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Statements

Subject Item
n2:DB06168
rdf:type
n3:Drug
n3: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.
n3:dosage
n18:271B498D-363D-11E5-9242-09173F13E4C5 n18:271B498E-363D-11E5-9242-09173F13E4C5
n3: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.
n3:group
investigational approved
n3:halfLife
26 days
n3: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).
owl:sameAs
n12:DB06168 n16:DB06168
dcterms:title
Canakinumab
adms:identifier
n10:DB06168 n15:D09315 n19:0078-0582-61 n20:Canakinumab
n3: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).
n3:routeOfElimination
The route of elimination for canakinumab has not yet been determined.
n3:synonym
ACZ-885 ACZ885
n3: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.
n3:volumeOfDistribution
* 6.01 L [typical CAPS patient weighing 70 kg]
n3:foodInteraction
No food effects were found.
n3:proteinBinding
Canakinumab binds to plasma IL-1β, but plasma protein binding was not quantified.
n13:hasConcept
n14:M0536437
foaf:page
n8:ilaris-drug.htm n21:canakinumab.html
n3:Molecular-Formula
n4:271B4990-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B498F-363D-11E5-9242-09173F13E4C5
n5:hasATCCode
n6:L04AC08
n3:absorption
The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
914613-48-2
n3:category
n3:clearance
* 0.174 L/day [typical CAPS patient weighing 70 kg]