Bone is the most common site of metastases in patients with solid tumor. Currently, bone metastases are virtually incurable and have high incidence. They can lead to a series of skeletal-related events, thus negatively impacting on the patients′ quality of life and burdening patients′ family financial problems. Biological mechanisms leading to metastases of tumor cells to bone are being studied. Among these are the osteoblast double regulation and osteoprotegerin-receptor activator of nuclear factor-κB ligand-receptor activator of nuclear factor-κB system, osteoclast activation via cytokines which produced by tumor cell and cells in the bone microenvironment as well as the roles of some molecules, such as parathyroid hormone related protein (PTHrP)-mediated vicious cycle. Several attractive molecules or pathways have been identified as new potential therapeutic targets for bone metastases, such as receptor activator of nuclear factor-κB ligand (RANKL), Cathepsin K, PTHrP and Wnt signaling. This review mainly present normal bone biology, metastatic tumor bone biology and the recent clinical advances in cell and molecular targeted therapeutic agents for bone metastases, including bisphosphonates, denosumab-RANKL inhibitor and odanacatib-cathepsin K inhibitor. Hopefully, with better understanding of the biology of the disease and the development of more robust targeted therapeutic drugs, the survival and quality of life of the affected individuals could be significantly improved.