143090-92-0 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.
Check Digit Verification of cas no
The CAS Registry Mumber 143090-92-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,4,3,0,9 and 0 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 143090-92:
(8*1)+(7*4)+(6*3)+(5*0)+(4*9)+(3*0)+(2*9)+(1*2)=110
110 % 10 = 0
So 143090-92-0 is a valid CAS Registry Number.