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| Primary information |
|---|
| ID | 10637 |
| Therapeutic ID | Th1132 |
| Protein Name | Belimumab |
| Sequence | NA
|
| Molecular Weight | 147000 |
| Chemical Formula | C 6358 H 9904 N 1728 O 2010 S 44 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting point | NA |
| Half-life | Elimination half life- 19.4 days, Distribution half life- 1.75 days |
| Description | RAV12 is a monoclonal antibody that is being studied in the treatment of certain cancers.It binds to a carbohydrate molecule found on gastric, colon, pancreatic, prostate, ovarian, breast, and kidney cancer cells. Administering RAV12 along with gemcitabine may kill more tumor cells than either one alone. |
| Indication/Disease | Adjunct treatment for auto-antibody-positive active systemic lupus erythematosus. |
| Pharmacodynamics | 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. |
| Mechanism of Action | 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. |
| Toxicity | The most commonly-reported adverse reactions, occurring in =5% of patients in clinical trials were nausea, diarrhea, pyrexia, nasopharyngitis, bronchitis, insomnia, pain in extremity, depression, migraine, and pharyngitis. The most common serious adverse reactions were serious infections. |
| Metabolism | Because belimumab is a protein, it is expected that it is degraded into peptides and amino acids by proteolytic enzymes. |
| Absorption | Cmax, 10 mg/kg, SLE patients = 313 µg/mL; AUC (0-8), 10 mg/kg, SLE patients = 3083. |
| Vdss, 10 mg/kg, SLE patients = 5.29 L. |
| Clearance | Systemic clearance, 10 mg/kg, SLE patients = 215 mL/day. |
| Categories | Monoclonal antibodies |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | NA |
| Target | Tumor necrosis factor ligand superfamily member 13B |
| Brand Name | Benlysta |
| Company | GlaxoSmithKline |
| Brand Description | GlaxoSmithKline |
| Prescribed For | NA |
| Chemical Name | NA |
| Formulation | Upon reconstitution with Sterile Water for Injection, USP, each single-use vial delivers 80 mg/mL belimumab in 0.16 mg/mL citric acid, 0.4 mg/mL polysorbate 80, 2.7 mg/mL sodium citrate, and 80 mg/mL sucrose, with a pH of 6.5. |
| Physical Appearance | BENLYSTA is supplied as a sterile, white to off-white, preservative-free, lyophilized powder for Intravenous infusion |
| Route of Administration | Intravenous infusion |
| Recommended Dosage | 10 mg/kg at 2-week intervals for the first 3 doses and at 4-week intervals thereafter. Reconstitute, dilute, and administer as an Intravenous infusion only, over a period of 1 hour. |
| Contraindication | anaphylaxis with belimumab |
| Side Effects | Mortality, Serious Infections, Malignancy, Hypersensitivity Reactions, Including Anaphylaxis, Infusion Reactions, Depression |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |