| Attributes | Values |
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| rdf:type
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| http://linked.open...gbank/description
| - Tocilizumab is a recombinant, humanized, anti-human interleukin 6 (IL-6) receptor monoclonal antibody that achieves a significant therapeutic response rate. The light chain is made up of 214 amino acids. The heavy chain is made up of 448 amino acids. The four polypeptide chains are linked intra- and inter-molecularly by disulfide bonds. FDA approved on January 8, 2010. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Mihara M, Nishimoto N, Ohsugi Y: The therapy of autoimmune diseases by anti-interleukin-6 receptor antibody. Expert Opin Biol Ther. 2005 May;5(5):683-90. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15934843 (en)
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - The half-life of tocilizumab is concentration-dependent. The concentration-dependent apparent half-life is up to 11 days for 4 mg/kg and up to 13 days for 8 mg/kg every 4 weeks in patients with RA at steady-state. The half-life in children with PJIA is up to 16 days. The half-life in pediatric patients with SJIA is up to 23 days. (en)
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| http://linked.open...ugbank/indication
| - Indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response to one or more Disease-Modifying Anti-Rheumatic Drugs (DMARDs). It is also indicated for the treatment of active polyarticular juvenile idiopathic arthritis (PJIA) and active systemic juvenile idiopathic arthritis (SJIA) in patients 2 years of age and older. (en)
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| sameAs
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - Interleukin (IL)-6 plays essential roles not only in the immune response, but also in haematopoiesis and the central nervous system. Deregulated production of IL-6 has been found in chronic inflammatory autoimmune diseases, such as rheumatoid arthritis (RA), systemic onset juvenile idiopathic arthritis (soJIA), Crohn's disease (CD) and systemic lupus erythematosus (SLE). Furthermore, IL-6 activities can explain many symptoms of these diseases. More importantly, serum levels of IL-6 are correlated with disease activity. 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. (en)
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - Following intravenous dosing, tocilizumab undergoes biphasic elimination from the circulation. (en)
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| http://linked.open.../drugbank/synonym
| - Atlizumab (en)
- MRA (en)
- RoActemra® (en)
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| http://linked.open...drugbank/toxicity
| - Most common adverse reactions (incidence of at least 5%): upper respiratory tract infections, nasopharyngitis, headache, hypertension, increased ALT. (en)
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| http://linked.open...umeOfDistribution
| - In rheumatoid arthritis patients the central volume of distribution was 3.5 L and the peripheral volume of distribution was 2.9 L, resulting in a volume of distribution at steady state of 6.4 L. In pediatric patients with PJIA, the central volume of distribution was 1.98 L, the peripheral volume of distribution was 2.1 L, resulting in a volume of distribution at steady state of 4.08 L. In pediatric patients with SJIA, the central volume of distribution was 0.94 L, the peripheral volume of distribution was 1.60 L resulting in a volume of distribution at steady state of 2.54 L. (en)
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| http://linked.open.../drug/hasAHFSCode
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| foaf:page
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...ugbank/absorption
| - When 4 mg/kg of tocilizumab was given every 4 weeks to RA patients, the pharmacokinetic parameters at steady state are as follows: AUC = 13000 ± 5800 mcg∙h/mL; Cmax = 88.3 ± 41.4 mcg/mL. Tocilizumab accumulates following repeated doses. Furthermore, an increased body weight may increase plasma levels of tocilizumab. When a dose of 8 mg/kg of tocilizumab is given to PJIA patients, the pharmacokinetic parameters are as follows: AUC = 29500 ± 8660 mcg∙h/mL; Cmax = 182 ± 37 mcg/mL. When a dose of 8 mg/kg of tocilizumab is given to SJIA patients, the pharmacokinetic parameters are as follows: AUC = 32200 ± 9960 mcg∙h/mL; Cmax = 245 ± 57.2 mcg/mL. (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...rugbank/clearance
| - The clearance of tocilizumab decreases with increasing dose. At the 10 mg/kg single dose in RA patients, mean clearance was 0.29 ± 0.10 mL/hr/kg. The total clearance of tocilizumab is concentration-dependent and is the sum of the linear clearance and the nonlinear clearance. At low concentrations, concentration-dependent nonlinear clearance is dominant. At high concentrations, linear clearance dominates. The estimated linear clearances for specific patient populations are as follows: RA = 12.5 mL/h; PJIA, pediatric patients = 5.8 mL/h; SJIA, pediatric patients = 7.1 mL/h. (en)
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