Golimumab

Identification

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Name
Golimumab
Accession Number
DB06674
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

Golimumab 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 structure
Db06674
Protein chemical formula
C6530H10068N1752O2026S44
Protein average weight
146943.1937 Da
Sequences
Not Available
Synonyms
Not Available
External IDs
CNTO 148 / CNTO-148
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SimponiSolution50 mgSubcutaneousJanssen Pharmaceuticals2009-06-22Not applicableCanada
SimponiInjection, solution100 mg/1mLSubcutaneousJanssen Biotech, Inc.2013-05-15Not applicableUs
SimponiInjection, solution50 mgSubcutaneousJanssen Biologics B.V.2009-10-01Not applicableEu
SimponiInjection, solution100 mgSubcutaneousJanssen Biologics B.V.2009-10-01Not applicableEu
SimponiSolution50 mgSubcutaneousJanssen Pharmaceuticals2009-06-22Not applicableCanada
SimponiInjection, solution50 mg/0.5mLSubcutaneousJanssen Biotech, Inc.2009-04-25Not applicableUs
SimponiInjection, solution50 mgSubcutaneousJanssen Biologics B.V.2009-10-01Not applicableEu
SimponiInjection, solution100 mgSubcutaneousJanssen Biologics B.V.2009-10-01Not applicableEu
SimponiInjection, solution100 mgSubcutaneousJanssen Biologics B.V.2009-10-01Not applicableEu
SimponiSolution100 mgSubcutaneousJanssen Pharmaceuticals2013-10-03Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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Categories
UNII
91X1KLU43E
CAS number
476181-74-5

Pharmacology

Indication

Used 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.

Associated Conditions
Pharmacodynamics

Golimumab 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 action

As 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.

TargetActionsOrganism
ATumor necrosis factor
antibody
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

After 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 binding

Plasma protein binding was not quantified.

Metabolism

The metabolism of golimumab has yet to be determined.

Route of elimination

The route of elimination for golimumab has yet to be determined.

Half life

Golimumab 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.

Toxicity

The 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be increased when combined with Golimumab.
(S)-WarfarinThe metabolism of (S)-Warfarin can be increased when combined with Golimumab.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Golimumab.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be increased when combined with Golimumab.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be increased when combined with Golimumab.
5-methoxy-N,N-dimethyltryptamineThe metabolism of 5-methoxy-N,N-dimethyltryptamine can be increased when combined with Golimumab.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be increased when combined with Golimumab.
8-azaguanineThe metabolism of 8-azaguanine can be increased when combined with Golimumab.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be increased when combined with Golimumab.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Golimumab is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity
    Severity

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  • Evidence Level
    Evidence Level

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  • Action
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Food Interactions
  • Since golimumab is administered by subcutaneous injection, there are no food effects.

