golimumab

{{Infobox drug

| Verifiedfields = changed

| Watchedfields = changed

| verifiedrevid = 458275071

| image = Golimumab 5yoy.png

| caption = Cartoon representation of the antibody golimumab's variable fragment. The heavy and light chain fragments are coloured blue and yellow, respectively. From PDB entry {{PDBe|5yoy}}

| type = mab

| mab_type = mab

| source = u

| target = TNFα

| tradename = Simponi, Simponi Aria

| Drugs.com = {{drugs.com|monograph|golimumab}}

| MedlinePlus = a610010

| DailyMedID = Golimumab

| pregnancy_AU = C

| pregnancy_category =

| routes_of_administration = Subcutaneous injection

| ATC_prefix = L04

| ATC_suffix = AB06

| legal_AU = S4

| legal_CA =

| legal_UK = POM

| legal_US = Rx-only

| legal_US_comment = {{cite web | title=Simponi- golimumab injection, solution | website=DailyMed | date=30 September 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f86cb4a7-c358-4136-ae57-b32bda9bba00 | access-date=11 November 2020}}{{cite web | title=Simponi Aria- golimumab solution | website=DailyMed | date=2 October 2020 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9e260a47-55af-4c92-8d88-a86ccc767fff | access-date=11 November 2020}}

| legal_EU = Rx-only

| legal_EU_comment = {{cite web | title=Simponi EPAR | website=European Medicines Agency (EMA) | date=17 September 2018 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/simponi | access-date=11 November 2020}}

| legal_status =

| bioavailability =

| protein_bound =

| metabolism =

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| CAS_number_Ref = {{cascite|changed|??}}

| CAS_number = 476181-74-5

| PubChem =

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| DrugBank_Ref = {{drugbankcite|correct|drugbank}}

| DrugBank = DB06674

| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}

| ChemSpiderID = none

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 91X1KLU43E

| KEGG_Ref = {{keggcite|correct|kegg}}

| KEGG = D04358

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| ChEBI =

| ChEMBL_Ref = {{ebicite|changed|EBI}}

| ChEMBL = 1201833

| NIAID_ChemDB =

| PDB_ligand =

| synonyms = CNTO-148{{cite journal | vauthors = Mazumdar S, Greenwald D | title = Golimumab | journal = mAbs | volume = 1 | issue = 5 | pages = 422–31 | year = 2009 | pmid = 20065639 | pmc = 2759491 | doi = 10.4161/mabs.1.5.9286 | url = http://www.landesbioscience.com/journals/mabs/article/9286/ }}

| C = 6530 | H = 10068 | N = 1752 | O = 2026 | S = 44

}}

Golimumab, sold under the brand name Simponi, is a human monoclonal antibody which is used as an immunosuppressive medication. Golimumab targets tumor necrosis factor alpha (TNF-alpha), a pro-inflammatory molecule[http://www.ama-assn.org/ama1/pub/upload/mm/365/golimumab.doc Statement On A Nonproprietary Name Adopted By The USAN Council – Golimumab] {{Webarchive|url=https://web.archive.org/web/20120220192926/http://www.ama-assn.org/ama1/pub/upload/mm/365/golimumab.doc |date=20 February 2012 }}, American Medical Association. and hence is a TNF inhibitor. Profound reduction in C-reactive protein (CRP) levels, interleukin (IL)-6, intercellular 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.{{cite journal | vauthors = Smolen JS, Landewé R, Breedveld FC, Buch M, Burmester G, Dougados M, Emery P, Gaujoux-Viala C, Gossec L, Nam J, Ramiro S, Winthrop K, de Wit M, Aletaha D, Betteridge N, Bijlsma JW, Boers M, Buttgereit F, Combe B, Cutolo M, Damjanov N, Hazes JM, Kouloumas M, Kvien TK, Mariette X, Pavelka K, van Riel PL, Rubbert-Roth A, Scholte-Voshaar M, Scott DL, Sokka-Isler T, Wong JB, van der Heijde D | title = EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2013 update | journal = Annals of the Rheumatic Diseases | volume = 73 | issue = 3 | pages = 492–509 | date = March 2014 | pmc = 4079096 | doi = 10.1136/annrheumdis-2013-204573 | pmid = 24161836 }} Golimumab is given via subcutaneous injection.{{cite journal | vauthors = Smolen JS, Landewé R, Breedveld FC, Buch M, Burmester G, Dougados M, Emery P, Gaujoux-Viala C, Gossec L, Nam J, Ramiro S, Winthrop K, de Wit M, Aletaha D, Betteridge N, Bijlsma JW, Boers M, Buttgereit F, Combe B, Cutolo M, Damjanov N, Hazes JM, Kouloumas M, Kvien TK, Mariette X, Pavelka K, van Riel PL, Rubbert-Roth A, Scholte-Voshaar M, Scott DL, Sokka-Isler T, Wong JB, van der Heijde D | title = EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2013 update | journal = Annals of the Rheumatic Diseases | volume = 73 | issue = 3 | pages = 492–509 | date = March 2014 | pmc = 4079096 | doi = 10.1136/annrheumdis-2013-204573 | pmid = 24161836 }}

