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
Related Articles
Protein chemical formulaC6358H9904N1728O2010S44
Protein average weight147000.0 Da
SequencesNot Available
SynonymsNot Available
External IDs Not Available
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BenlystaPowder, for solution120 mgIntravenousGlaxosmithkline Inc2011-08-24Not applicableCanada
BenlystaInjection, powder, for solution400 mgIntravenousGlaxo Group Limited2011-07-13Not applicableEu
BenlystaPowder, for solution400 mgIntravenousGlaxosmithkline Inc2011-08-24Not applicableCanada
BenlystaInjection, powder, lyophilized, for solution120 mg/1.5mLIntravenousHuman Genome Sciences, Inc.2011-03-10Not applicableUs
BenlystaInjection, powder, for solution120 mgIntravenousGlaxo Group Limited2011-07-13Not applicableEu
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
Categories
UNII73B0K5S26A
CAS number356547-88-1
Pharmacology
Indication

Adjunct treatment for auto-antibody-positive active systemic lupus erythematosus.

Structured Indications
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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Tumor necrosis factor ligand superfamily member 13BProteinyes
neutralizer
HumanQ9Y275 details
Related Articles
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 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 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.

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
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Belimumab.Approved
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Belimumab.Approved
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Belimumab.Approved, Investigational
BCG vaccineThe therapeutic efficacy of Bcg can be decreased when used in combination with Belimumab.Investigational
BelataceptThe risk or severity of adverse effects can be increased when Belatacept is combined with Belimumab.Approved
BenralizumabThe risk or severity of adverse effects can be increased when Medi 563 is combined with Belimumab.Investigational
BevacizumabThe risk or severity of adverse effects can be increased when Bevacizumab is combined with Belimumab.Approved, Investigational
BlinatumomabThe risk or severity of adverse effects can be increased when Blinatumomab is combined with Belimumab.Approved
BlosozumabThe risk or severity of adverse effects can be increased when Ly2541546 is combined with Belimumab.Investigational
BococizumabThe risk or severity of adverse effects can be increased when Pf 04950615 is combined with Belimumab.Investigational
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Brentuximab vedotin is combined with Belimumab.Approved
Certolizumab pegolThe risk or severity of adverse effects can be increased when Certolizumab pegol is combined with Belimumab.Approved
CetuximabThe risk or severity of adverse effects can be increased when Cetuximab is combined with Belimumab.Approved
ClazakizumabThe risk or severity of adverse effects can be increased when Clazakizumab is combined with Belimumab.Investigational
CMC-544The risk or severity of adverse effects can be increased when CMC-544 is combined with Belimumab.Investigational
ConcizumabThe risk or severity of adverse effects can be increased when Concizumab is combined with Belimumab.Investigational
CyclophosphamideThe risk or severity of adverse effects can be increased when Belimumab is combined with Cyclophosphamide.Approved, Investigational
DacetuzumabThe risk or severity of adverse effects can be increased when Dacetuzumab is combined with Belimumab.Investigational
DaclizumabThe risk or severity of adverse effects can be increased when Daclizumab is combined with Belimumab.Approved, Investigational
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Belimumab.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Belimumab.Approved
EculizumabThe risk or severity of adverse effects can be increased when Eculizumab is combined with Belimumab.Approved, Investigational
ElotuzumabThe risk or severity of adverse effects can be increased when Elotuzumab is combined with Belimumab.Approved
EmibetuzumabThe risk or severity of adverse effects can be increased when Ly2875358 is combined with Belimumab.Investigational
EpratuzumabThe risk or severity of adverse effects can be increased when Epratuzumab is combined with Belimumab.Investigational
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Belimumab.Approved, Investigational
