Anakinra

Identification

Name

Anakinra

Accession Number

DB00026

Description

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).

Associated Conditions

• Juvenile Idiopathic Arthritis (JIA)
• Neonatal-Onset Multisystem Inflammatory Disease (NOMID)
• Moderate Rheumatoid arthritis
• Recurrent Pericarditis
• Severe Rheumatoid arthritis

Contraindications & Blackbox Warnings

Learn about our commercial Contraindications & Blackbox Warnings data.

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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

Learn about our commercial Adverse Effects data.

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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.

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.

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• Withdrawn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

Drug	Interaction
Unlock Additional Data
Abatacept	The risk or severity of adverse effects can be increased when Anakinra is combined with Abatacept.
Abiraterone	The metabolism of Abiraterone 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.

Additional Data Available

Extended Description
Extended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
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Severity
Severity
A severity rating for each drug interaction, from minor to major.
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Evidence Level
Evidence Level
A rating for the strength of the evidence supporting each drug interaction.
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Action
Action
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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Food Interactions

Not Available

Products

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Unlock Additional Data
Kineret	Injection, solution	100 mg/0.67ml	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-03-08	Not applicable
Kineret	Injection, solution	100 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-03-08	Not applicable
Kineret	Injection, solution	100 mg/0.67ml	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-03-08	Not applicable
Kineret	Injection, solution	100 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-03-08	Not applicable
Kineret	Solution	150 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-05-29	Not applicable
Kineret	Injection, solution	100 mg/0.67ml	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-03-08	Not applicable
Kineret	Injection, solution	100 mg	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2002-03-08	Not applicable
Kineret	Injection, solution	100 mg/0.67mL	Subcutaneous	SWEDISH ORPHAN BIOVITRUM AB (PUBL)	2009-12-15	Not applicable

Additional Data Available

Application Number
Application Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
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Product Code
Product Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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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
• 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

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. [PubMed:11752352]
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. [PubMed:17947302]

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

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 / Novel Coronavirus Infectious Disease (COVID-19)	1
4	Terminated	Treatment	Rheumatoid Arthritis / Type 2 Diabetes Mellitus	1
4	Withdrawn	Treatment	Knee Injuries	1
3	Completed	Not Available	Hypersecretion; Cortisol / Metabolic Syndromes	1
3	Completed	Treatment	BMI >30 kg/m2 / Hypogonadism / Metabolic Syndromes	1
3	Completed	Treatment	Familial Mediterranean Fever (FMF )	1
3	Completed	Treatment	Rheumatoid Arthritis	1
3	Completed	Treatment	ST Segment Elevation Acute Myocardial Infarction	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

• Amgen Inc.
• BioVitrum AB

Dosage Forms

Form	Route	Strength
Injection, solution	Cutaneous; Parenteral	100 MG/0.67ML
Injection, solution	Parenteral; Subcutaneous	100 MG/0.67ML
Injection, solution	Subcutaneous	100 mg
Injection, solution	Subcutaneous	100 mg/0.67ml
Solution	Subcutaneous	150 mg

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

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Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
Unlock Additional Data
CA2141953	No	2008-04-08	2013-09-17
CA1341322	No	2001-11-27	2018-11-27

Additional Data Available

Filed On
Filed On
The date on which a patent was filed with the relevant government.
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Properties

State

Liquid

Experimental Properties

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

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Drug created on June 13, 2005 07:24 / Updated on October 27, 2020 11:13