It is on the World Health Organization's List of Essential Medicines.{{cite book | vauthors = ((World Health Organization)) | title = The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023) | year = 2023 | hdl = 10665/371090 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MHP/HPS/EML/2023.02 | hdl-access=free }}

Medical uses

The European Medicines Agency (EMA) has approved the use of golimumab as a treatment for rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis.{{cite web|url=https://www.drugs.com/newdrugs/simponi-golimumab-receives-fda-approval-first-once-monthly-anti-tnf-rheumatoid-arthritis-psoriatic-1329.html|title=Simponi (golimumab) Receives FDA Approval as First Once-Monthly Anti-TNF for Treatment of Rheumatoid Arthritis, Psoriatic Arthritis and Ankylosing Spondylitis|website=www.drugs.com|access-date=9 May 2016}} 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.{{cite journal | vauthors = Löwenberg M, de Boer NK, Hoentjen F | title = Golimumab for the treatment of ulcerative colitis | journal = Clinical and Experimental Gastroenterology | volume = 7 | pages = 53–9 | date = 12 March 2014 | pmid = 24648749 | pmc = 3958527 | doi = 10.2147/CEG.S48741 | doi-access = free }}{{cite web |url=http://sev.prnewswire.com/retail/20080415/NYTU07615042008-1.html |title=Johnson & Johnson Reports 2008 First-Quarter Results |access-date=28 April 2008 |archive-url=https://web.archive.org/web/20081007101023/http://sev.prnewswire.com/retail/20080415/NYTU07615042008-1.html |archive-date=7 October 2008 |url-status=dead }}

Golimumab is approved in Canada{{cite web|url=http://www.centocororthobiotech.com/cobi/viewDocumentByTitleAlias.html?title=PR_SIMPONI_CANADIAN_APPROVAL|title=Health Canada Approves Simponi (Golimumab) For Treatment Of Rheumatoid Arthritis, Psoriatic Arthritis And Ankylosing Spondylitis|archive-url=https://web.archive.org/web/20100202180811/http://www.centocororthobiotech.com/cobi/viewDocumentByTitleAlias.html?title=PR_SIMPONI_CANADIAN_APPROVAL|archive-date=2 February 2010|url-status=dead}} and the United States[https://www.drugs.com/newdrugs/simponi-golimumab-receives-fda-approval-first-once-monthly-anti-tnf-rheumatoid-arthritis-psoriatic-1329.html FDA Approves Simponi] as a once monthly subcutaneous treatment for adults with moderately to severely active rheumatoid arthritis, psoriatic arthritis, juvenile idiopathic arthritis and ankylosing spondylitis.{{cite news|url=http://www.nctimes.com/business/article_95a13fa4-8492-5080-8ee0-bbce644fb21b.html|title=FDA clears potential blockbuster arthritis drug|date=24 April 2009|work=North County Times|access-date=23 October 2010|publisher=Lee Enterprises|agency=Associated Press}}{{dead link|date=March 2017|bot=InternetArchiveBot|fix-attempted=yes}}{{cite journal | vauthors = Maxwell LJ, Zochling J, Boonen A, Singh JA, Veras MM, Tanjong Ghogomu E, Benkhalti Jandu M, Tugwell P, Wells GA | title = TNF-alpha inhibitors for ankylosing spondylitis | journal = The Cochrane Database of Systematic Reviews | volume = 4 | issue = 4 | pages = CD005468 | date = April 2015 | pmid = 25887212 | doi = 10.1002/14651858.CD005468.pub2 | url = http://ecite.utas.edu.au/120128 }}

