Tocilizumab
- Atc Codes:L04AC07
- CAS Codes:375823-41-9
- PHARMGKB ID:375823-41-9
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: RoActemra; Belgium: RoActemra; Bulgaria: RoActemra; Czech Republic: RoActemra; Denmark: RoActemra; Estonia: RoActemra; Finland: RoActemra; France: RoActemra; Germany: RoActemra; Greece: RoActemra; Hungary: RoActemra; Ireland: RoActemra; Italy: RoActemra; Latvia: RoActemra; Lithuania: RoActemra; Luxembourg: RoActemra; Malta: RoActemra; Netherlands: RoActemra; Poland: RoActemra; Portugal: RoActemra; Romania: RoActemra; Slovakia: RoActemra; Slovenia: RoActemra; Spain: RoActemra; Sweden: RoActemra; UK: RoActemra.
North America
Canada: Actemra; USA: Actemra.
Latin America
Argentina: Actemra; Brazil: Actemra; Mexico: RoActemra.
Asia
Japan: Actemra.
Drug combinations
Chemistry
Tocilizumab: C~6428~H~9976~N~1720~O~2018~S~42~. Mw: 148. Recombinant humanized anti-human interleukin 6 (IL-6) receptor monoclonal antibody of the immunoglobulin IgG1k (γ1, κ) subclass with a typical H2L2 polypeptide structure. Each light chain and heavy chain consists of 214 and 448 aa, respectively. The four polypeptide chains are linked intra- and inter-molecularly by disulfide bonds. CAS-375823-41-9.
Pharmacologic Category
Biologic Response Modifiers. Disease-modifying Antirheumatic Drugs; Interleukin-6 Receptor Antagonist. (ATC-Code: L04AC07).
Mechanism of action
Tocilizumab binds specifically to both soluble and membrane-bound IL-6 receptors (sIL-6R and mIL-6R), and has been shown to inhibit IL-6-mediated signaling through these receptors. IL-6 is a pleiotropic pro-inflammatory cytokine produced by a variety of cell types including T- and B-cells, lymphocytes, monocytes and fibroblasts. IL-6 has been shown to be involved in diverse physiological processes such as T-cell activation, induction of immunoglobulin secretion, initiation of hepatic acute phase protein synthesis, and stimulation of hematopoietic precursor cell proliferation and differentiation. IL-6 is also produced by synovial and endothelial cells leading to local production of IL-6 in joints affected by inflammatory processes such as rheumatoid arthritis (RA).
Therapeutic use
Treatment of adult patients with moderately-to-severely active rheumatoid arthritis who have had an inadequate response to one or more TNF antagonist therapies.
Pregnancy and lactiation implications
Based on animal data, may cause fetal harm. Pregnancy registry available. Not recommended during lactation.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Serious infections leading to hospitalization or death including tuberculosis (TB), bacterial, invasive fungal, viral, and other opportunistic infections have occurred in patients receiving tocilizumab (do not administer during an active infection, including localized infections; if a serious infection develops, interrupt therapy until the infection is controlled). Gastrointestinal perforation has been observed. Laboratory monitoring is recommended due to potential consequences of treatment-related changes in neutrophils, platelets, lipids, and liver function tests. Anaphylaxis or serious hypersensitivity reactions have occurred. Live vaccines should not be given with tocilizumab. Treatment with immunosuppressants may result in an increased risk of malignancies. Demyelinating disorders have been reported. Not recommended in patients with active hepatic disease or hepatic impairment.