Abstract: Bisphosphonate is one of the important antibone absorbents in the treatment of bone metabolic diseases. It is mainly used in Paget's disease, osteoporosis and bone disease associated with tumor. Bisphosphonates are not only used to treat bone-related diseases, but bisphosphonate functionalized imaging agents are widely used in the diagnosis of bone-related diseases in nuclear medical bone imaging. The radioactive tracer can be coupled with bisphosphonates by chelation, and the coupled probe can be used as a bone targeting tracer for bone imaging. The molecular structure of bisphosphonates contains P-C-P bonds, so they are resistant to enzymatic hydrolysis and are not easily hydrolyzed by enzymes in human body. Because of its high affinity with inorganic hydroxyapatite crystals in bone tissue, it has high selectivity in bone tissue. This paper is based on the general characteristics and mechanism of bisphosphonates and summarized the preclinical study on the treatment of osteoporosis with bisphosphonates and the application of bisphosphonates in the treatment of bone metastasis.