Golimumab

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Golimumab
Golimumab 5yoy.png
Cartoon representation of the antibody golimumab's variable fragment. The heavy and light chain fragments are coloured blue and yellow, respectively. From PDB entry 5yoy
Monoclonal antibody
Type Whole antibody
Source Human
Target TNFα
Clinical data
Trade names Simponi, Simponi Aria
Other namesCNTO-148 [1]
AHFS/Drugs.com Monograph
MedlinePlus a610010
License data
Pregnancy
category
  • AU:C
Routes of
administration
Subcutaneous injection
ATC code
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
ECHA InfoCard 100.226.360 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C6530H10068N1752O2026S44
Molar mass 146945.25 g·mol−1
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Golimumab, sold under the brand name Simponi, is a human monoclonal antibody which is used as an immunosuppressive medication. [3] [5] Golimumab targets tumor necrosis factor alpha (TNF-alpha), a pro-inflammatory molecule [6] and hence is a TNF inhibitor. Profound reduction in C-reactive protein (CRP) levels, interleukin (IL)-6, intercellaular adhesion molecules (ICAM)-1, matrix metalloproteinase (MMP)-3, and vascular endothelial growth factor (VEGF) demonstrates golimumab as an effective modulator of inflammatory markers and bone metabolism. [7] Golimumab is given via subcutaneous injection. [3] [5] [8]

Contents

It is on the World Health Organization's List of Essential Medicines. [9]

Medical uses

The European Medicines Agency (EMA) has approved the use of golimumab as a treatment for rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis. [5] [10] Golimumab was approved for the treatment by the US Food and Drug Administration (FDA) as well as the European Medicines Agency (EMA) in 2013 for the treatment of ulcerative colitis. [11] [12]

Golimumab is approved in Canada [13] and the United States [14] as a once monthly subcutaneous treatment for adults with moderately to severely active rheumatoid arthritis, psoriatic arthritis, juvenile idiopathic arthritis and ankylosing spondylitis. [15] [16]

Adverse effects

The most common adverse reactions (incidence >5%) are upper respiratory tract infection, nasopharyngitis, and injection site reactions. [17]

Development

Golimumab binds to both soluble and transmembrane forms of TNFα. The antibody was isolated from a hybridoma clone produced by transgenic mice immunized with human TNFα. The golimumab-secreting clone was selected after being assayed for human light and heavy chains and TNFα-binding. The commercial product is produced in a recombinant cell line cultured by continuous perfusion. [18]

Society and culture

Availability

Golimumab was developed by Janssen Biotech, Inc. (formerly Centocor Biotech, Inc.) which also markets the product in the United States. Janssen markets golimumab in Canada, Central and South America, the Middle East, Africa and Asia Pacific. In the European Union, Russia, and Turkey, golimumab distribution rights are held by MSD (Ireland), a subsidiary of Merck & Co., Inc. In Japan, Indonesia, and Taiwan, distribution rights are held by Mitsubishi Tanabe Pharma Corporation. [19]

Research

Rheumatoid arthritis

Large, double-blind randomized controlled trials in patients with rheumatoid arthritis have shown that golimumab in combination with methotrexate was more effective than methotrexate alone. [20] When clinically indicated, golimumab is estimated as a moderate cost-effective treatment option. National Institutes for Health and Care Excellence (NICE) stated that treatment with golimumab is recommended for RA patients who have failed prior TNFi treatment. [21] Unlike other TNFi treatments such as adalimumab and certolizumab pegol, there have been no reported cases of drug-induced lupus-like syndrome (DILS). [22]

Uveitis

There is preliminary evidence for golimumab as a treatment option for ocular inflammation. [23]

Related Research Articles

<span class="mw-page-title-main">Rheumatoid arthritis</span> Type of autoimmune arthritis

Rheumatoid arthritis (RA) is a long-term autoimmune disorder that primarily affects joints. It typically results in warm, swollen, and painful joints. Pain and stiffness often worsen following rest. Most commonly, the wrist and hands are involved, with the same joints typically involved on both sides of the body. The disease may also affect other parts of the body, including skin, eyes, lungs, heart, nerves, and blood. This may result in a low red blood cell count, inflammation around the lungs, and inflammation around the heart. Fever and low energy may also be present. Often, symptoms come on gradually over weeks to months.

