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Synonyms: Actemra® | R-1569 | RG-1569 | RHPM-1 | RoActemra®
tocilizumab is an approved drug (Japan (2005), EMA (2009), FDA (2010))
Compound class: Antibody
Comment: Tocilizumab is an anti-IL-6 receptor mAb, with immunosuppressive action  that is approved for chronic autoimmune indications.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
SARS-CoV-2 and COVID-19: In early March 2020, China's National Health Commission issued guidance that allows use of tocilizumab to treat patients with serious COVID-19-induced lung damage. Tocilizumab is predicted to mitigate against the uncontrolled immune response that is triggered by SARS-CoV-2 infection [3,15] in some patients and which leads to potentially life-threatening damage to the lungs and other organs. Clinical trials are beginning to reveal outcomes (Oct 2020), but the level of benefit remains unclear [4-5,12-13] and requires further investigations. Differences between the studies (timing of treatment, severity of disease at initiation of treatment etc.) make it difficult to compare results and form a solid conclusion. In early January 2021, data was reported from a small cohort of severely ill, mechanically ventilated COVID-19 patients in the REMAP-CAP trial (NCT02735707) who received tocilizumab. The information released (data not yet peer-reviewed) suggested that tocilizumab (compared to standard care) significantly reduced mortality and that patients treated with this mAb were able to leave intensive care 7-10 days earlier than those who didn't receive the drug. This effect appears to be in addition to the clinical benefit conferred by dexamathasone. As a result of this latest report, the UK Department of Health and Social Care was set to issue updated guidance (on 8th Jan; link to gov.uk press release) which will encourage NHS trusts across the UK to immediately begin using existing stocks of tocilizumab in their treatment of critically ill COVID-19 patients in ICUs.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: tocilizumab
|No information available.|
|Summary of Clinical Use|
|Tocilizumab had been approved in Japan in 2005 as a treament for giant lymph node hyperplasia (Castleman's disease) , before being granted EMA and FDA approvals for use as a treatment for rheumatoid arthritis [6,10] and systemic and polyarticular juvenile idiopathic arthritis .
In May 2017 tocilizumab became the first FDA approved drug for the treatment of adults with giant cell arteritis.
Phase 3 clinical trials for immune conditions including ankylosing spondylitis, hand osteoarthritis, systemic sclerosis and primary Sjögren's syndrome (pSS) are ongoing. Tocilizumab was initally used off-label to manage severe or life-threatening cytokine release syndrome (CRS), which is a serious, and potentially life-threatening side effect of CAR T-cell therapy. In September 2017, the FDA extended tocilizumab approval to include treatment of CAR T-cell therapy-induced CRS. It was approved particularly to manage CRS in patients ≥2 years of age receiving tisagenlecleucel (Kymriah®,CTL019), the first CAR T-cell therapy approved for relapsed and refractory B-cell ALL.
SARS-CoV-2 and COVID-19: China's National Health Commission authorised tocilizumab as a treatment for serious COVID-19 lung damage early on in the outbreak. The Chinese Clinical Trial Registry has two studies that are designed to evaluate tocilizumab efficacy in patients with severe COVID-19 pneumonia (Registration Numbers ChiCTR2000029765 and ChiCTR2000030442). Results from an observational study, of low-dose tocilizumab in patients with confirmed elevations in inflammatory markers, showed an indication of reduced mortality . This finding was not confirmed by preliminary results from Roche's Phase 3 COVACTA RCT (NCT04320615). The limitations and differences between the studies, and reasoning that might explain the apparently contradictory findings are discussed by Campochiaro and Dagna (2020) . In addition, early results from 20 severe COVID-19 patients treated with tocilizumab have been posted on the preprint server of the Chinese Academy of Sciences (ChinaRix) (url http://www.chinaxiv.org/abs/202003.00026, DOI: 10.12074/202003.00026). Tocilizumab appears to have reduced disease symptoms and aided full recovery in 19/20 patients. In mid-March 2020, the National Cancer Institute in Naples (Italy) began a Phase 2 observational trial of tocilizumab in patients with COVID-19 pneumonia; this study is named TOCIVID-19, and has clinicaltrials.gov registry ID NCT04317092.
|Mechanism Of Action and Pharmacodynamic Effects|
|Binds to soluble and membrane-bound IL-6 receptors to inhibit IL-6 signalling via these receptors [8-9], thereby reducing the effect of the elevated/deregulated circulating IL-6 which is a hallmark of the targeted chronic autoimmume diseases.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT04356937||Efficacy of Tocilizumab on Patients With COVID-19||Phase 3 Interventional||Massachusetts General Hospital||13|
|NCT04346355||Efficacy of Early Administration of Tocilizumab in COVID-19 Patients||Phase 2 Interventional||Azienda Unità Sanitaria Locale Reggio Emilia||12|
|NCT04331808||CORIMUNO-19 - Tocilizumab Trial - TOCI (CORIMUNO-TOCI)||Phase 2 Interventional||Assistance Publique - Hôpitaux de Paris||5|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)