The matrix metalloproteinases represent an attractive target for cancer treatment, and a number of matrix metalloproteinase inhibitors are undergoing clinical trials. The results of these studies will establish whether any of these compounds are therapeutically useful. Independent of the conclusions from the first generation of studies, the field of matrix metalloproteinase inhibitors remains attractive for creative and innovative research. In the future, the development of novel, less toxic, and more effective matrix metalloproteinase inhibitors, and the combination of conventional agents with these novel anticancer agents will constitute the main focus of research efforts.