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长春地辛:一种新的长春花生物碱。

Vindesine: a new vinca alkaloid.

作者信息

Bayssas M, Gouveia J, de Vassal F, Misset J L, Schwarzenberg L, Ribaud P, Musset M, Jasmin C, Hayat M, Mathé G

出版信息

Recent Results Cancer Res. 1980;74:91-7. doi: 10.1007/978-3-642-81488-4_13.

Abstract

Vindesine (VDS) is an analogue of the vinca alkaloids. Its spectrum of antitumoral activity is similar to that of vincristine (VCR), but with milder experimental neurotoxicity, and it inhibits the polymerization of tubulin. Its terminal half-life is 24 h and its plasma clearance is intermediate between those of vinblastine (VLB) and VCR. The maximal tolerated dose is 4-5 mg/m2/week, the dose-limiting toxicity being myelosuppression (nadir by days 7-8 and recovery by days 11-13). It has already been demonstrated as efficient in childhood acute lymphoid leukemia (ALL), non-Hodgkin's lymphoma, blastic crisis of chronic myeloid leukemia, and esophageal carcinoma. It has also shown activity in Hodgkin's disease, breast and germ cell carcinomas, and melanoma. Intolerance is mainly neurologic, with paresthesias, without motor impairment, or hematologic, with leukopenia, and sometimes alopecia, asthenia, and muscle pains. The results are better if the patients have not been treated previously; continuous infusion could be of interest and there appears to be no cross-resistance with its parent VCR, as documented in ALL.

摘要

长春地辛(VDS)是长春花生物碱的类似物。其抗肿瘤活性谱与长春新碱(VCR)相似,但实验性神经毒性较轻,且能抑制微管蛋白的聚合。其终末半衰期为24小时,血浆清除率介于长春碱(VLB)和VCR之间。最大耐受剂量为4 - 5mg/m²/周,剂量限制性毒性为骨髓抑制(第7 - 8天达到最低点,第11 - 13天恢复)。它已被证明对儿童急性淋巴细胞白血病(ALL)、非霍奇金淋巴瘤、慢性髓性白血病急变期和食管癌有效。它在霍奇金病、乳腺癌、生殖细胞癌和黑色素瘤中也显示出活性。不耐受主要表现为神经方面,有感觉异常但无运动障碍,或血液方面,有白细胞减少,有时还有脱发、乏力和肌肉疼痛。如果患者以前未接受过治疗,结果会更好;持续输注可能有意义,并且如在ALL中所记录的那样,与母体VCR似乎不存在交叉耐药性。

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