Anakinra

Base Information

• Chemical Name: Anakinra
• CAS No.: 143090-92-0
• Molecular Formula: C20H23N5O7S2
• Molecular Weight: 509.562
• Mol file: 143090-92-0.mol

Synonyms:26-177-Interleukin1 receptor antagonist [methionyl] (human); 2: PN:US6159460 PAGE: 27/28 claimed sequence; 2: PN: US6294170 SEQID: 2 claimedprotein; 4: PN: US6294170 SEQID: 4 unclaimed protein; Anakinra;Antril; Interleukin 1 receptor antagonist (humanclone pAMG21-IL-1ra); Interleukin 1 receptor antagonist (human precursor); Kinaret; Kineret;N2-L-Methionylinterleukin 1 receptor antagonist (human isoformx reduced)

Chemical Property of Anakinra

Chemical Property:

• PSA: 0.00000
• LogP: 0.00000

Purity/Quality:

99%, ^*data from raw suppliers

ANAKINRA 95.00% ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

Useful:

• Description: Anakinra was launched in the US as a new daily subcutaneous injection therapy 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. Anakinra, N2-L-methionylinterleukin-1 receptor antagonist (human isoform x reduced), is the first recombinant non-glycosylated human IL-1 receptor antagonist (IL-lra). It was isolated from human monocytes, cloned and expressed in Escherichia coll. IL-1ra is an endogenous cytokine that blocks the binding of the pro-inflammatory cytokine ILl to its receptor thereby balancing the cartilage destruction and bone resorption mediated by IL-1. In RA patients, the amount of endogenous IL-lra in the synovial joint is not sufficient to neutralize the detrimental effects of an excessive level of IL-1. In collageninduced arthritic mice, continuous i.p. infusion of IL-1ra suppressed the established arthritis, reduced cartilaginous destruction and restored the synthetic function in articular cartilage chondrocytes. In clinical trials with RA patients, anakinra was found to attenuate disease severity and to reduce joint destruction over 6 to 12 months. Treatment with anakinra was generally well tolerated, although skin reactions at the injection site were reported. Experiments in rat showed that subcutaneous or intradermal injection of high doses of anakinra or its vehicle caused a non-immunologically mediated cutaneous mast cell degranulation.
• Uses: Anti-inflammatory (nonsteroidal); suppressant (inflammatory bowel disease).
• 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.
• 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.
• Drug interactions: Potentially hazardous interactions with other drugs Adalimumab, certolizumab, etanercept, golimumab and infliximab: avoid concomitant use. Live vaccines: avoid concomitant use.