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| rdf:type
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| http://linked.open...gbank/description
| - Canakinumab is a recombinant, human anti-human-IL-1β monoclonal antibody that belongs to the IgG1/κ isotype subclass. It is expressed in a murine Sp2/0-Ag14 cell line and comprised of two 447- (or 448-) residue heavy chains and two 214-residue light chains, with a molecular mass of 145157 Daltons when deglycosylated. Both heavy chains of canakinumab contain oligosaccharide chains linked to the protein backbone at asparagine 298 (Asn 298). Canakinumab binds to human IL-1β and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1alpha or IL-1 receptor antagonist (IL-1ra). Canakinumab is marketed under the brand name Ilaris and indicated for patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). Clinical trials have established the administration of canakinumab every 2 weeks to be safe and effective, offering a considerable advantage over the existing treatment with the human IL-1 receptor antagonist, anakinra, which must be injected daily and which is often poorly tolerated by patients. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Church LD, McDermott MF: Canakinumab, a fully-human mAb against IL-1beta for the potential treatment of inflammatory disorders. Curr Opin Mol Ther. 2009 Feb;11(1):81-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19169963 # IMGT "Link":http://imgt.cines.fr/3Dstructure-DB/cgi/details.cgi?pdbcode=8836 # Lachmann HJ, Kone-Paut I, Kuemmerle-Deschner JB, Leslie KS, Hachulla E, Quartier P, Gitton X, Widmer A, Patel N, Hawkins PN: Use of canakinumab in the cryopyrin-associated periodic syndrome. N Engl J Med. 2009 Jun 4;360(23):2416-25. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19494217 # FDA label. (en)
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| http://linked.open...gy/drugbank/group
| - approved (en)
- investigational (en)
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| http://linked.open...drugbank/halfLife
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| http://linked.open...ugbank/indication
| - Used in patients 4 years of age and older to treat Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS), which are both part of the Cryopyrin-Associated Periodic Syndromes (CAPS) as well as for patients 2 years of age and older to treat systemic juvenile idiopathic arthritis (SJIA). (en)
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| Title
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| adms:identifier
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| http://linked.open...mechanismOfAction
| - In inflammatory diseases involving Cryopyrin-Associated Periodic Syndromes (CAPS), interleukin-1 beta (IL-1β) is excessively activated and drives inflammation. The protein cryopyrin controls the activation of IL-1β, and mutations in cryopyrin's gene, NLRP-3, up-regulate IL-1β activation. Canakinumab is a human monoclonal anti-human IL-1β antibody of the IgG1/κ isotype. Canakinumab binds to human IL-1β and neutralizes its inflammatory activity by blocking its interaction with IL-1 receptors, but it does not bind IL-1α or IL-1 receptor antagonist (IL-1ra). (en)
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| http://linked.open...outeOfElimination
| - The route of elimination for canakinumab has not yet been determined. (en)
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| http://linked.open.../drugbank/synonym
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| http://linked.open...drugbank/toxicity
| - The most common adverse reactions involved the central nervous system (headache and vertigo), gastrointestinal system (diarrhea and nausea), neuromuscular and skeletal system (musculoskeletal pain), and respiratory system (rhinitis, nasopharyngitis and bronchitis). Influenza was also reported. (en)
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| http://linked.open...umeOfDistribution
| - * 6.01 L [typical CAPS patient weighing 70 kg] (en)
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| http://linked.open...k/foodInteraction
| - No food effects were found. (en)
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| http://linked.open...nk/proteinBinding
| - Canakinumab binds to plasma IL-1β, but plasma protein binding was not quantified. (en)
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| http://linked.open...y/mesh/hasConcept
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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
| - The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%. (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...drugbank/category
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| http://linked.open...rugbank/clearance
| - * 0.174 L/day [typical CAPS patient weighing 70 kg] (en)
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