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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 [12] 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 to allow use of tocilizumab to treat patients with serious COVID-19-induced lung damage. Tocilizumab was predicted to mitigate against the uncontrolled immune response that is triggered by SARS-CoV-2 infection [4,17] in some patients and which leads to potentially life-threatening damage to the lungs and other organs. Clinical trials began to reveal outcomes by later in 2020, but the level of benefit remained unclear [5-6,14-15] and required further investigations. Differences between the studies (timing of treatment, severity of disease at initiation of treatment etc.) made 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 study results were published [13] in April 2021, and showed that tocilizumab (compared to standard care) significantly improved outcomes, including survival. This effect appears to be in addition to the clinical benefit conferred by dexamathasone. As a result of this report of efficacy the UK Department of Health and Social Care issued updated guidance on the use of tocilizumab (on 8th Jan; link to gov.uk press release) to NHS trusts across the UK. Long COVID: A UK clinical study (PHOSP-I) was initiated in 2024 to evaluate the benefit of tocilizumab therapy on health-related quality of life in patients with long COVID and persistent inflammation (ISRCTN46454974). Biosimilars:
Ligand Activity Visualisation ChartsThese 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 |
| Immunopharmacology Comments |
| Tocilizumab blocks IL-6R activation, which in turn leads to a reduction in cytokine and acute phase reactant production, and eventual symptomatic relief. |
| Immunopharmacology Disease | |||
| Disease | X-Refs | Comment | References |
| Temporal arteritis |
Disease Ontology:
DOID:13375 OMIM: 187360 Orphanet: ORPHA397 |
Approved drug for temporal (giant cell) arteritis (May 2017). | 16 |
| Juvenile idiopathic arthritis- systemic |
OMIM:
604302 |
An anti-IL-6 therapy approved for sJIA. | |
| Rheumatoid arthritis |
Disease Ontology:
DOID:7148 OMIM: 180300 |
Tocilizumab was the first humanized mAb to be developed against human IL-6 receptors, and is now an approved therapeutic for RA. | |
| Immunopaedia Case Studies Links |
| A case of lymphadenopathy and night sweats |
