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
Db00026
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).

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
AInterleukin-1 receptor type 1
antagonist
Humans
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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Toxicity

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.
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Anakinra is combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Anakinra.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Anakinra.
AcebutololThe metabolism of Acebutolol can be increased when combined with Anakinra.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Anakinra.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Anakinra.
AcetohexamideThe metabolism of Acetohexamide can be increased when combined with Anakinra.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be increased when combined with Anakinra.
AcyclovirThe metabolism of Acyclovir can be increased when combined with Anakinra.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Anakinra.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
KineretInjection, solutionSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2016-09-08Not applicableEU flag
KineretInjection, solutionSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2016-09-08Not applicableEU flag
KineretSolution150 mgSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2002-05-29Not applicableCanada flag
KineretInjection, solutionSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2016-09-08Not applicableEU flag
KineretInjection, solutionSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2016-09-08Not applicableEU flag
KineretInjection, solutionSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2016-09-08Not applicableEU flag
KineretInjection, solutionSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2016-09-08Not applicableEU flag
KineretInjection, solution100 mg/0.67mLSubcutaneousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2009-12-15Not applicableUS flag

Categories

ATC Codes
L04AC03 — Anakinra
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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
9013DUQ28K
CAS number
143090-92-0

References

General References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. 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]
UniProt
P18510
Genbank
M55646
KEGG Drug
D02934
PubChem Substance
46507944
RxNav
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
PhaseStatusPurposeConditionsCount
4CompletedTreatmentIdiopathic Recurrent Pericarditis1
4CompletedTreatmentRheumatoid Arthritis2
4RecruitingTreatmentCommunity-acquired Pneumonia, Influenza, COVID-19 / Coronavirus Disease 2019 (COVID‑19)1
4TerminatedTreatmentRheumatoid Arthritis / Type 2 Diabetes Mellitus1
4WithdrawnTreatmentKnee Injuries1
3Active Not RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)2
3CompletedNot AvailableHypersecretion; Cortisol / Syndrome, Metabolic1
3CompletedTreatmentBMI >30 kg/m2 / Hypogonadism / Syndrome, Metabolic1
3CompletedTreatmentFamilial Mediterranean Fever (FMF )1
3CompletedTreatmentRheumatoid Arthritis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amgen Inc.
  • BioVitrum AB
Dosage Forms
FormRouteStrength
Injection, solutionParenteral; Subcutaneous
Injection, solutionSubcutaneous
Injection, solutionSubcutaneous100 mg/0.67mL
SolutionSubcutaneous150 mg
Prices
Unit descriptionCostUnit
Kineret 1 Box = 7 Syringes, 4.69ml Box449.9USD box
Kineret 100 mg/0.67 ml syr61.8USD syringe
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2141953No2008-04-082013-09-17Canada flag
CA1341322No2001-11-272018-11-27Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.412Not Available
isoelectric point5.46Not Available

Targets

Drugtargets
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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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  6. 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]
  7. 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 May 10, 2021 04:40