Adverse effects

The most common adverse reactions (incidence >5%) are upper respiratory tract infection, nasopharyngitis, and injection site reactions.{{Drugs.com|pro|simponi}}

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.{{cite journal | vauthors = Mazumdar S, Greenwald D | title = Golimumab | journal = mAbs | volume = 1 | issue = 5 | pages = 422–31 | year = 2009 | pmid = 20065639 | pmc = 2759491 | doi = 10.4161/mabs.1.5.9286 }}

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.{{cite press release |url=http://www.jnj.com/news/all/SIMPONI-Receives-European-Commission-Approval-For-Treatment-Of-Non-Radiographic-Axial-Spondyloarthritis |title=Simponi Receives European Commission Approval For Treatment Of Non-Radiographic Axial Spondyloarthritis |website=Johnson & Johnson |access-date=9 May 2016 |archive-date=19 May 2016 |archive-url=https://web.archive.org/web/20160519204051/http://www.jnj.com/news/all/SIMPONI-Receives-European-Commission-Approval-For-Treatment-Of-Non-Radiographic-Axial-Spondyloarthritis |url-status=dead }}

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.{{cite journal | vauthors = Oldfield V, Plosker GL | title = Golimumab: in the treatment of rheumatoid arthritis, psoriatic arthritis, and ankylosing spondylitis | journal = BioDrugs | volume = 23 | issue = 2 | pages = 125–35 | year = 2009 | pmid = 19489653 | doi = 10.2165/00063030-200923020-00005 | s2cid = 195685167 }} 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.{{cite journal | vauthors = Tosh J, Archer R, Davis S, Stevenson M, Stevens JW | title = Golimumab for the treatment of rheumatoid arthritis after the failure of previous disease-modifying antirheumatic drugs: a NICE single technology appraisal | journal = PharmacoEconomics | volume = 31 | issue = 8 | pages = 653–61 | date = August 2013 | pmid = 23576019 | doi = 10.1007/s40273-013-0052-7 | s2cid = 23085023 }} Unlike other TNFi treatments such as adalimumab and certolizumab pegol, there have been no reported cases of drug-induced lupus-like syndrome (DILS).{{cite journal | vauthors = Williams VL, Cohen PR | title = TNF alpha antagonist-induced lupus-like syndrome: report and review of the literature with implications for treatment with alternative TNF alpha antagonists | journal = International Journal of Dermatology | volume = 50 | issue = 5 | pages = 619–25 | date = May 2011 | pmid = 21506984 | doi = 10.1111/j.1365-4632.2011.04871.x | s2cid = 21538173 }}

= Uveitis =

There is preliminary evidence for golimumab as a treatment option for ocular inflammation.{{cite journal | vauthors = Rifkin LM, Birnbaum AD, Goldstein DA | title = TNF inhibition for ophthalmic indications: current status and outlook | journal = BioDrugs | volume = 27 | issue = 4 | pages = 347–57 | date = August 2013 | pmid = 23568177 | doi = 10.1007/s40259-013-0022-9 | s2cid = 391892 }}

References

Category:Drugs developed by Johnson & Johnson

Category:Janssen Biotech

Category:Drugs developed by Schering-Plough

Category:Drugs developed by Merck & Co.

Category:TNF inhibitors

Category:Monoclonal antibodies

Category:World Health Organization essential medicines