DT-Web

DB08879 - Belimumab


Identification
Name Belimumab
Accession Number DB08879
Type biotech
Description Belimumab is an intravenous immunosupressant for the adjunctive treatment of systemic lupus erythematosus (SLE). More specifically, it is a fully human recombinant monoclonal IgG antibody and is the first biological treatment approved for this indication (SLE). Avoid concomitant use with live or inactivated vaccines. FDA approved on March 9, 2011.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 147 kDa
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication Adjunct treatment of autoantibody-positive active systemic lupus erythematosus
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.
Absorption Cmax, 10 mg/kg, SLE patients = 313 ug/mL; AUC (0-?), 10 mg/kg, SLE patients = 3083
Protein binding Not Available
Biotransformation 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
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
Interactions
Drug Interactions
Drug Mechanism of interaction
ado-trastuzumab emtansine Avoid combination due to the increased risk of belimumab associated side effects.
Belatacept Belimumab increases the immunosupressive effect. Interaction is significant so monitor closely.
Denosumab Belimumab increases the immunosupressive effect. Interaction is significant so monitor closely.
Fingolimod Belimumab increases the immunosupressive effect. Interaction is significant so monitor closely.
golimumab Avoid combination with belimumab due to the increased chance of belimumab associated side effects.
Hydroxyurea Belimumab increases the immunosupressive effect. Interaction is significant so monitor closely.
Food Interactions Not Available

Targets


Tumor necrosis factor ligand superfamily member 13B
Name Tumor necrosis factor ligand superfamily member 13B
Gene Name TNFSF13B
Pharmacological action yes
Actions neutralizer
References
  • Touma Z, Urowitz MB, Gladman DD: Systemic lupus erythematosus: an update on current pharmacotherapy and future directions. Expert Opin Biol Ther. 2013 May;13(5):723-37. doi: 10.1517/14712598.2013.764411. Epub 2013 Jan 23. Pubmed -
DTHybrid score 0.8993

