小分子肿瘤血管破坏剂研究进展

Research progress in small molecule vascular disrupting agents

靶向肿瘤血管系统作为肿瘤治疗的策略已经取得了很好的临床疗效。目前上市的药物主要是抑制肿瘤的血管新生,而肿瘤血管具有的分级不规则、网络混乱等特点使得靶向既存的肿瘤血管成为可能。小分子肿瘤血管破坏剂是近年来出现的一类靶向既存血管系统的化合物,该类化合物可以快速、选择性地破坏既存的肿瘤血管网络从而引发肿瘤的坏死。目前已经有多种小分子肿瘤血管破坏剂进入临床前和临床评价,其显示的良好的体内外抗肿瘤效果为肿瘤的治疗提供了新的策略。文中综述小分子血管破坏剂的作用效果、作用机制和临床研究进展,深入理解其具体作用机制对于这类药物的开发具有重要的意义。

Tumor vascular targeting system as a treatment strategy for cancer has achieved promising clinical results.Currently most of the available drugs are tumor angiogenesis inhibitors.The estabolished tumor blood vessels are characterized by irregular grade,network disorder and so on,which makes it possible for targeting the established tumor vascular.In recent years,small molecular vascular disrupting agents（VDAs） have been developed,which can cause rapid and selective disruption of the established tumour blood vessel network,resulting in tumor necrosis.Nowadays,many of them are undergoing preclinical or clinical evaluation.The good in vitro and in vivo antitumor effects suggest that small molecular VDAs is a new strategy for the treatment of cancer.Understanding the mechanism of action and the research progress in the clinical trials of small molecule VDAs is very important in new drug development in this field.