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Identification
NameGolimumab
Accession NumberDB06674
TypeBiotech
GroupsApproved
DescriptionGolimumab is a human IgG1қ monoclonal antibody derived from immunizing genetically engineered mice with human TNFα. Golimumab 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.
Protein structureDb06674
Related Articles
Protein chemical formulaC6530H10068N1752O2026S44
Protein average weight146943.1937 Da
SequencesNot Available
SynonymsNot Available
External Identifiers
  • CNTO 148
  • CNTO-148
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SimponiSolution for injection in pre- filled syringe100 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponiinjection, solution50 mg/.5mLsubcutaneousJanssen Biotech, Inc.2009-04-25Not applicableUs
SimponiSolution for injection in pre- filled syringe50 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponisolution50 mgsubcutaneousJanssen Inc2009-06-22Not applicableCanada
SimponiSolution for injection in pre- filled pen50 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponiinjection, solution100 mg/mLsubcutaneousJanssen Biotech, Inc.2013-05-15Not applicableUs
SimponiSolution for injection in pre- filled pen100 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponisolution50 mgsubcutaneousJanssen Inc2009-06-22Not applicableCanada
SimponiSolution for injection in pre- filled pen50 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponisolution100 mgsubcutaneousJanssen Inc2013-10-03Not applicableCanada
SimponiSolution for injection in pre- filled pen100 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponisolution100 mgsubcutaneousJanssen Inc2013-10-03Not applicableCanada
SimponiSolution for injection in pre- filled syringe50 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
SimponiSolution for injection in pre- filled syringe100 mgSubcutaneous useJanssen Biologics B.V.2009-10-01Not applicableEu
Simponi Ariasolution50 mg/4mLintravenousJanssen Biotech, Inc.2013-07-19Not applicableUs
Simponi I.V.solution50 mgintravenousJanssen Inc2013-12-12Not applicableCanada
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
UNII91X1KLU43E
CAS number476181-74-5
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
IndicationUsed 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 TNFα is 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.
Related Articles
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 distribution

After 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.

Protein bindingPlasma protein binding was not quantified.
Metabolism

The metabolism of golimumab has yet to be determined.

Route of eliminationThe route of elimination for golimumab has yet to be determined.
Half lifeGolimumab has a long half-life of about 2 weeks.
Clearance

After one IV dose of golimumab, the systemic clearance was about 4.9 to 6.7 mL/day/kg.

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.
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, solutionsubcutaneous100 mg/mL
Injection, solutionsubcutaneous50 mg/.5mL
Solutionsubcutaneous100 mg
Solutionsubcutaneous50 mg
Solution for injection in pre- filled penSubcutaneous use100 mg
Solution for injection in pre- filled penSubcutaneous use50 mg
Solution for injection in pre- filled syringeSubcutaneous use100 mg
Solution for injection in pre- filled syringeSubcutaneous use50 mg
Solutionintravenous50 mg/4mL
Solutionintravenous50 mg
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental PropertiesNot Available
References
Synthesis Reference

Zhou H, Jang H, Fleischmann RM, Bouman-Thio E, Xu Z, Marini JC, Pendley C, Jiao Q, Shankar G, Marciniak SJ, Cohen SB, Rahman MU, Baker D, Mascelli MA, Davis HM, Everitt DE: Pharmacokinetics and safety of golimumab, a fully human anti-TNF-alpha monoclonal antibody, in subjects with rheumatoid arthritis. J Clin Pharmacol. 2007 Mar;47(3):383-96.

General References
  1. Oldfield V, Plosker GL: Golimumab: in the treatment of rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis. BioDrugs. 2009;23(2):125-35. doi: 10.2165/00063030-200923020-00005. [PubMed:19489653 ]
  2. Sandborn WJ, Feagan BG, Marano C, Zhang H, Strauss R, Johanns J, Adedokun OJ, Guzzo C, Colombel JF, Reinisch W, Gibson PR, Collins J, Jarnerot G, Rutgeerts P: Subcutaneous golimumab maintains clinical response in patients with moderate-to-severe ulcerative colitis. Gastroenterology. 2014 Jan;146(1):96-109.e1. doi: 10.1053/j.gastro.2013.06.010. Epub 2013 Jun 14. [PubMed:23770005 ]
External Links
ATC CodesL04AB06
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (1.9 MB)
MSDSDownload (567 KB)
Interactions
Drug Interactions
Drug
AbataceptThe risk or severity of adverse effects can be increased when Golimumab is combined with Abatacept.
AnakinraThe risk or severity of adverse effects can be increased when Golimumab is combined with Anakinra.
CanakinumabThe risk or severity of adverse effects can be increased when Golimumab is combined with Canakinumab.
Certolizumab pegolGolimumab may increase the immunosuppressive activities of Certolizumab pegol.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Golimumab.
FingolimodGolimumab may increase the immunosuppressive activities of Fingolimod.
InfliximabGolimumab may increase the immunosuppressive activities of Infliximab.
LeflunomideThe risk or severity of adverse effects can be increased when Golimumab is combined with Leflunomide.
NatalizumabThe risk or severity of adverse effects can be increased when Golimumab is combined with Natalizumab.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Golimumab.
Rabies vaccineThe risk or severity of adverse effects can be increased when Golimumab is combined with Rabies vaccine.
RilonaceptThe risk or severity of adverse effects can be increased when Golimumab is combined with Rilonacept.
RoflumilastRoflumilast may increase the immunosuppressive activities of Golimumab.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Golimumab.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Golimumab.
TocilizumabTocilizumab may increase the immunosuppressive activities of Golimumab.
TofacitinibThe risk or severity of adverse effects can be increased when Golimumab is combined with Tofacitinib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Golimumab.
VedolizumabThe risk or severity of adverse effects can be increased when Golimumab is combined with Vedolizumab.
Food Interactions
  • Since golimumab is administered by subcutaneous injection, there are no food effects.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antibody
General Function:
Tumor necrosis factor receptor binding
Specific Function:
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs ...
Gene Name:
TNF
Uniprot ID:
P01375
Molecular Weight:
25644.15 Da
References
  1. Mittal M, Raychaudhuri SP: Golimumab and certolizumab: the two new anti-tumor necrosis factor kids on the block. Indian J Dermatol Venereol Leprol. 2010 Nov-Dec;76(6):602-8; quiz 609. doi: 10.4103/0378-6323.72445. [PubMed:21079302 ]
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Drug created on March 19, 2008 10:47 / Updated on August 25, 2016 16:24