Tocilizumab

verifiedfields	changed
watchedfields	changed
verifiedrevid	477864483
type	mab
mab type	mab
source	zu/o
target	IL-6 receptor
tradename	Actemra, Roactemra
medlineplus	a611004
dailymedid	Tocilizumab
pregnancy au	C
routes of administration	Intravenous, subcutaneous
atc prefix	L04
atc suffix	AC07
biosimilars	tocilizumab-aazg,‡R1R‡‡R2R‡‡R3R‡ tocilizumab-anoh,‡R4R‡ tocilizumab-bavi,‡R5R‡‡R6R‡ Avtozma,‡R7R‡ Tofidence,‡R5R‡‡R6R‡‡R8R‡ Tyenne‡R1R‡
legal au	S4
legal au comment	‡R9R‡‡R10R‡
legal ca	Rx-only
legal ca comment	‡R11R‡‡R12R‡
legal us	Rx-only
legal us comment	‡R13R‡ and Emergency Use Authorization
legal eu	Rx-only
legal eu comment	‡R14R‡‡R15R‡‡R16R‡
legal status	Rx-only
elimination half-life	8–14 days during steady state (dependent on concentration)
cas number	375823-41-9
drugbank	DB06273
chemspiderid	none
unii	I031V2H011
kegg	D02596
chembl	1237022
c	6428
h	9976
n	1720
o	2018
s	42

Tocilizumab, sold under the brand name Actemra among others, is an immunosuppressive drug, used for the treatment of rheumatoid arthritis, systemic juvenile idiopathic arthritis, polyarticular juvenile idiopathic arthritis, giant cell arteritis, cytokine release syndrome, COVID19, and systemic sclerosis-associated interstitial lung disease (SSc-ILD). It is a recombinant humanized monoclonal antibody of the immunoglobulin IgG1 subclass against the interleukin-6 receptor (IL-6R).[17] Interleukin 6 (IL-6) is a cytokine that plays an important role in immune response and is implicated in the pathogenesis of many diseases, such as autoimmune diseases, multiple myeloma and prostate cancer. Tocilizumab was jointly developed by Osaka University and Chugai, and was licensed in 2003 by Hoffmann-La Roche.[18]

Tocilizumab was approved for medical use in the European Union in January 2009,[19]

Medical uses

In the United States, tocilizumab is indicated for the treatment of rheumatoid arthritis, giant cell arteritis, systemic sclerosis-associated interstitial lung disease, polyarticular juvenile idiopathic arthritis, systemic juvenile idiopathic arthritis, cytokine release syndrome, and COVID19.[13]

In the European Union, tocilizumab is indicated for the treatment of rheumatoid arthritis, systemic juvenile idiopathic arthritis, juvenile idiopathic polyarthritis, giant cell arteritis, cytokine release syndrome, and COVID19.[19]

Rheumatoid arthritis

Tocilizumab is used for the treatment of moderate to severe rheumatoid arthritis, applied in combination with methotrexate, if other drugs like disease-modifying antirheumatic drugs (DMARDs) and TNF alpha blockers have proven to be ineffective or were not tolerated. It can be used as a monotherapy for patients who do not tolerate methotrexate.[22][23] The drug slows down the progression of the disease and can improve physical function of patients.[24]

Systemic juvenile idiopathic arthritis

The treatment of systemic juvenile idiopathic arthritis is similar to rheumatoid arthritis treatment: tocilizumab is combined with methotrexate unless the latter is not tolerated. General safety and effectiveness is established for children of two years and older.[25] In 2011, the US Food and Drug Administration (FDA) approved tocilizumab for the treatment of active systemic juvenile idiopathic arthritis.[26]

Castleman's disease

In Japan, tocilizumab is also approved for the treatment of Castleman's disease,[22][27] a rare benign tumor of B cells.

