Identification
- Summary
Canakinumab is an interleukin-1β blocker used to treat Periodic Fever Syndromes such as Cryopyrin-Associated Periodic Syndromes (CAPS) and Familial Mediterranean Fever (FMF), and also to treat active Systemic Juvenile Idiopathic Arthritis (SJIA).
- Brand Names
- Ilaris
- Generic Name
- Canakinumab
- DrugBank Accession Number
- DB06168
- Background
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
>pdb|5BVP|L Chain L, Canakinumab Fab light-chain EIVLTQSPDFQSVTPKEKVTITCRASQSIGSSLHWYQQKPDQSPKLLIKYASQSFSGVPS RFSGSGSGTDFTLTINSLEAEDAAAYYCHQSSSLPFTFGPGTKVDIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- Canakinumab
- 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).
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Adult Onset Still's Disease
- Cryopyrin-associated Periodic Syndromes (CAPS)
- Familial Cold Autoinflammatory Syndrome (FCAS)
- Familial Mediterranean Fever (FMF )
- Mevalonate Kinase Deficiency
- Muckle-Wells Syndrome (MWS)
- Neonatal-Onset Multisystem Inflammatory Disease (NOMID)
- Systemic Juvenile Idiopathic Arthritis (SJIA)
- Tumour necrosis factor receptor-associated periodic syndrome
- Active systemic Juvenile idiopathic arthritis
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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.
- 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 Integrate drug-drug
interactions in your softwareAbatacept 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. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Canakinumab. Abrocitinib The metabolism of Abrocitinib 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. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ilaris Injection, powder, for solution 150 mg Subcutaneous Novartis Europharm Limited 2016-09-08 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 2016-09-08 2019-06-21 EU Ilaris Solution 150 mg / mL 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 Ilaris Injection, powder, for solution 150 mg Subcutaneous Novartis Europharm Limited 2016-09-08 Not applicable EU Ilaris Powder, for solution 150 mg / vial Subcutaneous Novartis 2010-04-27 2020-01-13 Canada Ilaris Injection, solution 150 mg/ml Subcutaneous Novartis Europharm Limited 2020-12-16 Not applicable EU
Categories
- ATC Codes
- L04AC08 — Canakinumab
- Drug Categories
- Agents reducing cytokine levels
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antineoplastic and Immunomodulating Agents
- Blood Proteins
- Globulins
- Immunoglobulins
- Immunoproteins
- Immunosuppressive Agents
- Interleukin Inhibitors
- Interleukin-1beta, antagonists & inhibitors
- Proteins
- Serum Globulins
- 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
- Affected organisms
- Humans and other mammals
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. [Article]
- 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. [Article]
- External Links
- KEGG Drug
- D09315
- PubChem Substance
- 347910340
- 853491
- ChEMBL
- CHEMBL1201834
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Canakinumab
- FDA label
- Download (120 KB)
- MSDS
- Download (568 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Prevention Coronavirus Disease 2019 (COVID‑19) / Psoriatic Arthritis / Rheumatoid Arthritis / Spondylarthritis 1 3 Active Not Recruiting Treatment Non-Small Cell Lung Carcinoma (NSCLC) 2 3 Completed Treatment Acute Gouty Arthritis 4 3 Completed Treatment Acute Gouty Arthritis Flares 1 3 Completed Treatment Atherosclerosis 1 3 Completed Treatment Coronavirus Disease 2019 (COVID‑19) / Cytokine Release Syndrome (CRS) in Patients With COVID-19-induced Pneumonia 1 3 Completed Treatment Coronavirus Disease 2019 (COVID‑19) / Infections, Coronavirus / Type 2 Diabetes Mellitus 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 (MWS) / Neonatal-Onset Multisystem Inflammatory Disease (NOMID) 4 3 Completed Treatment Hereditary Periodic Fevers 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Subcutaneous 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 Parenteral; Subcutaneous 150 MG/ML Injection, solution Subcutaneous 150 mg/ml Injection, solution Subcutaneous 150 mg/1mL Powder, for solution Subcutaneous 150 mg / vial Solution Subcutaneous 150 mg / mL Injection, solution Subcutaneous Injection, powder, for solution 150 MG Powder, for solution Subcutaneous 150 mg Solution Subcutaneous 150 mg - 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. [Article]
Drug created at March 19, 2008 16:15 / Updated at June 27, 2022 14:55