delanzomib

Delanzomib is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, developed primarily for cancer therapy. It acts as a proteasome inhibitor, inducing apoptosis in multiple myeloma and other hematological and solid tumor cell lines by blocking proteasomal degradation of proteins such as IkappaBalpha. This leads to cytoplasmic sequestration of NF-kappaB, inhibition of its nuclear translocation, downregulation of cell growth-promoting factors, and ultimately apoptotic cell death in susceptible tumor cells. Delanzomib has shown favorable cytotoxicity profiles compared to bortezomib in preclinical studies and also exhibits antiangiogenic activity and repression of osteoclastogenesis. It was initially developed by Cephalon (a subsidiary of Teva) for multiple myeloma but has also been investigated for non-Hodgkin lymphoma, solid tumors, rheumatoid arthritis (preclinical), and systemic lupus erythematosus (preclinical). Clinical development reached phase II for multiple myeloma before discontinuation; trials continue at phase I for non-Hodgkin lymphoma and solid tumors[1][2][3][4][5][7].

Other names

847499-27-8