Golimumab (brand name Simponi) is a human IgG1 monoclonal antibody derived from immunizing genetically engineered mice with human TNFα. It is a full-size antibody with a molecular mass of approximately 150 kilodaltons that exhibits multiple glycoforms. The drug binds and inhibits soluble and transmembrane human TNFα. The product was originally isolated from a hybridoma clone produced by HuMab (Medarex) transgenic mice that had been immunized with human TNFα. The golimumab-secreting clone was selected after being assayed for human light and heavy chains, and for TNFα-binding. The commercial product is produced in a recombinant cell line cultured by continuous perfusion. Golimumab was approved in the US and Canada in April 2009 as a treatment for rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis. The product was developed by Centocor and Janssen Pharmaceutical KK, in collaboration with Schering-Plough and Mitsubishi Tanabe Pharma. 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. 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 not recommended for RA patients who have failed prior TNFi treatment. Unlike other TNFi treatments such as certolizumab pegol, there have been no reported cases of drug-induced lupus-like syndrome (DILS).
Autoimmune inflammatory diseases affect approximately 7.6-9.4% of the world population, especially among the young and middle-aged women. Frequently accompanied by severe and chronic morbidity, autoimmune diseases are also leading causes of death all around world. Excessive and prolonged activation of immune cells, such as T and B lymphocytes, and overexpression of the master pro-inflammatory cytokine tumor necrosis factor alpha (TNF), together with other mediators play a central role in the pathogenesis of autoimmune inflammatory responses in rheumatoid arthritis inflammatory bowel disease, Crohn’s disease, and ankylosing spondylitis. Tumor necrosis factor (TNF), a pleiotropic cytokine mainly produced by activated macrophages, modulates a wide range of biological functions in multiple tissues and organs. Besides its effects on tumor cell death, TNF is a key mediator of both acute and chronic inflammation that serves a key role in the pathogenesis of a variety of immunological diseases. As majority of TNF-α blockers, Golimumab inhibits soluble and transmembrane forms of TNF-α binding to their specific receptors and blocking in consequence their bioactivity. Furthermore, Golimumab neither bind nor inhibit other members of TNF-α such as the lymphotoxin (TNF-β) Competing with TNF-α receptors, Golimumab regulates TNF-α pro-inflammatory cytokines essentially produced by activated macrophages. Golimumab has also the power to fix complement inducing cell lysis and to participate in immune responses implicating antibody-dependent cell cytotoxicity function. Following Golimumab therapy, numerous positive responses related to RA disease cure were obtained, such as reductions in levels of C-reactive protein (CRP), IL-6, MMP-3, ICAM-1, and VEGF.
Fig 1. Mechanism of Action of Golimumab
Table 1. Clinical Projects of Golimumab*
NCT ID | Status | Conditions | Lead Sponsor | Update Time |
NCT03669029 | Not yet recruiting | Colitis, Ulcerative | Hospital de Manises | September 13, 2018 |
NCT03182166 | Recruiting | Ulcerative Colitis | Centre Hospitalier Universitaire de Saint Etienne | June 9, 2017 |
NCT03733925 | Recruiting | Spondylitis, Ankylosing, Arthritis, Psoriatic | Johnson & Johnson Private Limited | November 7, 2018 |
NCT03298542 | Recruiting | Pre-Symptomatic Type 1 Diabetes | Janssen Research & Development, LLC | October 2, 2017 |
NCT02277444 | Active, not recruiting | Arthritis, Juvenile | Janssen Research & Development, LLC | October 29, 2014 |
NCT01900574 | Active, not recruiting | Colitis, Ulcerative | Janssen Research & Development, LLC | July 16, 2013 |
NCT03394586 | Recruiting | Ulcerative Colitis, Flare Up, Symptom | University of Zurich | January 9, 2018 |
NCT03124121 | Recruiting | Ulcerative Colitis | Guy's and St Thomas' NHS Foundation Trust | April 21, 2017 |
NCT03729349 | Recruiting | Arthritis, Rheumatoid | Janssen Inc. | November 2, 2018 |
NCT03557853 | Active, not recruiting | Ankylosing Spondylitis, Coxitis | MSD Pharmaceuticals LLC | June 15, 2018 |
NCT02425865 | Not yet recruiting | ULCERATIVE COLITIS | Groupe d'Etude Therapeutique des Affections Inflammatoires Digestives | April 24, 2015 |
NCT02910375 | Active, not recruiting | Ulcerative Colitis | Universitaire Ziekenhuizen Leuven | September 22, 2016 |
NCT02728934 | Active, not recruiting | Arthritis, Rheumatoid | Janssen Scientific Affairs, LLC | April 5, 2016 |
