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肿瘤血管导向治疗作为肿瘤治疗新策略已被广泛接受，其理论依据可归纳于两点：（１）肿瘤的持续生长和侵袭转移依赖于血管生成；（２）肿瘤新生血管不同于正常血管．后者是靶向治疗的关键．在肿瘤血管生成过程中，内皮细胞快速增殖及迁移，过度表达一些正常血管不表达或低表达的分子，内皮周细胞和血管基底膜缺乏，血管渗漏性高．肿瘤血管生成的每一个环节中出现的异常分子，理论上都可作为肿瘤导向治疗的靶标，大概可分为三类，即血管内皮细胞、细胞黏附分子和基底膜．
As a new strategy for tumor treatment, tumor vasculotherapy has been widely accepted. Its theoretical basis can be summarized in two points: (1) The continuous growth and invasion and metastasis of tumor depend on angiogenesis; (2) Tumor neovascularization is different from normal blood vessels. The latter is the key to targeted therapy. In the course of tumor angiogenesis, endothelial cells rapidly proliferate and migrate, over-expressing some molecules that are not expressed or lowly expressed in normal blood vessels, lack of endothelial cells and vascular basement membrane, and high blood vessel leakage. Abnormal molecules that appear in every aspect of tumor angiogenesis can theoretically serve as targets for tumor-directed therapy, and can be divided into three categories, namely, vascular endothelial cells, cell adhesion molecules, and basement membrane.