143090-92-0

Basic information

• Product Name: Anakinra
• Synonyms: Anakinra;Kineret;Unii-9013duq28k;Interleukin1 receptor antagonist (huMan isoforM x reduced),N2-L-Methionyl- (9CI);human interleukin-1 receptor antagonist (IL-1Ra);Anakinra/Interleukin1 receptor antagonist
• CAS NO: 143090-92-0
• Molecular Formula: C20H23N5O7S2
• Molecular Weight: 509.562
• Mol File: 143090-92-0.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Anakinra(CAS DataBase Reference)
• NIST Chemistry Reference: Anakinra(143090-92-0)
• EPA Substance Registry System: Anakinra(143090-92-0)

Safety Data

• Hazardous Substances Data: 143090-92-0(Hazardous Substances Data)

Usage

Description

Anakinra, also known as N2-L-methionylinterleukin-1 receptor antagonist (human isoform x reduced), is a recombinant non-glycosylated human interleukin-1 receptor antagonist (IL-1ra). It is derived from human monocytes, cloned, and expressed in Escherichia coli. Anakinra functions by blocking the binding of the pro-inflammatory cytokine IL-1 to its receptor, thus balancing the cartilage destruction and bone resorption mediated by IL-1.

Uses

Used in Anti-inflammatory Applications:
Anakinra is used as an anti-inflammatory agent, particularly for the reduction of signs and symptoms of moderately to severely active rheumatoid arthritis (RA) in adults who have failed to respond to one or more disease-modifying antirheumatic drugs.
Used in Inflammatory Bowel Disease:
Anakinra is also used as a suppressant for inflammatory bowel disease, helping to manage the symptoms and reduce the severity of the condition.
Used in Pharmaceutical Industry:
Anakinra is used as a therapeutic agent in the pharmaceutical industry for the treatment of autoimmune and inflammatory conditions, such as rheumatoid arthritis and inflammatory bowel disease. Its ability to block the pro-inflammatory cytokine IL-1 makes it a valuable asset in managing these conditions and improving the quality of life for patients.

Originator

Amgen/University of Colorado (US)

Indications

Anakinra (Kineret) is the first antirheumatic agent that acts by blocking the action of IL-1. This drug was recently approved for the treatment of moderately to severely active rheumatoid arthritis in adults who have not responded to therapy with one or more DMARDs. Anakinra may be used alone or in combination with DMARDs other than the TNF antagonists. Clinical trials have shown anakinra to be more effective than placebo, either alone or in conjunction with methotrexate.

Biological Functions

IL-1Rα plays an important role for regulating synovial proinflammatory IL-1 activity by preventing IL-1 from binding to IL-1R1. Analysis of synovial fluid suggests that the rheumatoid synovium is characterized by an overexpression of IL-1. The resulting imbalance between IL-1 and IL-1Rα has been implicated in perpetuating the pro-inflammatory response and destructive tide of events in rheumatoid arthritis. If IL-1 is prevented from binding to IL-1R1, the inflammatory response decreases. The levels of the naturally occurring IL-lRα in synovium and synovial fluid from rheumatoid arthritis patients are insufficient to compete with the elevated amount of locally produced IL-1.

Pharmacology

Anakinra is a nonglycosylated form of the human IL-1 receptor antagonist (IL-1ra). It is produced in a recombinant Escherichia coli expression system and has an additional methionine residue at its amino terminus. In rheumatoid arthritis patients, the amount of naturally occurring IL-1ra in the synovial fluid is not sufficient to counteract the high levels of locally produced IL-1. Anakinra acts as a competitive antagonist of the type 1 IL-1 receptor and decreases the pain and inflammation produced by IL-1. It is administered as a daily subcutaneous injection.

Clinical Use

Anakinra is the first IL-1Rα to be approved for use in adults with moderate to severe active rheumatoid arthritis who have not responded adequately to conventional DMARD therapy. It may be used either alone or in combination with methotrexate. Anakinra is supplied in single-use, prefilled, glass syringes as sterile, clear, preservative-free solution that is administered daily as a self-administered subcutaneous injection under the skin. Some potential side effects include injection site reactions, decreased white blood cell counts, headache, and an increase in upper respiratory infections. There may be a slightly higher rate of respiratory infections in people who have asthma or chronic obstructive pulmonary disease. Persons with an active infection are advised not to use anakinra. Its elimination half-life after sc administration is 4 to 6 hours.

Side effects

The most common adverse reactions to anakinra are redness, bruising, pain, and inflammation at the injection site. Neutropenia may occur, and the risk of serious infection is somewhat elevated, particularly in asthmatic patients.Antibodies to anakinra can develop with long-term therapy, but no correlation between antibody development and clinical response or adverse effects has been observed.

Drug interactions

Potentially hazardous interactions with other drugs Adalimumab, certolizumab, etanercept, golimumab and infliximab: avoid concomitant use. Live vaccines: avoid concomitant use.

Metabolism

Renally metabolised and excreted.

Precautions

No drug interaction studies have been conducted in humans.Animal studies indicate no change in the clearanceor toxicity of either methotrexate or anakinrawhen the two agents are administered together. Concomitantadministration of a TNF blocker appears toincrease the risk of serious infection. The response tovaccines may be diminished in patients taking anakinra.