NCT02846545 | Active, not recruiting | Diabetes Mellitus, Type 1 | Janssen Research & Development, LLC | July 27, 2016 |
NCT03596645 | Recruiting | Colitis, Ulcerative | Janssen Research & Development, LLC | July 24, 2018 |
NCT03773445 | Recruiting | Ulcerative Colitis | Hospital San Carlos, Madrid | December 12, 2018 |
NCT03632759 | Recruiting | Type 1 Diabetes Mellitus | Carla Greenbaum, MD | August 15, 2018 |
NCT03270501 | Not yet recruiting | Axial Spondyloarthritis | University Ghent | September 1, 2017 |
NCT02868398 | Recruiting | Ulcerative Colitis | Evangelismos Hospital | August 16, 2016 |
NCT03662542 | Recruiting | Colitis, Ulcerative | Janssen Research & Development, LLC | September 7, 2018 |
NCT02914717 | Active, not recruiting | Ulcerative Colitis | Universitaire Ziekenhuizen Leuven | September 26, 2016 |
NCT03253796 | Active, not recruiting | Spondyloarthritis | Merck Sharp & Dohme Corp. | August 18, 2017 |
NCT02758782 | Active, not recruiting | Ankylosing Spondylitis | Charite University, Berlin, Germany | May 2, 2016 |
NCT01804166 | Recruiting | Hepatosplenic T-Cell Lymphoma | Janssen Scientific Affairs, LLC | March 5, 2013 |
NCT02687724 | Recruiting | Colitis | University College Dublin | February 22, 2016 |
NCT03011268 | Recruiting | Colitis,Ulcerative | Helse Møre og Romsdal HF | January 5, 2017 |
NCT02935387 | Recruiting | Arthritis, Rheumatoid | UMC Utrecht | October 17, 2016 |
NCT01602302 | Recruiting | Rheumatoid Arthritis | Medical University of Graz | May 18, 2012 |
NCT02808780 | Recruiting | Ulcerative Colitis | Janssen Biotech, Inc. | June 22, 2016 |
NCT01965132 | Recruiting | Rheumatoid Arthritis, Ankylosing Spondylitis, Psoriatic Arthritis | Seoul National University Hospital | October 18, 2013 |
NCT03445845 | Not yet recruiting | Axial Spondyloarthritis | Centre Hospitalier Universitaire de Saint Etienne | February 26, 2018 |
NCT03100253 | Recruiting | Rheumatoid Arthritis | Mario Negri Institute for Pharmacological Research | April 4, 2017 |
NCT02456363 | Recruiting | Ankylosing Spondylitis | Chung Shan Medical University | May 28, 2015 |
NCT03679546 | Not yet recruiting | Ulcerative Colitis | Rennes University Hospital | September 20, 2018 |
NCT03016260 | Recruiting | RheumatoId Arthritis | TcLand Expression S.A. | January 10, 2017 |
NCT03168347 | Recruiting | Psoriasis | Wake Forest University Health Sciences | May 30, 2017 |
NCT03219359 | Recruiting | Crohn Disease | Icahn School of Medicine at Mount Sinai | July 17, 2017 |
NCT02674308 | Recruiting | Ulcerative Colitis and Crohn's Disease | Takeda | February 4, 2016 |
NCT02755194 | Recruiting | Lactation | The Hospital for Sick Children | April 28, 2016 |
NCT03710486 | Recruiting | Ulcerative Colitis, Crohn's Disease | Takeda | October 18, 2018 |
NCT02714634 | Not yet recruiting | Rheumatoid Arthritis, Insufficient Response to Methotrexate. | University Hospital, Strasbourg, France | March 21, 2016 |
NCT01764321 | Active, not recruiting | Rheumatoid Arthritis | UCB Pharma SA | January 9, 2013 |
NCT03775824 | Active, not recruiting | Rheumatoid Arthritis | Region Skane | December 14, 2018 |
NCT03591770 | Not yet recruiting | Inflammatory Bowel Diseases | Boston Medical Center | July 19, 2018 |
NCT02242474 | Recruiting | Rheumatoid Arthritis | CHU de Quebec-Universite Laval | September 17, 2014 |
NCT01848028 | Recruiting | Psoriasis, Psoriatic-arthritis | Universitätsklinikum Hamburg-Eppendorf | May 7, 2013 |
NCT03056924 | Recruiting | Inflammatory Bowel Diseases | Boston Medical Center | February 17, 2017 |
Table 2. Approved Drugs of Golimumab**
INN (trade name) | Therapeutic area | Dose | Strength | Route | Company | Marketing start | Market |
Simponi | Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, Ulcerative Colitis | Concentrate for injection | 50MG | Subcutaneous injection | Centocor Ortho Biotech | April 24, 2019 |
![]() |
Simponi | Active rheumatoid arthritis, Active and progressive psoriatic arthritis, Axial spondyloarthritis, Moderately to severely active ulcerative colitis, Polyarticular juvenile idiopathic arthritis | Solution for injection | 50MG | Subcutaneous injection | Janssen Biologics | October 1, 2009 |
![]() |
Reference
*The table was excerpted from the following website
https://clinicaltrials.gov/ct2/results?term=Golimumab
**Information presented in the table were collected from the following website:
https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=125289
For research use only. Not intended for any clinical use.
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.