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长春瑞滨(诺维本):一种第三代长春花生物碱。

Vinorelbine (Navelbine): a third-generation vinca alkaloid.

作者信息

Budman D R

机构信息

Don Monti Division of Oncology, North Shore University Hospital, Manhasset, New York, USA.

出版信息

Cancer Invest. 1997;15(5):475-90. doi: 10.3109/07357909709047587.

Abstract

The vinca alkaloids represent one of the oldest classes of antineoplastic agents used in humans with a wide spectrum of activity against both animal and human tumors. These agents are known to inhibit microtubule polymerization. Vinorelbine is a semisynthetic analog that reached clinical trial on the basis of less preclinical evidence of toxicity to neuronal tissue and greater cytotoxic activity in preclinical models than the older compounds of this class. In humans, the clearance of this agent shows a wide variation among subjects with the predominant toxicity being hematological. Significant antitumor activity has been observed in diseases that previously have been shown to respond to vinca alkaloids.

摘要

长春花生物碱是用于人类的最古老的一类抗肿瘤药物之一,对动物和人类肿瘤均具有广泛的活性。已知这些药物可抑制微管聚合。长春瑞滨是一种半合成类似物,基于其对神经组织毒性的临床前证据较少,且在临床前模型中比该类旧化合物具有更大的细胞毒性活性,从而进入临床试验。在人类中,该药物的清除率在受试者之间存在很大差异,主要毒性为血液学毒性。在先前已证明对长春花生物碱有反应的疾病中观察到了显著的抗肿瘤活性。

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