EtaracizumabThe risk or severity of adverse effects can be increased when Medi 522 is combined with Belimumab.Investigational
EtrolizumabThe risk or severity of adverse effects can be increased when Etrolizumab is combined with Belimumab.Investigational
FarletuzumabThe risk or severity of adverse effects can be increased when Farletuzumab is combined with Belimumab.Investigational
FingolimodBelimumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FirategrastThe risk or severity of adverse effects can be increased when Sb 683699 is combined with Belimumab.Investigational
FontolizumabThe risk or severity of adverse effects can be increased when Fontolizumab is combined with Belimumab.Investigational
G17DTThe risk or severity of adverse effects can be increased when Belimumab is combined with G17DT.Investigational
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Belimumab.Approved, Investigational, Withdrawn
GevokizumabThe risk or severity of adverse effects can be increased when Gevokizumab is combined with Belimumab.Investigational
IdarucizumabThe risk or severity of adverse effects can be increased when Idarucizumab is combined with Belimumab.Approved
InfliximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Belimumab.Approved
INGN 201The risk or severity of adverse effects can be increased when Belimumab is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Belimumab is combined with INGN 225.Investigational
IpilimumabThe risk or severity of adverse effects can be increased when Ipilimumab is combined with Belimumab.Approved
IxekizumabThe risk or severity of adverse effects can be increased when Ixekizumab is combined with Belimumab.Approved, Investigational
LabetuzumabThe risk or severity of adverse effects can be increased when Labetuzumab is combined with Belimumab.Investigational
LandogrozumabThe risk or severity of adverse effects can be increased when Ly2495655 is combined with Belimumab.Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Belimumab is combined with Leflunomide.Approved, Investigational
LigelizumabThe risk or severity of adverse effects can be increased when Qge031 is combined with Belimumab.Investigational
MatuzumabThe risk or severity of adverse effects can be increased when Matuzumab is combined with Belimumab.Investigational
MepolizumabThe risk or severity of adverse effects can be increased when Mepolizumab is combined with Belimumab.Approved, Investigational
Mirvetuximab SoravtansineThe risk or severity of adverse effects can be increased when Mirvetuximab Soravtansine is combined with Belimumab.Investigational
MuromonabThe risk or severity of adverse effects can be increased when Muromonab is combined with Belimumab.Approved, Investigational
NatalizumabThe risk or severity of adverse effects can be increased when Belimumab is combined with Natalizumab.Approved, Investigational
NecitumumabThe risk or severity of adverse effects can be increased when Necitumumab is combined with Belimumab.Approved
NivolumabThe risk or severity of adverse effects can be increased when Nivolumab is combined with Belimumab.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Obinutuzumab is combined with Belimumab.Approved
OfatumumabThe risk or severity of adverse effects can be increased when Ofatumumab is combined with Belimumab.Approved
OlokizumabThe risk or severity of adverse effects can be increased when Cdp6038 is combined with Belimumab.Investigational
OmalizumabThe risk or severity of adverse effects can be increased when Omalizumab is combined with Belimumab.Approved, Investigational
OtelixizumabThe risk or severity of adverse effects can be increased when TRX4 is combined with Belimumab.Investigational
OzanezumabThe risk or severity of adverse effects can be increased when Gsk1223249 is combined with Belimumab.Investigational
PalivizumabThe risk or severity of adverse effects can be increased when Palivizumab is combined with Belimumab.Approved, Investigational
PanitumumabThe risk or severity of adverse effects can be increased when Panitumumab is combined with Belimumab.Approved, Investigational
PembrolizumabThe risk or severity of adverse effects can be increased when Pembrolizumab is combined with Belimumab.Approved
PertuzumabThe risk or severity of adverse effects can be increased when Pertuzumab is combined with Belimumab.Approved
PexelizumabThe risk or severity of adverse effects can be increased when Pexelizumab is combined with Belimumab.Investigational
