Golimumab

Golimumab
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
TypeWhole antibody
SourceHuman
TargetTNFα
Clinical data
Trade namesSimponi, Simponi Aria
Other namesCNTO-148[1]
AHFS/Drugs.comMonograph
MedlinePlusa610010
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 InfoCard100.226.360 Edit this at Wikidata
Chemical and physical data
FormulaC6530H10068N1752O2026S44
Molar mass146945.25 g·mol−1
 ☒NcheckY (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]

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]

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. ^ a b c "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. ^ a b c d "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.