Belimumab
Belimumab Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
| Trade Name | Belimumab |
| Availability | Prescription only |
| Generic | Belimumab |
| Belimumab Other Names | Belimumab |
| Related Drugs | Benlysta, aspirin, prednisone, dexamethasone, triamcinolone, hydroxychloroquine, Plaquenil, Lupkynis, voclosporin |
| Weight | 120mg, 400mg, 200mg/ml, |
| Type | Intravenous Powder For Injection, Subcutaneous Solution, Intravenous |
| Formula | C6358H9904N1728O2010S44 |
| Weight | 147000.0 Da |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Belimumab is a B-lymphocyte stimulator (BLyS)-specific inhibitor that indirectly inhibits B cell survival, and is used to treat patients with autoantibody positive, active systemic lupus erythematosus.
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.
Belimumab is also used to associated treatment for these conditions: Active autoantibody-positive Systemic lupus erythematosus
How Belimumab works
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.
Food Interaction
No interactions found.Belimumab Drug Interaction
Unknown: charcoal, pioglitazone, amphetamine / dextroamphetamine, amoxicillin / clavulanate, loratadine, glucose, hydromorphone, arginine, levocarnitine, cysteine, lithium, acetaminophen, hydroxychloroquine, valproic acid, thiamine, cyanocobalamin, pyridoxine, cholecalciferol, phytonadione, menaquinone
Belimumab Disease Interaction
Volume of Distribution
Vdss, 10 mg/kg, SLE patients = 5.29 L.
Elimination Route
Cmax, 10 mg/kg, SLE patients = 313 µg/mL; AUC (0-∞), 10 mg/kg, SLE patients = 3083.
Half Life
Terminal elimination half-life, 10 mg/kg, SLE patients= 19.4 days; Distribution half-life, 10 mg/kg, SLE patients = 1.75 days.
Clearance
Systemic clearance, 10 mg/kg, SLE patients = 215 mL/day.
Innovators Monograph
You find simplified version here Belimumab