Predictions


Id Partner name Gene Name Score
3352 Structural polyprotein Not Available 0.2356
3628 Structural polyprotein Not Available 0.2356
4892 Structural polyprotein Not Available 0.2356
2548 Subtilisin Carlsberg apr 0.1648
5591 Complement component C8 gamma chain C8G 0.0111
5577 N5-carboxyaminoimidazole ribonucleotide mutase purE 0.0111
2300 Lysozyme E 0.0111
3633 Lysozyme R 0.0111
5597 Lysozyme 17 0.0111
5582 Regulator of transcription; stringent starvation protein A sspA 0.0111
2838 Ribose-5-phosphate isomerase A rpiA 0.0111
2952 Ribose-5-phosphate isomerase A rpiA 0.0111
5595 Ribose-5-phosphate isomerase A rpiA 0.0111
5598 Glycerol uptake operon antiterminator-related protein TM_1436 0.0111
4238 50S ribosomal protein L4 rplD 0.0111
5578 50S ribosomal protein L4 rplD 0.0111
6173 50S ribosomal protein L4 rplD 0.0111
6219 50S ribosomal protein L4 rplD 0.0111
4695 UPF0124 protein yfiH yfiH 0.0111
5590 N utilization substance protein B homolog nusB 0.0111
5588 Cell division protein FtsY TM_0570 0.0111
5592 Ribonucleoside-diphosphate reductase subunit beta nrdF 0.0111
5583 RNA 3'-terminal phosphate cyclase rtcA 0.0111
5587 Iron(III)-binding periplasmic protein fbpA 0.0111
5600 Pyruvate decarboxylase pdc 0.0111
3792 KHG/KDPG aldolase [Includes: 4-hydroxy-2-oxoglutarate aldolase eda 0.0111
5593 Transferase Not Available 0.0111
5581 Beta-fructosidase bfrA 0.0111
5060 Intron-associated endonuclease 1 ITEVIR 0.0111
4375 Glutamine synthetase 1 glnA1 0.0111
5575 Short tail fiber protein 12 0.011
5574 Invasin YPTB1668 0.011
5586 Pleckstrin homology domain-containing family A member 1 PLEKHA1 0.011
5580 Hexon protein PII 0.011
4533 Glyoxalase family protein BC_1747 0.0096
4992 Cytochrome c peroxidase Not Available 0.0096
5006 RNASE4 protein RNASE4 0.0096
3132 Tryptophan synthase alpha chain trpA 0.0096
6568 Tryptophan synthase alpha chain trpA 0.0096
5328 Prostaglandin F synthase Tb11.02.2310 0.0096
5599 3-carboxy-cis,cis-muconate cycloisomerase pcaB 0.0096
3085 Molybdopterin-guanine dinucleotide biosynthesis protein A mobA 0.0096
3729 Citrate synthase gltA 0.0096
4575 Citrate synthase cit 0.0096
4580 Citrate synthase gltA 0.0096
3087 Nicotinate-nucleotide adenylyltransferase nadD 0.0096
4469 Nicotinate-nucleotide adenylyltransferase nadD 0.0096
355 GMP synthase [glutamine-hydrolyzing] GMPS 0.0096
4353 GMP synthase [glutamine-hydrolyzing] guaA 0.0096
2555 Pol polyprotein pol 0.0096
3242 Pol polyprotein gag-pol 0.0096
3471 Pol polyprotein gag-pro-pol 0.0096
5256 Pol polyprotein pol 0.0096
6469 Pol polyprotein gag-pol 0.0096
6565 Pol polyprotein Not Available 0.0096
3583 6-phosphogluconolactonase pgl 0.0089
2149 Angiogenin ANG 0.0089
2521 Cell division protein ftsZ ftsZ 0.0089
3301 Cell division protein ftsZ ftsZ 0.0089
2603 Beta-lactamase II blm 0.0089
4373 Medium-chain-fatty-acid--CoA ligase Not Available 0.0089
2869 1-deoxy-D-xylulose 5-phosphate reductoisomerase dxr 0.0084
3486 Fumarate hydratase class II fumC 0.0084
4366 Riboflavin kinase/FMN adenylyltransferase TM_0857 0.0084
2942 Sialidase nanH 0.0084
3546 Sialidase nedA 0.0084
2286 Isocitrate dehydrogenase [NADP] icd 0.0084
2302 Isocitrate dehydrogenase [NADP] icd 0.0084
2771 Isocitrate dehydrogenase [NADP] icd 0.0084
857 Malate dehydrogenase, mitochondrial MDH2 0.0083
941 Betaine--homocysteine S-methyltransferase 1 BHMT 0.0082
332 Beta-lactamase blaZ 0.0081
2478 Beta-lactamase ampC 0.0081
2613 Beta-lactamase ampC 0.0081
2635 Beta-lactamase ampC 0.0081
2700 Beta-lactamase penP 0.0081
5445 Beta-lactamase blaB 0.0081
6019 Beta-lactamase SHV-7 0.0081
6701 Beta-lactamase cphA 0.0081
1123 Eosinophil cationic protein RNASE3 0.0081
2805 Heparan sulfate glucosamine 3-O-sulfotransferase 3A1 HS3ST3A1 0.008
2452 Tryptophanyl-tRNA synthetase trpS 0.0078
2697 Uridine-cytidine kinase 2 UCK2 0.0077
2936 Oxygen-insensitive NAD(P)H nitroreductase nfnB 0.0077
5184 Oxygen-insensitive NAD(P)H nitroreductase nfnB 0.0077
411 Glycine N-methyltransferase GNMT 0.0073
5579 Carboxypeptidase B CPB1 0.0073
3478 Glucose-1-phosphate thymidylyltransferase rmlA 0.0072
4277 Glucose-1-phosphate thymidylyltransferase rmlA 0.0072
3384 Macrophage migration inhibitory factor MIF 0.0071
128 Adenine phosphoribosyltransferase APRT 0.0067
204 cGMP-specific 3',5'-cyclic phosphodiesterase PDE5A 0.0058
5682 Ribonuclease pancreatic RNASE1 0.0056
822 Aldose reductase AKR1B1 0.0055
933 Proto-oncogene tyrosine-protein kinase Src SRC 0.0052
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0045
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