Wnt/β-catenin signaling pathway is an important cellular signal transduction pathway and plays an important role in cell proliferation and differentiation. Current researchs indicate that Wnt/β-catenin signaling pathway is significant in bone metabolism and its abnormalities relate to the occurrence of osteoporosis. Wnt/β-catenin signaling pathway antagonists can inhibit the Wnt/β-catenin signaling pathway and cause the pathway abnormal expression. Further studys of the Wnt/β-catenin signaling pathway antagonists and designing the materials to block the pathway antagonists can provide a new kind of osteoporosis treatment approach.