Abstract: Matrix metalloproteinases (MMPs) are a group of zinc and calcium dependent proteolytic enzymes that degrade extracellular matrix and basement membrane. They play very important roles in the processes of tumor angiogenesis, metastasis and invasion. MMP inhibitors (MMPIs) have become the focus of anticancer agents R & D. This paper reviewed the progress in clinical development of MMPIs as anticancer agents, so as to provide references for their further investigation and application.