tocilizumab   Click here for help

GtoPdb Ligand ID: 6881

Synonyms: Actemra® | R-1569 | RG-1569 | RHPM-1 | RoActemra®
Approved drug Immunopharmacology Ligand
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 [11] 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 The information released (data not yet peer-reviewed) suggested that tocilizumab (compared to standard care) significantly reduced mortality and that patients treated with this mAb were able to leave intensive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 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.

NameTrade nameCompanyClinical PhaseIndications
tocilizumab-bavi; BIIB800Tofidence BiogenApproved (2023)As per reference agent
QX003Sn/aQyuns Therapeutics1rheumatoid arthritis
tocilizumab-aazg; MSB11456n/aFresenius Kabi3rheumatoid arthritis
LZM008n/a Livzon Mabpharm1rheumatoid arthritis
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View more information in the IUPHAR Pharmacology Education Project: tocilizumab

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Summary of Clinical Use Click here for help
Tocilizumab had been approved in Japan in 2005 as a treament for giant lymph node hyperplasia (Castleman's disease) [7], before being granted EMA and FDA approvals for use as a treatment for rheumatoid arthritis [6,10] and systemic and polyarticular juvenile idiopathic arthritis [16].
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 [1]. 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) [2]. 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, 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 registry ID NCT04317092.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
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 Trials
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
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