Canakinumab
- Atc Codes:L04AC08
- CAS Codes:914613-48-2
- PHARMGKB ID:914613-48-2
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
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Ilaris; Bulgaria: Ilaris; Czech Republic: Ilaris; Denmark: Ilaris; Estonia: Ilaris; Finland: Ilaris; France: Ilaris; Germany: Ilaris; Greece: Ilaris; Hungary: Ilaris; Ireland: Ilaris; Latvia: Ilaris; Lithuania: Ilaris; Luxembourg: Ilaris; Netherlands: Ilaris; Poland: Ilaris; Portugal: Ilaris; Slovakia: Ilaris; Slovenia: Ilaris; Sweden: Ilaris; UK: Ilaris.
North America
Canada: Ilaris; USA: Ilaris.
Drug combinations
Chemistry
Canakinumab: C~6452~H~9958~N~1722~O~2010~S~42~. Mw: 145 kDa (deglycosylated). (1) Immunoglobulin G~1~, anti-[Homo sapiens interleukin 1, β (IL1β)] human monoclonal ACZ885; (2) γ~1~ heavy chain (Homo sapiens VH-IGHG1*03)(221-214′)-disulfide with κ light chain (Homo sapiens V-κ-IGKC*01); (3)(227-227»:230-230»)-bisdisulfide dimer. (4) Recombinant human anti-human-IL-1β monoclonal antibody IgG~1~/κ isotype subclass comprised of two 447- (or 448-) residue heavy chains and two 214-residue light chains. CAS: 914613-48-2.
Pharmacologic Category
Immunosuppressive Agents, Selective Interleukin-1-beta (IL-1-β) Inhibitor. (ATC-Code: L04AC08).
Mechanism of action
Canakinumab is a human monoclonal anti-human IL-1-β antibody of the IgG~1~/κ isotype. Canakinumab binds to human IL-1-β and neutralizes its activity by blocking its interaction with IL-1 receptors, but it does not bind to IL-1-α or IL-1 receptor antagonist. Cryopyrin-Associated Periodic Syndromes (CAPS) refer to rare genetic syndromes generally caused by mutations in the NLRP-3 (NLR family, pyrin domain containing 3) gene (also known as Cold-Induced Auto-inflammatory Syndrome-1 [CIAS1]). The NLRP-3 gene encodes the protein cryopyrin, an important component of the inflammasome. Cryopyrin regulates the protease caspase-1 and controls the activation of interleukin-1-β (IL-1-β). Mutations in NLRP-3 result in an overactive inflammasome resulting in excessive release of activated IL-1-β that drives inflammation.
Therapeutic use
Canakinumab is an interleukin-1-β blocker indicated for the treatment of CAPS, in adults and children 4 years of age and older including Familial Cold Autoinflammatory Syndrome (FCAS) and Muckle-Wells Syndrome (MWS).
Pregnancy and lactiation implications
No human data in pregnancy. This drug should be used during pregnancy only if clearly needed. Caution should be exercised when administered to a nursing woman.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Interleukin-1 blockade may interfere with immune response to infections. Treatment with medications that work through inhibition of IL-1 has been associated with an increased risk of serious infections. Caution when administering this drug to patients with infections, history of recurring infections or underlying conditions which may predispose them to infections. Treatment should be discontinued if patient develops a serious infection. Treatment should not be initiated in patients with active infection requiring medical intervention. Live vaccines should not be given concurrently with this product. Prior to initiation of therapy, patients should receive all recommended vaccinations.