VBY-825 is a novel, potent and reversible cathepsin inhibitor with high activity against cathepsins B, L, S and V. VBY-825 had no effect on body weight or IgG2b level, frequency of soft tissue tumors or intraosseous tumor area. VBY-825 decreased total and MOLA, consistent with inhibited resorption. There was also a trend of increased relative trabecular bone area. Serum TRACP 5b activity in the VBY-825 treated group did not differ from the respective vehicle group, whereas the number of osteoclasts at tumor-bone interface was increased in VBY-825 treated animals. These findings suggest that VBY-825 decreased osteoclast function and resorption activity without decreasing the number of osteoclasts In conclusion, VBY-825 had no effects on tumor growth but it inhibited bone destruction in this mouse model of MM, which is consistent with its potency on cathepsin S and K, which are known to be important in osteoclast-mediated bone resorption. VBY-825 is a promising candidate for the treatment of tumor-associated bone disease.

纯度：≥98%

CAS：1310340-58-9