Abstract: Given its pivotal role in growth and survival, the tumor vasculature represents an attractive target for anticancer therapy. Over the last few decades, rapid progress has been achieved in the understanding of tumor angiogenesis including signaling pathways and their regulation. This has enabled the development of numerous potentially effective vasculature-targeted anticancer drugs (VTAD), which are being tested in the clinical setting. In this review I will focus on the most promising and advanced drugs targeting the tumor vasculature, briefly summarizing their mechanism of action and the clinical results so far obtained.