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<span class="mw-page-title-main">Ankylosing spondylitis</span> Type of arthritis of the spine

Ankylosing spondylitis (AS) is a type of arthritis characterized by long-term inflammation of the joints of the spine, typically where the spine joins the pelvis. With AS, eye and bowel problems, and back pain may occur. Joint mobility in the affected areas sometimes worsens over time. Ankylosing spondylitis is believed to involve a combination of genetic and environmental factors. More than 90% of people affected in the UK have a specific human leukocyte antigen known as the HLA-B27 antigen. The underlying mechanism is believed to be autoimmune or autoinflammatory. Diagnosis is based on symptoms with support from medical imaging and blood tests. AS is a type of seronegative spondyloarthropathy, meaning that tests show no presence of rheumatoid factor (RF) antibodies.

Spondyloarthropathy or spondyloarthrosis refers to any joint disease of the vertebral column. As such, it is a class or category of diseases rather than a single, specific entity. It differs from spondylopathy, which is a disease of the vertebra itself, but many conditions involve both spondylopathy and spondyloarthropathy.

<span class="mw-page-title-main">Psoriatic arthritis</span> Long-term inflammatory arthritis

Psoriatic arthritis (PsA) is a long-term inflammatory arthritis that occurs in people affected by the autoimmune disease psoriasis. The classic feature of psoriatic arthritis is swelling of entire fingers and toes with a sausage-like appearance. This often happens in association with changes to the nails such as small depressions in the nail (pitting), thickening of the nails, and detachment of the nail from the nailbed. Skin changes consistent with psoriasis frequently occur before the onset of psoriatic arthritis but psoriatic arthritis can precede the rash in 15% of affected individuals. It is classified as a type of seronegative spondyloarthropathy.

Etanercept, sold under the brand name Enbrel among others, is a biologic medical product that is used to treat autoimmune diseases by interfering with tumor necrosis factor (TNF), a soluble inflammatory cytokine, by acting as a TNF inhibitor. It has US Food and Drug Administration (FDA) approval to treat rheumatoid arthritis, juvenile idiopathic arthritis and psoriatic arthritis, plaque psoriasis and ankylosing spondylitis. Tumor necrosis factor alpha (TNFα) is the "master regulator" of the inflammatory (immune) response in many organ systems. Autoimmune diseases are caused by an overactive immune response. Etanercept has the potential to treat these diseases by inhibiting TNF-alpha.

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<span class="mw-page-title-main">Biological therapy for inflammatory bowel disease</span>

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<span class="mw-page-title-main">Axial spondyloarthritis</span> Medical condition

Axial spondyloarthritis is a chronic, immune-mediated disease predominantly affecting the axial skeleton. The term itself is an umbrella term characterizing a diverse disease family united by shared clinical and genetic features, such as the involvement of the axial skeleton. The 2009 introduced term axial spondyloarthritis is a preferred term nowadays and substitutes the old term ankylosing spondylitis.

<span class="mw-page-title-main">Upadacitinib</span> Chemical compound (medication)

