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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
- 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
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Active polyarticular juvenile idiopathic arthritis (pjia) •••••••••••• •••••••• ••••••••• Management of Severe ulcerative colitis •••••••••••• ••••• Management of Active ankylosing spondylitis •••••••••••• ••••• ••••••••• Used in combination to manage Active psoriatic arthritis Regimen in combination with: Methotrexate (DB00563) •••••••••••• ••••• ••••••••• Management of Active psoriatic arthritis •••••••••••• •••••• •••••••• ••••••••• - Contraindications & Blackbox Warnings
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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.
Target Actions Organism ATumor necrosis factor antibodyHumans - 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
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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of infection can be increased when Golimumab is combined with Abatacept. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Golimumab. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Golimumab. Abrocitinib The metabolism of Abrocitinib can be increased when combined with Golimumab. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Golimumab. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Simponi Injection, solution 50 mg Subcutaneous Janssen Biologics B.V. 2016-09-08 Not applicable EU 
Simponi Injection, solution 100 mg/1mL Subcutaneous Janssen Biotech, Inc. 2013-05-15 Not applicable US 
Simponi Solution 50 mg / 0.5 mL Subcutaneous Janssen Pharmaceuticals 2009-06-22 Not applicable Canada 
Simponi Injection, solution 45 mg/0.45ml Subcutaneous Janssen Biologics B.V. 2020-12-21 Not applicable EU Simponi Injection, solution 100 mg Subcutaneous Janssen Biologics B.V. 2016-09-08 Not applicable EU
Categories
- ATC Codes
- L04AB06 — Golimumab
- Drug Categories
- Agents reducing cytokine levels
- Amino Acids, Peptides, and Proteins
- Anti-Inflammatory Agents
- Antibodies
- Antibodies, Monoclonal
- Antineoplastic and Immunomodulating Agents
- Antirheumatic Agents
- Biologics for Rheumatoid Arthritis Treatment
- Blood Proteins
- Disease-modifying Antirheumatic Agents
- Globulins
- Immunoglobulins
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Proteins
- Serum Globulins
- Tumor necrosis factor alpha (TNF-alpha) inhibitors
- Tumor Necrosis Factor Blockers
- Tumor Necrosis Factor Receptor Blocking Activity
- 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
- 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]
- 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]
- FDA Approved Products: SIMPONI ARIA (golimumab) injection, for intravenous use [Link]
- FDA Approved Products: SIMPONI (golimumab) injection, for intravenous use [Link]
- External Links
- KEGG Drug
- D04358
- PubChem Substance
- 347910358
- 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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Treatment Brain Disorders / Decline, Cognitive / Depression / Fatigue / Hand Rheumatism / Pain / Rheumatoid Arthritis 1 somestatus stop reason just information to hide Not Available Completed Not Available Ankylosing Spondylitis (AS) / Coxitis 1 somestatus stop reason just information to hide Not Available Completed Not Available Ankylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis 2 somestatus stop reason just information to hide Not Available Completed Not Available Axial Spondyloarthritis (AxSpA) 1 somestatus stop reason just information to hide Not Available Completed Not Available Enthesitis / Psoriasis / Psoriatic Arthritis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Subcutaneous 50 mg/0.5ml Injection, solution Parenteral; Subcutaneous 100 MG Injection, solution Parenteral; Subcutaneous 45 MG/0.45ML Injection, solution Parenteral; Subcutaneous 50 MG Injection, solution Subcutaneous 100 mg/1mL Injection, solution Subcutaneous 100 mg Injection, solution Subcutaneous 50 mg/0.5mL Solution Subcutaneous 100 mg / 1.0 mL Solution Subcutaneous 50 mg / 0.5 mL Solution Subcutaneous 50.000 mg Injection, solution Parenteral 100 MG Injection, solution Parenteral 50 MG Injection, solution 50 mg Injection 50 mg/5ml Injection 50 mg Solution Intravenous 50 mg/4mL Solution Intravenous 50 mg / 4.0 mL Injection, solution Intravenous 12.5 mg/1ml Injection, solution Subcutaneous 50 mg Solution 50 mg/0.5ml Injection, solution Subcutaneous 45 mg/0.45ml Solution Intravenous 12.5 mg/1ml Injection, solution Subcutaneous 100 mg/1.0ml Solution Intravenous 50 mg Solution Subcutaneous 50 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General 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 regulatory T-cells (Treg) function in individuals with rheumatoid arthritis via FOXP3 dephosphorylation. Up-regulates the expression of protein phosphatase 1 (PP1), which dephosphorylates the key 'Ser-418' residue of FOXP3, thereby inactivating FOXP3 and rendering Treg cells functionally defective (PubMed:23396208). Key mediator of cell death in the anticancer action of BCG-stimulated neutrophils in combination with DIABLO/SMAC mimetic in the RT4v6 bladder cancer cell line (PubMed:16829952, PubMed:22517918, PubMed:23396208). Induces insulin resistance in adipocytes via inhibition of insulin-induced IRS1 tyrosine phosphorylation and insulin-induced glucose uptake. Induces GKAP42 protein degradation in adipocytes which is partially responsible for TNF-induced insulin resistance (By similarity). Plays a role in angiogenesis by inducing VEGF production synergistically with IL1B and IL6 (PubMed:12794819). Promotes osteoclastogenesis and therefore mediates bone resorption (By similarity)
- Specific Function
- cytokine activity
- Gene Name
- TNF
- Uniprot ID
- P01375
- Uniprot Name
- Tumor necrosis factor
- Molecular Weight
- 25644.15 Da
References
- 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 at March 19, 2008 16:47 / Updated at June 03, 2022 07:24