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 for the treatment of rheumatoid arthritis.

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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Associated Conditions

• Deficiency of the interleukin-1 receptor antagonist
• Idiopathic Recurrent Pericarditis
• Moderately to Severely Active Rheumatoid Arthritis
• Neonatal-Onset Multisystem Inflammatory Disease (NOMID)
• Systemic Juvenile Idiopathic Arthritis (SJIA)

Contraindications & Blackbox Warnings

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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.

Target	Actions	Organism
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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abatacept	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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Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Kineret	Solution	150 mg / mL	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-05-29	Not applicable
Kineret	Injection, solution	100 mg/0.67ml	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2016-09-08	Not applicable
Kineret	Injection, solution	100 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2016-09-08	Not applicable
Kineret	Injection, solution	100 mg/0.67mL	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2009-12-15	Not applicable
Kineret	Injection, solution	100 mg/0.67ml	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2016-09-08	Not applicable
Kineret	Injection, solution	100 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2016-09-08	Not applicable
Kineret	Injection, solution	100 mg/0.67ml	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2016-09-08	Not applicable
Kineret	Injection, solution	100 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2016-09-08	Not applicable

Categories

ATC Codes

L04AC03 — Anakinra

• L04AC — Interleukin inhibitors
• L04A — IMMUNOSUPPRESSANTS
• L04 — IMMUNOSUPPRESSANTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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

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]
3. FDA Approved Drug Products: KINERET (anakinra) injection [Link]

External Links

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

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	Terminated	Treatment	Rheumatoid Arthritis / Type 2 Diabetes Mellitus	1
4	Withdrawn	Treatment	Injuries:Knee Injuries	1
3	Active Not Recruiting	Treatment	Coronavirus Disease 2019 (COVID‑19)	1
3	Active Not Recruiting	Treatment	Coronavirus Disease 2019 (COVID‑19) / Cytokine Storm	1
3	Completed	Not Available	Hypersecretion; Cortisol / Syndrome, Metabolic	1
3	Completed	Treatment	Acute Myocardial Infarction With ST Segment Elevation	1
3	Completed	Treatment	Coronavirus Disease 2019 (COVID‑19)	1
3	Completed	Treatment	Familial Mediterranean Fever (FMF )	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

• Amgen Inc.
• BioVitrum AB

Dosage Forms

Form	Route	Strength
Injection, solution	Parenteral; Subcutaneous	100 MG/0.67ML
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
CA1341322	No	2001-11-27	2018-11-27

Properties

State

Liquid

Experimental Properties

Property	Value	Source
hydrophobicity	-0.412	Not Available
isoelectric point	5.46	Not Available

Targets

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Details1. Interleukin-1 receptor type 1

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]

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Drug created at June 13, 2005 13:24 / Updated at January 19, 2022 01:13