Anakinra
Identification
- Summary
Anakinra is a recombinant form of human interleukin-1 receptor antagonist used in the treatment of rheumatoid arthritis and neonatal-onset multisystem inflammatory disease.
- Brand Names
- Kineret
- Generic Name
- Anakinra
- DrugBank Accession Number
- DB00026
- Background
Anakinra is a recombinant, nonglycosylated human interleukin-1 receptor antagonist (IL-1Ra). The difference between anakinra and the native human IL-1Ra is that anakinra has an extra methionine residue at the amino terminus. It is manufactured by using the E. coli expression system. Anakinra is composed of 153 amino acid residues. FDA approved on November 14, 2001.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Interleukin-based products - Protein Structure
- Protein Chemical Formula
- C759H1186N208O232S10
- Protein Average Weight
- 17257.6 Da
- Sequences
>DB00026 sequence MRPSGRKSSKMQAFRIWDVNQKTFYLRNNQLVAGYLQGPNVNLEEKIDVVPIEPHALFLG IHGGKMCLSCVKSGDETRLQLEAVNITDLSENRKQDKRFAFIRSDSGPTTSFESAACPGW FLCTAMEADQPVSLTNMPDEGVMVTKFYFQEDE
Download FASTA Format- Synonyms
- Anakinra
- IL-1RA
- Interleukin-1 receptor antagonist anakinra
Pharmacology
- Indication
For the treatment of adult rheumatoid arthritis and treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID).
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- Contraindications & Blackbox Warnings
Contraindications & Blackbox WarningsWith our commercial data, access important information on dangerous risks, contraindications, and adverse effects.Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects- Pharmacodynamics
Used to treat rheumatoid arthritis, Anakinra blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI), which is expressed in a wide variety of tissues and organs. IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic responses including inflammatory and immunological responses. Patients with rheumatoid arthritis have elevated levels of IL-1. The levels of the naturally occurring IL-1Ra in synovium and synovial fluid from rheumatoid arthritis (RA) patients are not sufficient to compete with the elevated amount of locally produced IL-1. Increasing the levels of IL-1Ra by artificial means reduces the negative effects (cartilage degradation, bone resorption) of IL-1.
- Mechanism of action
Anakinra binds competitively to the Interleukin-1 type I receptor (IL-1RI), thereby inhibiting the action of elevated levels IL-1 which normally can lead to cartilage degradation and bone resorption.
Target Actions Organism AInterleukin-1 receptor type 1 antagonistHumans - Absorption
When a 70 mg subcutaneous bolus injection is given to healthy subjects, the absolute bioavailability is 95%. Accumulation does not occur following daily subcutaneous doses. Tmax, SubQ, 1-2 mg/kg, healthy subjects = 3-7 hours; Cmax, SubQ, 3 mg/kg once daily, NOMID patients = 3628 ng/mL.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Healthy subjects = 4 - 6 hours; NOMID patients = 5.7 hours (range of 3.1 - 28.2 hours).
- Clearance
Clearance is variable and increases with increasing creatinine clearance and body weight. However, gender and age were not significant factors.
- Adverse Effects
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Most common adverse reactions (incidence ≥ 5%) are injection site reaction, worsening of rheumatoid arthritis, upper respiratory tract infection, headache, nausea, diarrhea, sinusitis, arthralgia, flu like-symptoms, and abdominal pain when anakinra is used in RA patients. In NOMID patients, the most common AEs during the first 6 months of treatment (incidence >10%) are injection site reaction, headache, vomiting, arthralgia, pyrexia, and nasopharyngitis.
- 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 Anakinra is combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Anakinra. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Anakinra. Acebutolol The metabolism of Acebutolol can be increased when combined with Anakinra. Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Anakinra. Acetaminophen The metabolism of Acetaminophen can be increased when combined with Anakinra. Acetohexamide The metabolism of Acetohexamide can be increased when combined with Anakinra. Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be increased when combined with Anakinra. Acyclovir The metabolism of Acyclovir can be increased when combined with Anakinra. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Anakinra. 
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- No interactions found.
