Belimumab

Identification

Summary

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.

Brand Names
Benlysta
Generic Name
Belimumab
DrugBank Accession Number
DB08879
Background

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
Db08879
Protein Chemical Formula
C6358H9904N1728O2010S44
Protein Average Weight
147000.0 Da
Sequences
Not Available
Synonyms
  • Belimumab

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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
ATumor necrosis factor ligand superfamily member 13B
neutralizer
Humans
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
Adverseeffects
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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.

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.
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Belimumab.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Belimumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Belimumab.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Belimumab.
AducanumabThe risk or severity of adverse effects can be increased when Belimumab is combined with Aducanumab.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Belimumab.
AlefaceptThe risk or severity of adverse effects can be increased when Alefacept is combined with Belimumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Belimumab.
AlirocumabThe risk or severity of adverse effects can be increased when Belimumab is combined with Alirocumab.
Allogeneic processed thymus tissueThe therapeutic efficacy of Allogeneic processed thymus tissue can be decreased when used in combination with Belimumab.
Interactions
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BenlystaInjection, solution200 mgSubcutaneousGlaxo Smith Kline (Ireland) Limited2020-12-16Not applicableEU flag
BenlystaInjection, powder, lyophilized, for solution120 mg/1.5mLIntravenousGlaxoSmithKline Manufacturing SpA2011-03-102018-03-12US flag
BenlystaSolution200 mg / 1 mLSubcutaneousGlaxosmithkline Inc2018-05-14Not applicableCanada flag
BenlystaInjection, solution200 mgSubcutaneousGlaxo Smith Kline (Ireland) Limited2020-12-16Not applicableEU flag
BenlystaPowder, for solution400 mg / vialIntravenousGlaxosmithkline Inc2011-08-24Not applicableCanada flag
BenlystaInjection, powder, lyophilized, for solution120 mg/1.5mLIntravenousGlaxoSmithKline LLC2011-03-10Not applicableUS flag
BenlystaInjection, solution200 mgSubcutaneousGlaxo Smith Kline (Ireland) Limited2020-12-16Not applicableEU flag
BenlystaInjection, powder, lyophilized, for solution400 mg/5mLIntravenousGlaxoSmithKline Manufacturing SpA2011-03-102018-03-12US flag
BenlystaSolution200 mg / 1 mLSubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada flag
BenlystaInjection, solution200 mgSubcutaneousGlaxo Smith Kline (Ireland) Limited2020-12-16Not applicableEU flag

Categories

ATC Codes
L04AA26 — Belimumab
Drug Categories
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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
73B0K5S26A
CAS number
356547-88-1

References

General References
  1. 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. [Article]
KEGG Drug
D03068
PubChem Substance
347910378
RxNav
1092437
ChEMBL
CHEMBL1789843
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Belimumab
FDA label
Download (1.59 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentSystemic Lupus Erythematosus (SLE)1
4CompletedTreatmentSystemic Lupus Erythematosus (SLE)2
4Not Yet RecruitingBasic ScienceSystemic Lupus Erythematosus (SLE)1
4Not Yet RecruitingTreatmentSystemic Lupus Erythematosus (SLE)3
4RecruitingPreventionSystemic Lupus Erythematosus (SLE)1
4RecruitingTreatmentIgG4 Related Disease1
4RecruitingTreatmentLupus Erythematosus / Systemic Lupus Erythematosus (SLE)1
4Unknown StatusTreatmentSystemic Lupus Erythematosus (SLE)1
3CompletedTreatmentLupus Nephritis1
3CompletedTreatmentSystemic Lupus Erythematosus (SLE)9

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionIntravenous120 MG
Injection, powder, for solutionIntravenous400 MG
Injection, powder, lyophilized, for solutionIntravenous120 mg/1.5mL
Injection, powder, lyophilized, for solutionIntravenous400 mg/5mL
Injection, solutionParenteral; Subcutaneous200 MG
Injection, solutionSubcutaneous200 mg
Powder, for solutionIntravenous120 mg / vial
Powder, for solutionIntravenous400 mg / vial
SolutionSubcutaneous200 mg/1mL
SolutionSubcutaneous200 mg / 1 mL
Injection, solutionIntravenous
Injection, powder, lyophilized, for solutionIntravenous120 mg
InjectionIntravenous
Injection, powder, lyophilized, for solutionIntracavernous400 mg
Injection, powder, for solutionIntravenous
Injection, powder, lyophilized, for solutionIntravenous400 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2266439No2009-06-162016-10-25Canada flag
CA2407910No2009-06-162021-06-15Canada flag

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets2
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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 18, 2013 00:41 / Updated on October 16, 2021 12:32