Metastatic spread of cancer to bone is a frequent complication in several types of malignancies. Normal bone metabolic process is affected and the imbalance between bone formation and resorption defines bone disease in cancer. Bisphosphonates are potent inhibitors of osteoclast-mediated bone resorption that also exhibit antitumor activity. In this article, we describe the osteolytic mechanisms, the signaling pathways which are involved and the inhibitory mode of action of bps and the results obtained from a pilot study.