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 The information released (data not yet peer-reviewed) suggested that tocilizumab (compared to standard care) significantly reduced mortality and that patients treated with this mAb were able to leave intensive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

1. Biran N, Ip A, Ahn J, Go RC, Wang S, Mathura S, Sinclaire BA, Bednarz U, Marafelias M, Hansen E et al.. (2020)
Tocilizumab among patients with COVID-19 in the intensive care unit: a multicentre observational study.
The Lancet, [Epub ahead of print]. DOI: 10.1016/S2665-9913(20)30277-0
2. Campochiaro C, Dagna L. (2020)
The conundrum of interleukin-6 blockade in COVID-19.
The Lancet, [Epub ahead of print]. DOI: 10.1016/S2665-9913(20)30287-3
3. Chen X, Zhao B, Qu Y, Chen Y, Xiong J, Feng Y, Men D, Huang Q, Liu Y, Yang B et al.. (2020)
Detectable Serum Severe Acute Respiratory Syndrome Coronavirus 2 Viral Load (RNAemia) Is Closely Correlated With Drastically Elevated Interleukin 6 Level in Critically Ill Patients With Coronavirus Disease 2019.
Clin Infect Dis, 71 (8): 1937-1942. [PMID:32301997]
4. Gupta S, Wang W, Hayek SS, Chan L, Mathews KS, Melamed ML, Brenner SK, Leonberg-Yoo A, Schenck EJ, Radbel J et al.. (2021)
Association Between Early Treatment With Tocilizumab and Mortality Among Critically Ill Patients With COVID-19.
JAMA Intern Med, 181 (1): 41-51. [PMID:33080002]
5. Hermine O, Mariette X, Tharaux PL, Resche-Rigon M, Porcher R, Ravaud P, CORIMUNO-19 Collaborative Group. (2021)
Effect of Tocilizumab vs Usual Care in Adults Hospitalized With COVID-19 and Moderate or Severe Pneumonia: A Randomized Clinical Trial.
JAMA Intern Med, 181 (1): 32-40. [PMID:33080017]
6. Maini RN, Taylor PC, Szechinski J, Pavelka K, Bröll J, Balint G, Emery P, Raemen F, Petersen J, Smolen J et al.. (2006)
Double-blind randomized controlled clinical trial of the interleukin-6 receptor antagonist, tocilizumab, in European patients with rheumatoid arthritis who had an incomplete response to methotrexate.
Arthritis Rheum, 54 (9): 2817-29. [PMID:16947782]
7. Matsuyama M, Suzuki T, Tsuboi H, Ito S, Mamura M, Goto D, Matsumoto I, Tsutsumi A, Sumida T. (2007)
Anti-interleukin-6 receptor antibody (tocilizumab) treatment of multicentric Castleman's disease.
Intern Med, 46 (11): 771-4. [PMID:17541233]
8. Mihara M, Kasutani K, Okazaki M, Nakamura A, Kawai S, Sugimoto M, Matsumoto Y, Ohsugi Y. (2005)
Tocilizumab inhibits signal transduction mediated by both mIL-6R and sIL-6R, but not by the receptors of other members of IL-6 cytokine family.
Int Immunopharmacol, 5 (12): 1731-40. [PMID:16102523]
9. Nishimoto N, Kishimoto T. (2008)
Humanized antihuman IL-6 receptor antibody, tocilizumab.
Handb Exp Pharmacol, (181): 151-60. [PMID:18071945]
10. Ohsugi Y, Kishimoto T. (2008)
The recombinant humanized anti-IL-6 receptor antibody tocilizumab, an innovative drug for the treatment of rheumatoid arthritis.
Expert Opin Biol Ther, 8 (5): 669-81. [PMID:18407769]
11. Paul-Pletzer K. (2006)
Tocilizumab: blockade of interleukin-6 signaling pathway as a therapeutic strategy for inflammatory disorders.
Drugs Today, 42 (9): 559-76. [PMID:17028666]
12. Salvarani C, Dolci G, Massari M, Merlo DF, Cavuto S, Savoldi L, Bruzzi P, Boni F, Braglia L, Turrà C et al.. (2021)
Effect of Tocilizumab vs Standard Care on Clinical Worsening in Patients Hospitalized With COVID-19 Pneumonia: A Randomized Clinical Trial.
JAMA Intern Med, 181 (1): 24-31. [PMID:33080005]
13. Stone JH, Frigault MJ, Serling-Boyd NJ, Fernandes AD, Harvey L, Foulkes AS, Horick NK, Healy BC, Shah R, Bensaci AM et al.. (2020)
Efficacy of Tocilizumab in Patients Hospitalized with Covid-19.
N Engl J Med, 383 (24): 2333-2344. [PMID:33085857]
14. Unizony S, Kermani TA. (2018)
IL-6 Blockade and its Therapeutic Success in Giant Cell Arteritis.
J Neuroophthalmol, 38 (4): 551-558. [PMID:30199509]
15. Wang W, Liu X, Wu S, Chen S, Li Y, Nong L, Lie P, Huang L, Cheng L, Lin Y et al.. (2020)
Definition and Risks of Cytokine Release Syndrome in 11 Critically Ill COVID-19 Patients With Pneumonia: Analysis of Disease Characteristics.
J Infect Dis, 222 (9): 1444-1451. [PMID:32601708]
16. Yokota S, Miyamae T, Imagawa T, Katakura S, Kurosawa R, Mori M. (2005)
Clinical study of tocilizumab in children with systemic-onset juvenile idiopathic arthritis.
Clin Rev Allergy Immunol, 28 (3): 231-8. [PMID:16129907]