Repositioning Candidate Details
| Candidate ID: | R1175 |
| Source ID: | DB08879 |
| Source Type: | approved |
| Compound Type: | biotech |
| Compound Name: | Belimumab |
| Synonyms: | Belimumab |
| Molecular Formula: | -- |
| SMILES: | -- |
| DrugBank Description: | Belimumab is an intravenous immunosupressant for the adjunctive treatment of systemic lupus erythematosus (SLE). More specifically, it is a fully human recombinant IgG1λ monoclonal antibody produced from a recombinant NS0 cell line stably transfected with the belimumab heavy chain and light chain genes. It is the first biological treatment approved for the indication of SLE. Concomitant use with live or inactivated vaccines must be avoided. Belimumab was FDA approved on March 9, 2011. Belimumab consists of 2 heavy chains, and 2 light chains of the lambda subclass. Each heavy chain contains 452 amino acid residues and each light chain contains 214 amino acid residues. There are 3 post-translational modifications: a conserved N-linked glycosylation on the CH2 domain at Asn 303 of the heavy chain, the conversion of the N-terminal glutamine residue of the heavy chain into pyroglutamate, and loss of C-terminal lysine residue of the heavy chain. |
| CAS Number: | 356547-88-1 |
| Molecular Weight: | |
| DrugBank Indication: | Adjunct treatment for auto-antibody-positive active systemic lupus erythematosus (SLE). The intravenous injectable form is the only FDA approved treatment for pediatric patients with SLE. |
| DrugBank Pharmacology: | By the 52nd week of treatment with belimumab, a reduction in CD19+, CD20+, naive and activated B cells, plasma cells, plasmacytoid cells, and SLE B-cell subset can be observed. Reductions in plasma cells and SLE B-cell subset can be seen by the eighth week and these levels were maintained to week 52. Belimumab also reduced levels of IgG and anti-dsDNA. |
| DrugBank MoA: | Belimumab selectively binds to soluble human B lymphocyte stimulator protein (BLyS) so that BLyS is unable to bind to receptors on B lymphocytes. The binding of BLyS to its receptor is essential for the survival of B lymphocytes. Consequently, belimumab reduces B-cell mediated immunity and the autoimmune response. |
| Targets: | Tumor necrosis factor ligand superfamily member 13B neutralizer |
| Inclusion Criteria: | Target associated |
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