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
KEGG Drug
D04358
PubChem Substance
347910358
ChEMBL
CHEMBL1201833
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Golimumab
ATC Codes
L04AB06 — Golimumab
AHFS Codes
  • 92:36.00 — Disease-modifying Antirheumatic Agents
FDA label
Download (1.9 MB)
MSDS
Download (567 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingBasic ScienceType 1 Insulin-Dependent Diabetes Mellitus1
1Active Not RecruitingTreatmentUlcerative Colitis1
1CompletedTreatmentHealthy Adult Chinese Males1
1CompletedTreatmentRheumatoid Arthritis1
1RecruitingTreatmentPre-Symptomatic Type 1 Diabetes1
1RecruitingTreatmentPsoriatic Arthritis1
1, 2TerminatedTreatmentAutoimmune Inner Ear Disease1
2Active Not RecruitingTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentAsthma1
2CompletedTreatmentRheumatoid Arthritis2
2CompletedTreatmentSarcoidosis1
2CompletedTreatmentUlcerative Colitis1
2RecruitingTreatmentAnkylosing Spondylitis (AS)1
2RecruitingTreatmentUlcerative Colitis2
2TerminatedTreatmentRheumatoid Arthritis1
2WithdrawnTreatmentAsthma1
2, 3CompletedTreatmentUlcerative Colitis1
2, 3TerminatedTreatmentUlcerative Colitis1
3Active Not RecruitingTreatmentJuvenile Idiopathic Arthritis (JIA)1
3CompletedTreatmentAnkylosing Spondylitis (AS)4
3CompletedTreatmentArthritis / Autoimmune Diseases / Rheumatoid Arthritis1
3CompletedTreatmentPeripheral Spondylarthritis1
3CompletedTreatmentPsoriatic Arthritis3
3CompletedTreatmentRheumatoid Arthritis9
3CompletedTreatmentUlcerative Colitis2
3Not Yet RecruitingTreatmentSpondyloarthritis, Axial1
3RecruitingTreatmentPsoriatic Arthritis2
3RecruitingTreatmentUlcerative Colitis1
3TerminatedTreatmentJuvenile Idiopathic Arthritis (JIA)1
3TerminatedTreatmentRheumatoid Arthritis1
3TerminatedTreatmentSpondyloarthritis, Axial2
4Active Not RecruitingTreatmentAnkylosing Spondylitis (AS)1
4Active Not RecruitingTreatmentSpondyloarthritis1
4CompletedDiagnosticUlcerative Colitis1
4CompletedTreatmentAnkylosing Spondylitis (AS)2
4CompletedTreatmentRheumatoid Arthritis1
4CompletedTreatmentSpondylarthropathy1
4CompletedTreatmentSpondyloarthropathies1
4CompletedTreatmentUlcerative Colitis2
4Not Yet RecruitingTreatmentUlcerative Colitis2
4RecruitingOtherHepatosplenic T-Cell Lymphoma1
4RecruitingTreatmentAnkylosing Spondylitis (AS) / Psoriatic Arthritis1
4RecruitingTreatmentColitis1
4RecruitingTreatmentCrohn's Disease (CD) / Inflammatory Bowel Diseases (IBD) / Ulcerative Colitis1
4RecruitingTreatmentRheumatoid Arthritis3
4RecruitingTreatmentUlcerative Colitis3
4TerminatedNot AvailableRheumatoid Arthritis1
4Unknown StatusDiagnosticUlcerative Colitis1
4WithdrawnNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis1
Not AvailableActive Not RecruitingNot AvailableAnkylosing Spondylitis (AS) / Coxitis1
Not AvailableActive Not RecruitingNot AvailableRheumatoid Arthritis1
Not AvailableAvailableNot AvailableType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableCompletedNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis2
Not AvailableCompletedNot AvailableInflammatory Bowel Diseases (IBD)1
Not AvailableCompletedNot AvailablePsoriatic Arthritis / Rheumatoid Arthritis / Spondyloarthritis1
Not AvailableCompletedNot AvailableRheumatoid Arthritis1
Not AvailableCompletedNot AvailableSpondyloarthritis, Axial1
Not AvailableCompletedNot AvailableSpondyloarthritis / Ultrasonography1
Not AvailableCompletedTreatmentSpondyloarthritis1
Not AvailableNot Yet RecruitingNot AvailableInfection NOS / Rheumatoid Arthritis1
Not AvailableRecruitingNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis1
Not AvailableRecruitingNot AvailableEnthesitis / Psoriasis / Psoriatic Arthritis1
Not AvailableRecruitingNot AvailableFlare Up, Symptom / Ulcerative Colitis1
Not AvailableRecruitingNot AvailableRheumatoid Arthritis2
Not AvailableRecruitingNot AvailableUlcerative Colitis1
Not AvailableTerminatedNot AvailableRheumatoid Arthritis1
Not AvailableTerminatedOtherPsoriatic Arthritis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous100 mg/1mL
Injection, solutionSubcutaneous100 mg
Injection, solutionSubcutaneous50 mg/0.5mL
Injection, solutionSubcutaneous50 mg
SolutionSubcutaneous100 mg
SolutionSubcutaneous50 mg
SolutionIntravenous50 mg/4mL
SolutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
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 ac...
Gene Name
TNF
Uniprot ID
P01375
Uniprot Name
Tumor necrosis factor
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]

Drug created on March 19, 2008 10:47 / Updated on November 12, 2019 22:47