Golimumab

Identification

Summary

Golimumab is a TNFα inhibitor used in the symptomatic treatment of various active inflammatory disorders, such as rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and ulcerative colitis.

Brand Names
Simponi
Generic Name
Golimumab
DrugBank Accession Number
DB06674
Background

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.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Protein Structure
Db06674
Protein Chemical Formula
C6530H10068N1752O2026S44
Protein Average Weight
146943.1937 Da
Sequences
Not Available
Synonyms
  • Golimumab
External IDs
  • CNTO 148
  • CNTO-148

Pharmacology

Indication

Used in adults (i) as an adjunct to methotrexate treatment in patients with moderate to severe active rheumatoid arthritis (RA)3, (ii) in patients 2 years old and above with active psoriatic arthritis (PsA)3, (iii) as a single agent in patients with active ankylosing spondylitis (AS) or in combination with methotrexate4, 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.4 It is also indicated (v) for the treatment of active polyarticular juvenile idiopathic arthritis (pJIA) in patients 2 years of age and older.3

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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
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.

Adverse Effects
Adverseeffects
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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.

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
AbataceptThe risk or severity of infection can be increased when Golimumab is combined with Abatacept.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Golimumab.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Golimumab.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Golimumab.
AcebutololThe metabolism of Acebutolol can be increased when combined with Golimumab.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Golimumab.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Golimumab.
AcetohexamideThe metabolism of Acetohexamide can be increased when combined with Golimumab.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be increased when combined with Golimumab.
AcyclovirThe metabolism of Acyclovir can be increased when combined with Golimumab.
Interactions
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
SimponiSolution50 mg / 0.5 mLSubcutaneousJanssen Pharmaceuticals2009-06-22Not applicableCanada flag
SimponiInjection, solution50 mgSubcutaneousJanssen Biologics B.V.2016-09-08Not applicableEU flag
SimponiInjection, solution100 mg/1mLSubcutaneousJanssen Biotech, Inc.2013-05-15Not applicableUS flag
SimponiSolution100 mg / 1.0 mLSubcutaneousJanssen Pharmaceuticals2013-10-03Not applicableCanada flag
SimponiInjection, solution100 mgSubcutaneousJanssen Biologics B.V.2016-09-08Not applicableEU flag
SimponiInjection, solution50 mgSubcutaneousJanssen Biologics B.V.2016-09-08Not applicableEU flag
SimponiSolution100 mg / 1.0 mLSubcutaneousJanssen Pharmaceuticals2013-10-03Not applicableCanada flag
SimponiInjection, solution50 mgSubcutaneousJanssen Biologics B.V.2016-09-08Not applicableEU flag
SimponiSolution50 mg / 0.5 mLSubcutaneousJanssen Pharmaceuticals2009-06-22Not applicableCanada flag
SimponiInjection, solution45 mg/0.45mlSubcutaneousJanssen Biologics B.V.2020-12-21Not applicableEU flag

Categories

ATC Codes
L04AB06 — Golimumab
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
91X1KLU43E
CAS number
476181-74-5

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. [Article]
  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. [Article]
  3. FDA Approved Products: SIMPONI ARIA (golimumab) injection, for intravenous use [Link]
  4. FDA Approved Products: SIMPONI (golimumab) injection, for intravenous use [Link]
KEGG Drug
D04358
PubChem Substance
347910358
RxNav
819300
ChEMBL
CHEMBL1201833
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Golimumab
FDA label
Download (1.9 MB)
MSDS
Download (567 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAnkylosing Spondylitis (AS) / Psoriatic Arthritis1
4Active Not RecruitingTreatmentUlcerative Colitis1
4CompletedDiagnosticUlcerative Colitis1
4CompletedOtherHepato-splenic T-cell Lymphoma1
4CompletedTreatmentAnkylosing Spondylitis (AS)3
4CompletedTreatmentRheumatoid Arthritis1
4CompletedTreatmentSpondylarthropathy1
4CompletedTreatmentSpondyloarthritis (SpA)1
4CompletedTreatmentSpondyloarthropathies1
4CompletedTreatmentUlcerative Colitis3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionSubcutaneous
Injection, solutionParenteral; Subcutaneous100 MG
Injection, solutionParenteral; Subcutaneous45 MG/0.45ML
Injection, solutionParenteral; Subcutaneous50 MG
Injection, solutionSubcutaneous100 mg
Injection, solutionSubcutaneous100 mg/1mL
Injection, solutionSubcutaneous45 mg/0.45ml
Injection, solutionSubcutaneous50 mg/0.5mL
Injection, solutionSubcutaneous50 mg
SolutionSubcutaneous100 mg / 1.0 mL
SolutionSubcutaneous50 mg / 0.5 mL
Injection, solutionParenteral100 MG
Injection, solutionParenteral50 MG
Injection, solution
Injection
SolutionIntravenous50 mg/4mL
SolutionIntravenous50 mg / 4.0 mL
Injection, solutionIntravenous
Injection, solutionSubcutaneous
Solution50 mg/0.5ml
SolutionIntravenous50 mg
SolutionSubcutaneous50 mg
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets2
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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. [Article]

Drug created on March 19, 2008 16:47 / Updated on September 16, 2021 13:04