| In this review, we highlight the studies of targeted drugs and their targets utilized in treatments of osteoporosis in the last 3 years. According to the mechanism, the therapeutic strategy includes drugs to enhance activity of alkaline phosphatase (ALP) and long-chain unsaturated fatty acid receptor, and to regulate protein targets and other therapeutic targets. The newly discovered targets and relevant advance are also introduced. ALP is an enzyme secreted by osteoblasts. The expression of ALP is a specific phenotype of osteoblast differentiation. Increase of ALP activity leads to enhanced differentiation of osteoblast and anti-osteoporosis effect. It has been found that long-chain fatty acid receptor GPR30, GPR40, and GPR120 play an important role in the treatment of osteoporosis. Protein kinase K inhibitors that regulate the protein targets can inhibit osteoclasts while do not inhibit new bone formation. They may even stimulate bone formation on the surface of cortical bone. Meanwhile, 6 new targets have been found, including CB2 receptor，TRPV1 receptor, Siglec-15 receptor, DMT1 gene, ER-induced osteoblast signal pathway, and RXR. The progress in osteoporosis-targeted drugs and in the study of targets is striking. This may improve the development of new targeted. |