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 [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:
NameTrade nameCompanyClinical PhaseIndications
tocilizumab-bavi; BIIB800Tofidence BiogenApproved (2023)As per reference agent
QX003Sn/aQyuns Therapeutics1 [19]inflammatory/immune diseases
tocilizumab-aazg; MSB11456TyenneFresenius KabiApproved (2023)As per reference agent
LZM008n/a Livzon Mabpharm1 [3]inflammatory/immune diseases
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Bioactivity Comments
Unfortunately, we have been unable to find publicly available data providing a binding affinity for this antibody at its molecular target.
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
Interleukin-6 receptor Primary target of this compound Hs Antibody Binding 8.6 pKd -
pKd 8.6 (Kd 2.54x10-9 M)