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Identification
NameBelimumab
Accession NumberDB08879
TypeBiotech
GroupsApproved
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.

Protein structureDb08879
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Protein chemical formulaC6358H9904N1728O2010S44
Protein average weight147000.0 Da
SequencesNot Available
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Benlystainjection, powder, lyophilized, for solution120 mg/1.5mLintravenousHuman Genome Sciences, Inc.2011-03-10Not applicableUs
Benlystapowder for solution400 mgintravenousGlaxosmithkline Inc2011-08-24Not applicableCanada
Benlystapowder for solution120 mgintravenousGlaxosmithkline Inc2011-08-24Not applicableCanada
Benlystainjection, powder, lyophilized, for solution400 mg/5mLintravenousHuman Genome Sciences, Inc.2011-03-10Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII73B0K5S26A
CAS number356547-88-1
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationAdjunct treatment for auto-antibody-positive active systemic lupus erythematosus.
PharmacodynamicsBy 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 actionBelimumab 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.
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AbsorptionCmax, 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 bindingNot Available
Metabolism

Because belimumab is a protein, it is expected that it is degraded into peptides and amino acids by proteolytic enzymes.

Route of eliminationNot Available
Half lifeTerminal 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.

ToxicityThe 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintravenous120 mg/1.5mL
Injection, powder, lyophilized, for solutionintravenous400 mg/5mL
Powder for solutionintravenous120 mg
Powder for solutionintravenous400 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2266439 No2009-06-162016-10-25Canada
CA2407910 No2009-06-162021-06-15Canada
Properties
StateLiquid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
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. [PubMed:22428610 ]
External Links
ATC CodesL04AA26
AHFS Codes
  • 92:44
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
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.
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 Alirocumab is combined with Belimumab.
BasilThe risk or severity of adverse effects can be increased when Basil is combined with Belimumab.
BasiliximabThe risk or severity of adverse effects can be increased when Basiliximab is combined with Belimumab.
BelataceptThe risk or severity of adverse effects can be increased when Belatacept is combined with Belimumab.
BevacizumabThe risk or severity of adverse effects can be increased when Bevacizumab is combined with Belimumab.
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Brentuximab vedotin is combined with Belimumab.
CanakinumabThe risk or severity of adverse effects can be increased when Canakinumab is combined with Belimumab.
CyclophosphamideThe risk or severity of adverse effects can be increased when Belimumab is combined with Cyclophosphamide.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Belimumab.
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Belimumab.
EculizumabThe risk or severity of adverse effects can be increased when Eculizumab is combined with Belimumab.
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Belimumab.
EvolocumabThe risk or severity of adverse effects can be increased when Evolocumab is combined with Belimumab.
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Belimumab.
golimumabThe risk or severity of adverse effects can be increased when golimumab is combined with Belimumab.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ibritumomab is combined with Belimumab.
InfliximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Belimumab.
IpilimumabThe risk or severity of adverse effects can be increased when Ipilimumab is combined with Belimumab.
LeflunomideThe risk or severity of adverse effects can be increased when Belimumab is combined with Leflunomide.
NatalizumabThe risk or severity of adverse effects can be increased when Natalizumab is combined with Belimumab.
NivolumabThe risk or severity of adverse effects can be increased when Nivolumab is combined with Belimumab.
ObinutuzumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Belimumab.
OmalizumabThe risk or severity of adverse effects can be increased when Omalizumab is combined with Belimumab.
PalivizumabThe risk or severity of adverse effects can be increased when Palivizumab is combined with Belimumab.
PertuzumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Belimumab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Belimumab.
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Belimumab.
RamucirumabThe risk or severity of adverse effects can be increased when Ramucirumab is combined with Belimumab.
RanibizumabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Belimumab.
RaxibacumabThe risk or severity of adverse effects can be increased when Raxibacumab is combined with Belimumab.
RituximabThe risk or severity of adverse effects can be increased when Rituximab is combined with Belimumab.
RoflumilastRoflumilast may increase the immunosuppressive activities of Belimumab.
SecukinumabThe risk or severity of adverse effects can be increased when Secukinumab is combined with Belimumab.
SiltuximabThe risk or severity of adverse effects can be increased when Siltuximab is combined with Belimumab.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Belimumab.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belimumab.
TocilizumabThe risk or severity of adverse effects can be increased when Tocilizumab is combined with Belimumab.
TofacitinibBelimumab may increase the immunosuppressive activities of Tofacitinib.
TositumomabThe risk or severity of adverse effects can be increased when Tositumomab is combined with Belimumab.
TrastuzumabThe risk or severity of adverse effects can be increased when Trastuzumab is combined with Belimumab.
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when ado-trastuzumab emtansine is combined with Belimumab.
UstekinumabThe risk or severity of adverse effects can be increased when Ustekinumab is combined with Belimumab.
VedolizumabThe risk or severity of adverse effects can be increased when Vedolizumab is combined with Belimumab.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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-cell function and the regulation of humoral immunity. A third B-cell specific BAFF-receptor (BAFFR/BR3) promotes the survival of mature B-cells and the B-cell response.Isoform 2 seems to inhibit isoform...
Gene Name:
TNFSF13B
Uniprot ID:
Q9Y275
Molecular Weight:
31222.48 Da
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Drug created on May 17, 2013 18:41 / Updated on March 14, 2016 10:05