Products
Comprehensive & structured drug product infoFrom application numbers to product codes, connect different identifiers through our commercial datasets.Easily connect various identifiers back to our datasets- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Kineret Injection, solution 100 mg/0.67ml Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2016-09-08 Not applicable EU 
Kineret Injection, solution 100 mg Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2016-09-08 Not applicable EU Kineret Injection, solution 100 mg/0.67mL Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2009-12-15 Not applicable US 
Kineret Injection, solution 100 mg/0.67ml Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2016-09-08 Not applicable EU Kineret Injection, solution 100 mg Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2016-09-08 Not applicable EU Kineret Solution 150 mg / mL Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2002-05-29 Not applicable Canada 
Kineret Injection, solution 100 mg/0.67ml Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2016-09-08 Not applicable EU Kineret Injection, solution 100 mg Subcutaneous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2016-09-08 Not applicable EU
Categories
- ATC Codes
- L04AC03 — Anakinra
- Drug Categories
- Agents reducing cytokine levels
- Amino Acids, Peptides, and Proteins
- Antineoplastic and Immunomodulating Agents
- Antirheumatic Agents
- Biological Factors
- Biologics for Rheumatoid Arthritis Treatment
- Cytokines
- Disease-modifying Antirheumatic Agents
- Immunosuppressive Agents
- Immunotherapy
- Intercellular Signaling Peptides and Proteins
- Interleukin Inhibitors
- Interleukin-1 Receptor Antagonist
- Peptides
- Proteins
- 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
- 9013DUQ28K
- CAS number
- 143090-92-0
References
- General References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Lequerre T, Quartier P, Rosellini D, Alaoui F, De Bandt M, Mejjad O, Kone-Paut I, Michel M, Dernis E, Khellaf M, Limal N, Job-Deslandre C, Fautrel B, Le Loet X, Sibilia J: Interleukin-1 receptor antagonist (anakinra) treatment in patients with systemic-onset juvenile idiopathic arthritis or adult onset Still disease: preliminary experience in France. Ann Rheum Dis. 2008 Mar;67(3):302-8. Epub 2007 Oct 18. [Article]
- External Links
- UniProt
- P18510
- Genbank
- M55646
- KEGG Drug
- D02934
- PubChem Substance
- 46507944
- 72435
- ChEMBL
- CHEMBL1201570
- Therapeutic Targets Database
- DAP000095
- PharmGKB
- PA10799
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Anakinra
- AHFS Codes
- 92:36.00 — Disease-modifying Antirheumatic Agents
- FDA label
- Download (62.3 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Idiopathic Recurrent Pericarditis 1 4 Completed Treatment Rheumatoid Arthritis 2 4 Recruiting Treatment Community-acquired Pneumonia, Influenza, COVID-19 / Coronavirus Disease 2019 (COVID‑19) 1 4 Terminated Treatment Rheumatoid Arthritis / Type 2 Diabetes Mellitus 1 4 Withdrawn Treatment Knee Injuries 1 3 Active Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 2 3 Completed Not Available Hypersecretion; Cortisol / Syndrome, Metabolic 1 3 Completed Treatment BMI >30 kg/m2 / Hypogonadism / Syndrome, Metabolic 1 3 Completed Treatment Familial Mediterranean Fever (FMF ) 1 3 Completed Treatment Rheumatoid Arthritis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Amgen Inc.
- BioVitrum AB
- Dosage Forms
Form Route Strength Injection, solution Parenteral; Subcutaneous Injection, solution Subcutaneous 100 mg Injection, solution Subcutaneous 100 mg/0.67mL Solution Subcutaneous 150 mg / mL - Prices
Unit description Cost Unit Kineret 1 Box = 7 Syringes, 4.69ml Box 449.9USD box Kineret 100 mg/0.67 ml syr 61.8USD syringe DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2141953 No 2008-04-08 2013-09-17 Canada CA1341322 No 2001-11-27 2018-11-27 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source hydrophobicity -0.412 Not Available isoelectric point 5.46 Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- Receptor for IL1A, IL1B and IL1RN. After binding to interleukin-1 associates with the corecptor IL1RAP to form the high affinity interleukin-1 receptor complex which mediates interleukin-1-dependen...
- Gene Name
- IL1R1
- Uniprot ID
- P14778
- Uniprot Name
- Interleukin-1 receptor type 1
- Molecular Weight
- 65401.91 Da
References
- Tang YH, Zhang SP, Liang Y, Deng CQ: [Effects of Panax notoginseng saponins on mRNA expressions of interleukin-1 beta, its correlative factors and cysteinyl-aspartate specific protease after cerebral ischemia-reperfusion in rats]. Zhong Xi Yi Jie He Xue Bao. 2007 May;5(3):328-32. [Article]
- Dayer JM: The pivotal role of interleukin-1 in the clinical manifestations of rheumatoid arthritis. Rheumatology (Oxford). 2003 May;42 Suppl 2:ii3-10. [Article]
- Vamvakopoulos J, Green C, Metcalfe S: Genetic control of IL-1beta bioactivity through differential regulation of the IL-1 receptor antagonist. Eur J Immunol. 2002 Oct;32(10):2988-96. [Article]
- Do H, Vasilescu A, Carpentier W, Meyer L, Diop G, Hirtzig T, Coulonges C, Labib T, Spadoni JL, Therwath A, Lathrop M, Matsuda F, Zagury JF: Exhaustive genotyping of the interleukin-1 family genes and associations with AIDS progression in a French cohort. J Infect Dis. 2006 Dec 1;194(11):1492-504. Epub 2006 Oct 26. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- So A, De Smedt T, Revaz S, Tschopp J: A pilot study of IL-1 inhibition by anakinra in acute gout. Arthritis Res Ther. 2007;9(2):R28. [Article]
- Vannier E, Kaser A, Atkins MB, Fantuzzi G, Dinarello CA, Mier JW, Tilg H: Elevated circulating levels of soluble interleukin-1 receptor type II during interleukin-2 immunotherapy. Eur Cytokine Netw. 1999 Mar;10(1):37-42. [Article]
Drug created on June 13, 2005 13:24 / Updated on June 22, 2021 09:25