Abstract: Zoledronic acid belongs to the third generation of diphosphonate and mainly be applied for treatment of malignant hypercalcinemia and bone metastasis. Except inhibiting bone resorption, it also has direct and indirect antitumor activities. Antiangiogenesis effect is one kind of its indirect antitumor activities, by inhibiting the secretion of VEGF from tumor cells and mesenchyma cells to regulate VEGF-VEGFR endocrine cycle, depressing migration and adhesion of endothelial cells, inducing apoptosis of endothelial progenitor cells, inhibiting the secretion of MMPs from tumor cells and tumor-associated macrophages(TAM) and inhibiting vasculogenic mimicry of tumor cells. However, the dose of Zoledronic acid used for antineoplastic activity is different from that for bone metastasis. How it can inhibit vasculogenic mimicry is still needed further research.