==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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Primary information
ThPP IDTh1125
Therapeutic Peptide/Protein NameGolimumab
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight146943.1937
Chemical FormulaC6530H10068N1752O2026S44
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half LifeAbout 2 weeks
DescriptionHuman IgG1қ monoclonal antibody derived from immunizing genetically engineered mice with human TNFα. It binds and inhibits soluble and transmembrane human TNFα. Increased TNFα is associated with chronic inflammation. Thus golimumab is indicated for use in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications. In the U.S. and Canada, golimumab is marketed under the brand name Simponi. The FDA label includes a black box warning of serious infections and malignancy. Additionally in children and adolescents taking golimumab, there have been lymphoma and other malignancies observed.
Indication/DiseaseUsed in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA), (ii) alone or as an adjunct to methotrexate treatment in patients with active psoriatic arthritis (PsA), (iii) as a single agent in patients with active ankylosing spondylitis (AS), and (iv) as a single agent in patients with moderate to severe ulcerative colitis (UC) who require chronic steroids or have experienced intolerance or only a partial response to previous medications.
PharmacodynamicsGolimumab inhibits the activity of the cytokine, tumor necrosis factor alpha (TNFα). In areas such as the joints and blood, increased TNFαis associated with chronic inflammation seen in patients with rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis. Thus golimumab decreases the inflammation in these conditions. Concerning ulcerative colitis, the physiological effects of golimumab has yet to be determined.
Mechanism of ActionAs a human monoclonal antibody, golimumab binds and inhibits soluble and transmembrane human TNFα. Inhibition of TNFα prevents it binding to its receptors, which prevents both leukocyte infiltration through prevention of cell adhesion proteins such as E-selectin, ICAM-1 and VCAM-1, and pro-inflammatory cytokine secretion such as IL-6, IL-8, G-CSF and GM-CSF in vitro. Consequently, in patients with chronic inflammatory conditions, decreases in ICAM-1 and IL-6 as well as C-reactive protein (CRP), matrix metalloproteinase 3 (MMP-3), and vascular endothelial growth factor (VEGF) were observed.
ToxicityThe FDA label includes a black box warning of serious infections and malignancy. Specifically there have been hospitalizations or death from infections such as bacterial sepsis, tuberculosis (TB), and invasive fungal (histoplasmosis) and other opportunistic infections. Additionally in children and adolescents taking golimumab, there have been lymphoma and other malignancies observed.
MetabolismThe metabolism of golimumab has yet to be determined.
AbsorptionAfter subcutaneous administration, golimumab can achieve maximum serum concentrations in 2 to 6 days and has an approximate bioavailability of 53%. In healthy volunteers, the maximum average concentration reached was 3.2 ± 1.4 μg/mL.
Volume of DistributionAfter IV administration, golimumab has a volume of distribution of about 58 to 126 mL/kg. This means that golimumab stays mostly in the circulatory system.
ClearanceAfter one IV dose of golimumab, the systemic clearance was about 4.9 to 6.7 mL/day/kg.
CategoriesAntipsoriatic Agents and Monoclonal antibodies and TNF inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameSimponi Aria
CompanyN.A.
Brand DiscriptionSIMPONI ARIA (golimumab) is a human IgG1k monoclonal antibody specific for human tumor necrosis factor alpha (TNFα) that exhibits multiple glycoforms with molecular masses of approximately 150 to 151 kilodaltons. SIMPONI ARIA was created using genetically engineered mice immunized with human TNF, resulting in an antibody with human-derived antibody variable and constant regions. SIMPONI ARIA is produced by a recombinant cell line cultured by continuous perfusion and is purified by a series of steps that includes measures to inactivate and remove viruses.
Prescribed forrheumatoid arthritis.
Chemical NameN.A.
FormulationSIMPONI ARIA does not contain preservatives, natural rubber or latex. The solution is colorless to light yellow with a pH of approximately 5.5. Each 4 mL vial of SIMPONI ARIA contains 50 mg golimumab, 9.5 mM histidine, 4.5% (w/v) sorbitol, and 0.015% (w/v) polysorbate 80.
Physcial AppearnceThe SIMPONI ARIA drug product is a sterile concentrated solution of the golimumab antibody supplied in a 4 mL glass vial for Intravenous infusion.
Route of AdministrationIntravenous infusion
Recommended Dosage2 mg per kg
ContraindicationN.A.
Side Effectssepsis, pneumonia, cellulitis, abscess, opportunistic infections, tuberculosis (TB), and invasive fungal infections, Malignancies, Liver Enzyme Elevations, Autoimmune Disorders And Autoantibodies
Useful Linkhttp://www.rxlist.com/simponi-aria-drug.htm https://www.simponiaria.com/ http://www.fda.gov/downloads/Drugs/DrugSafety/UCM362202.pdf
PubMed ID25629655, 25627338, 25623393, 25602858, 25547737, 23770005, 19489653
3-D StructureN.A.