Belimumab
Identification
- Name
- Belimumab
- Accession Number
- DB08879
- 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.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6358H9904N1728O2010S44
- Protein Average Weight
- 147000.0 Da
- Sequences
- Not Available
- Synonyms
- Not Available
Pharmacology
- 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.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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.
Target Actions Organism ATumor necrosis factor ligand superfamily member 13B neutralizerHumans - Absorption
Cmax, 10 mg/kg, SLE patients = 313 µg/mL; AUC (0-∞), 10 mg/kg, SLE patients = 3083.
- Volume of distribution
Vdss, 10 mg/kg, SLE patients = 5.29 L.
- Protein binding
- Not Available
- Metabolism
Because belimumab is a protein, it is expected that it is degraded into peptides and amino acids by proteolytic enzymes.
- Route of elimination
- Not Available
- 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.
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- 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.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Belimumab. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Belimumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Belimumab. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Belimumab. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Belimumab. Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Belimumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Belimumab. Alirocumab The risk or severity of adverse effects can be increased when Belimumab is combined with Alirocumab. Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Belimumab. Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Belimumab. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBenlysta Injection, powder, lyophilized, for solution 120 mg/1.5mL Intravenous GlaxoSmithKline Manufacturing SpA 2011-03-10 2018-03-12 US 
Benlysta Powder, for solution 400 mg Intravenous Glaxosmithkline Inc 2011-08-24 Not applicable Canada 
Benlysta Injection, powder, for solution 120 mg Intravenous Glaxo Group Limited 2011-07-13 Not applicable EU 
Benlysta Injection, powder, lyophilized, for solution 120 mg/1.5mL Intravenous Human Genome Sciences, Inc. 2011-03-10 Not applicable US Benlysta Solution 200 mg Subcutaneous Glaxosmithkline Inc 2018-05-14 Not applicable Canada Benlysta Injection, powder, lyophilized, for solution 400 mg/5mL Intravenous GlaxoSmithKline Manufacturing SpA 2011-03-10 2018-03-12 US Benlysta Powder, for solution 120 mg Intravenous Glaxosmithkline Inc 2011-08-24 Not applicable Canada Benlysta Injection, powder, lyophilized, for solution 400 mg/5mL Intravenous Human Genome Sciences, Inc. 2011-03-10 Not applicable US Benlysta Solution 200 mg Subcutaneous Glaxosmithkline Inc Not applicable Not applicable Canada Benlysta Injection, powder, for solution 400 mg Intravenous Glaxo Group Limited 2011-07-13 Not applicable EU Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
Categories
- ATC Codes
- L04AA26 — Belimumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antineoplastic and Immunomodulating Agents
- B Lymphocyte Stimulator-directed Antibody Interactions
- B Lymphocyte Stimulator-specific Inhibitor
- Blood Proteins
- Decreased B Lymphocyte Activation
- Globulins
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Proteins
- Selective Immunosuppressants
- Serum Globulins
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
Chemical Identifiers
- UNII
- 73B0K5S26A
- CAS number
- 356547-88-1
References
- General References
- Scott LJ, Burness CB, McCormack PL: Belimumab: a guide to its use in systemic lupus erythematosus. BioDrugs. 2012 Jun 1;26(3):195-9. doi: 10.2165/11209060-000000000-00000. [PubMed:22428610]
- External Links
- KEGG Drug
- D03068
- PubChem Substance
- 347910378
- 1092437
- ChEMBL
- CHEMBL1789843
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Belimumab
- AHFS Codes
- 92:44.00 — Immunosuppressive Agents
- FDA label
- Download (1.59 MB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Systemic Lupus Erythematosus (SLE) 1 4 Completed Treatment Systemic Lupus Erythematosus (SLE) 2 4 Not Yet Recruiting Basic Science Systemic Lupus Erythematosus (SLE) 1 4 Not Yet Recruiting Prevention Systemic Lupus Erythematosus (SLE) 1 4 Recruiting Treatment Lupus Erythematosus / Systemic Lupus Erythematosus (SLE) 1 4 Unknown Status Treatment Systemic Lupus Erythematosus (SLE) 1 3 Active Not Recruiting Treatment Systemic Lupus Erythematosus (SLE) 1 3 Completed Treatment Nephritis, Lupus 1 3 Completed Treatment Systemic Lupus Erythematosus (SLE) 8 3 Completed Treatment Vasculitis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Intravenous 120 mg Injection, powder, for solution Intravenous 400 mg Injection, powder, for solution Intravenous; Parenteral 120 MG Injection, powder, for solution Intravenous; Parenteral 400 MG Injection, powder, lyophilized, for solution Intravenous 120 mg/1.5mL Injection, powder, lyophilized, for solution Intravenous 400 mg/5mL Injection, solution Cutaneous 200 MG Injection, solution, concentrate Intravenous 120 mg Injection, solution, concentrate Intravenous 400 mg Powder, for solution Intravenous 120 mg Powder, for solution Intravenous 400 mg Solution Subcutaneous 200 mg Solution Subcutaneous 200 mg/1mL Injection, solution Intravenous 120 mg Injection Intravenous 400 mg Powder - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataCA2266439 No 2009-06-16 2016-10-25 Canada CA2407910 No 2009-06-16 2021-06-15 Canada Additional Data Available- Filed On
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Neutralizer
- General Function
- Receptor binding
- Specific Function
- Cytokine that binds to TNFRSF13B/TACI and TNFRSF17/BCMA. TNFSF13/APRIL binds to the same 2 receptors. Together, they form a 2 ligands -2 receptors pathway involved in the stimulation of B- and T-ce...
- Gene Name
- TNFSF13B
- Uniprot ID
- Q9Y275
- Uniprot Name
- Tumor necrosis factor ligand superfamily member 13B
- Molecular Weight
- 31222.48 Da
Drug created on May 17, 2013 18:41 / Updated on October 27, 2020 11:13
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