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References

  1. Mazumdar S, Greenwald D (2009). "Golimumab". mAbs. 1 (5): 422–31. doi:10.4161/mabs.1.5.9286. PMC   2759491 . PMID   20065639.
  2. "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA . Retrieved 22 October 2023.
  3. 1 2 3 "Simponi- golimumab injection, solution". DailyMed. 30 September 2019. Retrieved 11 November 2020.
  4. "Simponi Aria- golimumab solution". DailyMed. 2 October 2020. Retrieved 11 November 2020.
  5. 1 2 3 4 "Simponi EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 11 November 2020.
  6. Statement On A Nonproprietary Name Adopted By The USAN Council – Golimumab Archived 20 February 2012 at the Wayback Machine , American Medical Association.
  7. Smolen JS, Landewé R, Breedveld FC, Buch M, Burmester G, Dougados M, et al. (March 2014). "EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2013 update". Annals of the Rheumatic Diseases. 73 (3): 492–509. doi:10.1136/annrheumdis-2013-204573. PMC   4079096 . PMID   24161836.
  8. Smolen JS, Landewé R, Breedveld FC, Buch M, Burmester G, Dougados M, et al. (March 2014). "EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2013 update". Annals of the Rheumatic Diseases. 73 (3): 492–509. doi:10.1136/annrheumdis-2013-204573. PMC   4079096 . PMID   24161836.
  9. World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl: 10665/371090 . WHO/MHP/HPS/EML/2023.02.
  10. "Simponi (golimumab) Receives FDA Approval as First Once-Monthly Anti-TNF for Treatment of Rheumatoid Arthritis, Psoriatic Arthritis and Ankylosing Spondylitis". www.drugs.com. Retrieved 9 May 2016.
  11. Löwenberg M, de Boer NK, Hoentjen F (12 March 2014). "Golimumab for the treatment of ulcerative colitis". Clinical and Experimental Gastroenterology. 7: 53–9. doi: 10.2147/CEG.S48741 . PMC   3958527 . PMID   24648749.
  12. "Johnson & Johnson Reports 2008 First-Quarter Results". Archived from the original on 7 October 2008. Retrieved 28 April 2008.
  13. "Health Canada Approves Simponi (Golimumab) For Treatment Of Rheumatoid Arthritis, Psoriatic Arthritis And Ankylosing Spondylitis". Archived from the original on 2 February 2010.
  14. FDA Approves Simponi
  15. "FDA clears potential blockbuster arthritis drug". North County Times . Lee Enterprises. Associated Press. 24 April 2009. Retrieved 23 October 2010.[ permanent dead link ]
  16. Maxwell LJ, Zochling J, Boonen A, Singh JA, Veras MM, Tanjong Ghogomu E, et al. (April 2015). "TNF-alpha inhibitors for ankylosing spondylitis". The Cochrane Database of Systematic Reviews. 4 (4): CD005468. doi:10.1002/14651858.CD005468.pub2. PMID   25887212.
  17. FDA Professional Drug Information
  18. Mazumdar S, Greenwald D (2009). "Golimumab". mAbs. 1 (5): 422–31. doi:10.4161/mabs.1.5.9286. PMC   2759491 . PMID   20065639.
  19. "Simponi Receives European Commission Approval For Treatment Of Non-Radiographic Axial Spondyloarthritis". Johnson & Johnson (Press release). Archived from the original on 19 May 2016. Retrieved 9 May 2016.
  20. Oldfield V, Plosker GL (2009). "Golimumab: in the treatment of rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis". BioDrugs. 23 (2): 125–35. doi:10.2165/00063030-200923020-00005. PMID   19489653. S2CID   195685167.
  21. Tosh J, Archer R, Davis S, Stevenson M, Stevens JW (August 2013). "Golimumab for the treatment of rheumatoid arthritis after the failure of previous disease-modifying antirheumatic drugs: a NICE single technology appraisal". PharmacoEconomics. 31 (8): 653–61. doi:10.1007/s40273-013-0052-7. PMID   23576019. S2CID   23085023.
  22. Williams VL, Cohen PR (May 2011). "TNF alpha antagonist-induced lupus-like syndrome: report and review of the literature with implications for treatment with alternative TNF alpha antagonists". International Journal of Dermatology. 50 (5): 619–25. doi:10.1111/j.1365-4632.2011.04871.x. PMID   21506984. S2CID   21538173.
  23. Rifkin LM, Birnbaum AD, Goldstein DA (August 2013). "TNF inhibition for ophthalmic indications: current status and outlook". BioDrugs. 27 (4): 347–57. doi:10.1007/s40259-013-0022-9. PMID   23568177. S2CID   391892.