贝利尤单抗 (Benlysta)

概览

Belimumab is a B-lymphocyte stimulator (BLyS)-specific inhibitor used to treat systemic lupus erythematosus and active lupus nephritis as an add-on therapy.

作用机制

Systemic lupus erythematosus (SLE) and lupus nephritis, a common and serious manifestation of SLE, are autoimmune disorders characterized by the presence of autoreactive B lymphocytes (B cells), which promotes the production of autoantibodies that cause inflammation and progressive and irreversible tissue damage. One of the key cytokines involved in B cell homeostasis and survival is B lymphocyte stimulator protein (BLyS), which is a member of tumour necrosis factor (TNF) superfamily of cytokines. While the contribution of BLyS to the pathophysiology of autoimmune diseases is not fully understood, BLyS has been identified as a key therapeutic target for the treatment of SLE as BLyS levels are elevated in patients with SLE along with other autoimmune diseases. Belimumab is an antibody directed against BLyS: it selectively binds BLyS with high affinity, neutralizes it, and blocks its interaction with B cell receptors - transmembrane activator and calcium-modulator and cyclophilin ligand interactor (TACI), B-cell maturation antigen (BCMA), and BLyS receptor 3 (BR3). Belimumab ultimately inhibits the survival of B cells, promotes apoptosis, and reduces the differentiation and maturation of B cells into immunoglobulin-producing plasma cells.

适应症

In the US, belimumab is indicated to treat active systemic lupus erythematosus (SLE) and active lupus nephritis in patients aged five years and older who are receiving standard therapy. In Europe, belimumab is also used to treat SLE and lupus nephritis but only in adults. The efficacy of belimumab has not been evaluated in patients with severe active central nervous system lupus. Use of belimumab is not recommended in this situation.

• Active Systemic Lupus Erythematosus
• Lupus Nephritis