Giant cell arteritis

In May 2017, the FDA approved tocilizumab for giant cell arteritis.[28]

Cytokine release syndrome

On 30 August 2017, the FDA approved tocilizumab for cytokine release syndrome, a side effect of CAR-T cell therapies.[29]

COVID-19

As early as March 2020, at the height of the pandemic in Italy, Paolo Antonio Ascierto, an Italian oncologist, researched alongside his colleagues the use of the arthritis drug tocilizumab to treat severe COVID-19 pneumonia, seeing some results.[30] The results were recognized nationally and prompted national calls for treatment protocols surrounding the research.[31] Ascierto was heard in an official hearing at the Italian Chamber of Deputies, presenting data suggesting tocilizumab reduced COVID-19 mortality by approximately 22% in clinical use, underscoring its potential benefit.[32] Paolo was at the center of the development of multicenter evaluations of tocilizumab against COVID-19 pneumonia during the whole year, being essential to it.[32]

In 2021 his research of the usage of tocilizumab against COVID-19 was evaluated by the European Medicines Agency and the European Union, where Ascierto was called to as to support such thesis.[33]

Society and culture

Legal status

Tocilizumab was approved for medical use in the European Union in January 2009,[19] and in the United States in January 2010.[20][21]

Biosimilars

In September 2023, Tyenne became the first tocilizumab biosimilar authorized for medical use in the European Union,[15][48] and in March 2024, became the first biosimilar with both intravenous and subcutaneous formulations to be approved in the United States.[49][50]

In April 2024, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Tofidence, intended for the treatment of rheumatoid arthritis (RA), systemic juvenile idiopathic arthritis (sJIA), polyarticular juvenile idiopathic arthritis (pJIA) and coronavirus disease 2019 (COVID-19).[51] The applicant for this medicinal product is Biogen Netherlands B.V.[52] Tofidence is a biosimilar medicinal product.[52] Tofidence was authorized for medical use in the European Union in June 2024.[53]

Tyenne was approved for medical use in Canada in October 2024.[54][55]

In December 2024, the CHMP adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Avtozma, intended for the treatment of rheumatoid arthritis, systemic juvenile idiopathic arthritis, polyarticular juvenile idiopathic arthritis, giant cell arteritis, CAR-T cell-induced severe or life-threatening cytokine release syndrome and COVID-19.[17] The applicant for this medicinal product is Celltrion Healthcare Hungary Kft.[17] Avtozma is a biosimilar medicinal product.[17]

Tocilizumab-anoh (Avtozma) was approved for medical use in the United States in January 2025.[56][57][58]

Avtozma was approved for medical use in Canada in October 2025.[59]

COVID-19

Tocilizumab was approved for the treatment of COVID19 in the European Union in December 2021,[19] and in the United States in December 2022.[34]

In September 2021, Indian pharmaceutical firm Hetero obtained emergency use approval from the country's health authority, Drugs Controller General of India (DCGI), to produce a generic version of tocilizumab to treat COVID19 in adults.[60]

In December 2021, tocilizumab was granted a provisional approval by the Australian regulator, Therapeutic Goods Administration, for treatment of adults.[61]

Tocilizumab was granted an emergency use authorization (EUA) for the treatment of COVID19 in the United States in June 2021.[62][63]

Biosimilars

COVID-19

Tocilizumab was approved for the treatment of COVID19 in the European Union in December 2021,[19] and in the United States in December 2022.[34]

In December 2021, tocilizumab was granted a provisional approval by the Australian regulator, Therapeutic Goods Administration, for treatment of adults.[61]

Tocilizumab was granted an emergency use authorization (EUA) for the treatment of COVID19 in the United States in June 2021.[62][63]

Tocilizumab

Medical uses

Rheumatoid arthritis

Systemic juvenile idiopathic arthritis

Castleman's disease

Giant cell arteritis

Cytokine release syndrome

COVID-19

Adverse effects

Interactions

Mechanism of action

History

Society and culture

Legal status

Biosimilars

COVID-19

Biosimilars

COVID-19

Research

COVID-19

Neuromyelitis optica

Graves' ophthalmopathy

External links

References