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Belimumab.Approved, Investigational
RamucirumabThe risk or severity of adverse effects can be increased when Ramucirumab is combined with Belimumab.Approved, Investigational
RanibizumabThe risk or severity of adverse effects can be increased when Ranibizumab is combined with Belimumab.Approved
RI 624The risk or severity of adverse effects can be increased when RI 624 is combined with Belimumab.Investigational
RindopepimutThe risk or severity of adverse effects can be increased when Belimumab is combined with CDX-110.Investigational
RituximabThe risk or severity of adverse effects can be increased when Rituximab is combined with Belimumab.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Belimumab.Approved
RontalizumabThe risk or severity of adverse effects can be increased when Rontalizumab is combined with Belimumab.Investigational
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Belimumab.Approved
SRP 299The risk or severity of adverse effects can be increased when Belimumab is combined with SRP 299.Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Belimumab.Approved, Investigational
TanezumabThe risk or severity of adverse effects can be increased when Rn624 is combined with Belimumab.Investigational
TNX-901The risk or severity of adverse effects can be increased when TNX-901 is combined with Belimumab.Investigational
TocilizumabThe risk or severity of adverse effects can be increased when Tocilizumab is combined with Belimumab.Approved
TofacitinibBelimumab may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TrastuzumabThe risk or severity of adverse effects can be increased when Trastuzumab is combined with Belimumab.Approved, Investigational
Trastuzumab emtansineThe risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Belimumab.Approved
UstekinumabThe risk or severity of adverse effects can be increased when Ustekinumab is combined with Belimumab.Approved, Investigational
VedolizumabThe risk or severity of adverse effects can be increased when Vedolizumab is combined with Belimumab.Approved
Food InteractionsNot 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 — Belimumab
AHFS Codes
  • 92:44
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentSystemic Lupus Erythematosus (SLE)2
1RecruitingTreatmentSystemic Lupus Erythematosus (SLE)1
1, 2RecruitingTreatmentKidney Transplant Rejection1
2Active Not RecruitingTreatmentNephritis, Lupus1
2CompletedTreatmentGlomerulonephritis, Membranous1
2CompletedTreatmentLupus Erythematosus, Systemic1
2CompletedTreatmentMyasthaenia Gravis1
2CompletedTreatmentRheumatoid Arthritis1
2CompletedTreatmentSclerosis, Progressive Systemic1
2CompletedTreatmentSjögren's Syndrome2
2CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
2CompletedTreatmentTransplantation, Organ1
2RecruitingTreatmentLupus Erythematosus, Systemic1
2RecruitingTreatmentSjogren's Syndrome1
2RecruitingTreatmentSystemic Lupus Erythematosus (SLE)1
2TerminatedTreatmentDesensitization Before Kidney Transplant1
2TerminatedTreatmentRheumatoid Arthritis1
2TerminatedTreatmentSystemic Lupus Erythematosus (SLE)1
2Unknown StatusTreatmentSymptomatic Waldenstroms Macroglobulinaemia1
2WithdrawnNot AvailablePurpura, Thrombocytopaenic, Idiopathic1
2WithdrawnTreatmentGlomerulonephritis, Membranous1
2, 3RecruitingTreatmentMuscle Inflammation1
3Active Not RecruitingTreatmentSystemic Lupus Erythematosus (SLE)2
3CompletedTreatmentSystemic Lupus Erythematosus (SLE)5
3CompletedTreatmentVasculitis1
3RecruitingTreatmentNephritis, Lupus1
3RecruitingTreatmentSystemic Lupus Erythematosus (SLE)1
4CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
4No Longer AvailableNot AvailableRheumatoid Arthritis1
4RecruitingTreatmentSystemic Lupus Erythematosus (SLE)2
Not AvailableAvailableNot AvailableSystemic Lupus Erythematosus (SLE)1
Not AvailableCompletedNot AvailableLupus Erythematosus, Discoid1
Not AvailableCompletedNot AvailableSystemic Lupus Erythematosus (SLE)1
Not AvailableRecruitingNot AvailableSystemic Lupus Erythematosus (SLE)2
Pharmacoeconomics
ManufacturersNot Available
PackagersNot 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
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
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

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
Drug created on May 17, 2013 18:41 / Updated on August 17, 2016 12:24