最近,间歇给药在急性白血病复发(一次6mg/kg剂量)以及一名耐药伯基特淋巴瘤患者中显示出活性。在非霍奇金淋巴瘤中,间歇给药方案(3mg/kg/天×3周)的完全缓解率达到71%。还观察到皮肤受累明显缩小。去甲柔红霉素在蕈样肉芽肿中显示出高活性(6例患者中有5例病情缓解),在软组织肉瘤、骨肉瘤和各种实体瘤中也有一定活性。

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