Canakinumab
Identification
- Name
- Canakinumab
- Accession Number
- DB06168
- 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.
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- C6452H9958N1722O2010S42
- Protein Average Weight
- 145200.0 Da
- Sequences
>8836_H|canakinumab|Homo sapiens||H-GAMMA-1 (VH(1-118)+CH1(119-216)+HINGE-REGION(217-231)+CH2(232-341)+CH3(342-448))|||||||448||||MW 49253.6|MW 49253.6| QVQLVESGGGVVQPGRSLRLSCAASGFTFSVYGMNWVRQAPGKGLEWVAIIWYDGDNQYY ADSVKGRFTISRDNSKNTLYLQMNGLRAEDTAVYYCARDLRTGPFDYWGQGTLVTVSSAS TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL YSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPS VFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNST YRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMT KNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQ GNVFSCSVMHEALHNHYTQKSLSLSPGK
>8836_L|canakinumab|Homo sapiens||L-KAPPA (V-KAPPA(1-107)+C-KAPPA(108-214))|||||||214||||MW 23357.9|MW 23357.9| QVQLVESGGGVVQPGRSLRLSCAASGFTFSVYGMNWVRQAPGKGLEWVAIIWYDGDNQYY ADSVKGRFTISRDNSKNTLYLQMNGLRAEDTAVYYCARDLRTGPFDYWGQGTLVTVSSAS TKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGL EIVLTQSPDFQSVTPKEKVTITCRASQSIGSSLHWYQQKPDQSPKLLIKYASQSFSGVPS RFSGSGSGTDFTLTINSLEAEDAAAYYCHQSSSLPFTFGPGTKVDIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- Not Available
- External IDs
- ACZ-885
- ACZ885
Pharmacology
- 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).
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Novartis AG has developed canakinumab as a subcutaneous injection and fully human mAb that neutralizes the bioactivity of human IL-1beta, which is involved in several inflammatory disorders. Canakinumab has promising clinical safety and pharmacokinetic properties, and demonstrated potential for the treatment of cryopyrin-associated periodic syndromes (CAPS), systemic juvenile idiopathic arthritis (SJIA), and possibly for other complex inflammatory diseases, such as rheumatoid arthritis, COPD disease and ocular diseases.
- Mechanism of action
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).
Target Actions Organism AInterleukin-1 beta binderHumans - Absorption
The absolute bioavailability of subcutaneous canakinumab is estimated to be 70%.
- Volume of distribution
- 6.01 L [typical CAPS patient weighing 70 kg]
- Protein binding
Canakinumab binds to plasma IL-1β, but plasma protein binding was not quantified.
- Metabolism
The metabolism of canakinumab is not yet determined.
- Route of elimination
The route of elimination for canakinumab has not yet been determined.
- Half-life
26 days
- Clearance
- 0.174 L/day [typical CAPS patient weighing 70 kg]
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- 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.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Canakinumab. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Canakinumab. Abiraterone The metabolism of Abiraterone can be increased when combined with Canakinumab. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Canakinumab. Acebutolol The metabolism of Acebutolol can be increased when combined with Canakinumab. Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Canakinumab. Acetaminophen The metabolism of Acetaminophen can be increased when combined with Canakinumab. Acetohexamide The metabolism of Acetohexamide can be increased when combined with Canakinumab. Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be increased when combined with Canakinumab. Acyclovir The metabolism of Acyclovir can be increased when combined with Canakinumab. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Take with or without food.
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataIlaris Injection, powder, for solution 150 mg Subcutaneous Novartis Europharm Limited 2009-10-23 Not applicable EU 
Ilaris Powder, for solution 150 mg Subcutaneous Novartis 2010-04-27 2020-01-13 Canada 
Ilaris Injection, powder, for solution 150 mg Subcutaneous Novartis Europharm Limited 2009-10-23 Not applicable EU Ilaris Injection, solution 150 mg/1mL Subcutaneous Novartis Pharmaceuticals Corporation 2016-12-22 Not applicable US 
Ilaris Injection, powder, for solution 150 mg Subcutaneous Novartis Europharm Limited 2009-10-23 Not applicable EU Ilaris Solution 150 mg Subcutaneous Novartis 2017-08-22 Not applicable Canada Ilaris Injection, powder, lyophilized, for solution 150 mg/1mL Subcutaneous Novartis Pharmaceuticals Corporation 2009-06-18 2020-02-29 US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
Categories
- ATC Codes
- L04AC08 — Canakinumab
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
Chemical Identifiers
- UNII
- 37CQ2C7X93
- CAS number
- 914613-48-2
References
- General References
- 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:19169963]
- 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. doi: 10.1056/NEJMoa0810787. [PubMed:19494217]
- External Links
- KEGG Drug
- D09315
- PubChem Substance
- 347910340
- 853491
- ChEMBL
- CHEMBL1201834
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Canakinumab
- AHFS Codes
- 92:44.00 — Immunosuppressive Agents
- FDA label
- Download (120 KB)
- MSDS
- Download (568 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Active Not Recruiting Treatment Non-Small Cell Lung Carcinoma (NSCLC) 1 3 Active Not Recruiting Treatment Non-Small-Cell Lung 1 3 Active Not Recruiting Treatment Novel Coronavirus Infectious Disease (COVID-19) / Pneumonia and Cytokine Release Syndrome (Covid-19) 1 3 Completed Treatment Acute Gouty Arthritis 4 3 Completed Treatment Acute Gouty Arthritis Flares 1 3 Completed Treatment Atherosclerosis 1 3 Completed Treatment Cryopyrin-associated Periodic Syndromes (CAPS) 1 3 Completed Treatment Cryopyrin-associated Periodic Syndromes (CAPS) / Familial Cold Autoinflammatory Syndrome (FCAS) / Muckle Wells Syndrome / Muckle-Wells Syndrome (MWS) / Neonatal-Onset Multisystem Inflammatory Disease (NOMID) 1 3 Completed Treatment Cryopyrin-associated Periodic Syndromes (CAPS) / Familial Cold Autoinflammatory Syndrome (FCAS) / Muckle-Wells Syndrome (MWS) / Neonatal-Onset Multisystem Inflammatory Disease (NOMID) 3 3 Completed Treatment Hereditary Periodic Fevers 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Subcutaneous 150 mg/ml Injection, powder, for solution 150 mg Injection, powder, for solution Cutaneous 150 MG Injection, powder, for solution Parenteral; Subcutaneous 150 MG Injection, powder, for solution Subcutaneous 150 mg Injection, powder, lyophilized, for solution Subcutaneous 150 mg/1mL Injection, solution Cutaneous; Parenteral 150 MG/ML Injection, solution Subcutaneous 150 mg/1mL Powder, for solution Subcutaneous 150 mg Solution Subcutaneous 150 mg Injection 150 mg/ml Powder - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Protein domain specific binding
- Specific Function
- Potent proinflammatory cytokine. Initially discovered as the major endogenous pyrogen, induces prostaglandin synthesis, neutrophil influx and activation, T-cell activation and cytokine production, ...
- Gene Name
- IL1B
- Uniprot ID
- P01584
- Uniprot Name
- Interleukin-1 beta
- Molecular Weight
- 30747.7 Da
References
- 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:19169963]
Drug created on March 19, 2008 10:15 / Updated on October 21, 2020 01:55
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