Rheumatoid arthritis anakinra

Anakinra Anakinra is likewise indicated for the treatment of patients with rheumatoid arthritis. Anakinra is the recombinant form of human IL-1 receptor antagonist (IL-lra) and is identical to the naturally occurring, nonglycosylated form of the protein, with an additional N-terminal methionine residue. Binding of IL-lra to the IL-1R1 receptor does not initiate IL-1 mediated cell signaling,... 

IL-1 receptor antagonist Anakinra A naturally occurring complete antagonist, effective in rheumatoid arthritis. 

Anakinra/Kineret, an IL-1 receptor antagonist approved for use in rheumatoid arthritis, was recently evaluated in a small phase II trial. When initiated within 6 hours after stroke onset, Anakinra treatment yielded promising preliminary results it was deemed safe with demonstrable biologic activity and likely favorable clinical outcome." ... 

Anakinra - recombinant version of human lL-1 Rheumatoid arthritis patients failing to respond... 

Kineret (anakinra rIL-1 receptor antagonist produced in E. coli) Vaccines Amgen Rheumatoid arthritis 2001 (USA)... 

Anakinra is the first biologic drug that has been developed specifically as an interleukin (IL)-l receptor antagonist and is derived from an endogenous IL-IRa. The drug blocks the activity of IL-1 in synovial joints, reducing the infiammatory and joint destructive processes associated with rheumatoid arthritis. It is administered subcutaneously and is generally well tolerated. Injection-site reactions are the most commonly reported adverse event. 

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. 

Anakinra is a nonglycosylated form of the human IL-1 receptor antagonist (IL-lra). 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-lra in the synovial fluid is not sufhcient 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. 

Pharmacokinetics The absolute bioavailability after a 70 mg subcutaneous dose of Kineret in healthy subjects is 95%. In subjects with rheumatoid arthritis, maximum plasma concentrations of anakinra occurred 3 to 7 hours after subcutaneous administration. The terminal half-life ranged from 4 to 6 hours. No unusual pharmacokinetics was observed on repeated daily dosing. 

Anakinra (Kineret) blocks the effects of interleukin-1 on joint tissues. Like TNF-a, interleukin-1 is a cytokine that promotes inflammation and joint destruction in rheumatoid arthritis.23,36 By blocking interleukin-1 receptors on joint tissues, anakinra prevents the destructive events mediated by this cytokine. This drug appears to be moderately effective in limiting the progression of rheumatoid arthritis, and it is generally well tolerated.36 Hence, anakinra is another option that can be used alone or in combination with other DMARDs such as methotrexate.23... 

Cohen SB. The use of anakinra, an interleukin-1 receptor antagonist, in the treatment of rheumatoid arthritis. Rheum Dis Clin North Am. 2004 30 365-380. 

Furst DE. Anakinra review of recombinant human interleukin-I receptor antagonist in the treatment of rheumatoid arthritis. Clin Ther. 2004 26 1960-1975. 

Anakinra is a recombinant form of an endogenous antagonist at the interleukin-1 receptor it is used in rheumatoid arthritis (p.332). 

Anakinra is an interleukin-1 receptor antagonist. It has been used to treat rheumatoid arthritis (1,2). It has been tried in graft-versus-host disease, but without success (3). According to published trial data, moderate injection site reactions were the primary adverse effect and required treatment withdrawal in under 5% of patients. An erythematous rash was seldom observed. Although a few patients have developed antibodies to anakinra, these have not so far been associated with lack of efficacy or allergic skin reactions. 

Regulatory agencies have issued an important postmarketing warning of an increased risk of serious infections and neutropenia in patients who receive concomitant anakinra and etanercept (4). This warning was based on an analysis of a randomized clinical trial in 242 patients with rheumatoid arthritis, in which 7% of patients receiving concomitant treatment had serious infections, compared with none in those treated with etanercept alone. Concurrent administration of these two drugs was therefore not recommended. 

The best-characterized receptor-binding antagonist is the IL-1 receptor antagonist (IL-IRA). IL-IRA blocks the binding of IL-1 to its receptor by competing for the same binding site, but IL-1RA does not possess agonist activity." A recombinant IL-IRA, anakinra, is used clinically for the treatment of severe rheumatoid arthritis." ... 

Cohen S, Hurd E, Cush J, et al. Treatment of rheumatoid arthritis with anakinra, a recombinant human interleukin-1 receptor antagonist, in combination with methotrexate Results of a twenty-four-week, multicenter, randomized, double-blind, placebo-controlled trial. Arthritis Rheum 2002 46 614-624. 

Inhibitors of IL-1 Anakinra inhibits the activity of IL-1. It is licensed for use in combination with methotrexate for rheumatoid arthritis that is unresponsive to methotrexate alone. Anakinra is given by sub-cutaneous injection once weekly. National... 

Anakinra is the first IL-1 Ra 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. 

Anakinra rhlT. receptor antagrmist Rheumatoid arthritis Infections, injection site reactions... 

Anakinra interleukin-1 receptor antagonist IL-1 Ra (Kineret) 17.3 - 4-6 SC (0.95) Rheumatoid arthritis ... 

In a study in patients with active rheumatoid arthritis taking etanercept and anakinra for up to 24 weeks, serious infections occurred in 7% of patients, compared with none in patients taking etanercept alone. Neutropenia occurred in 2% of patients taking both drugs. Infections are very coimnon adverse effects of treatment with etanercept but serious infections are reported to be uncoimnon (occurring in about 1% of etanercept- and placebo-treated groups in clinical studies). - Further, the combination of etanercept with anakinra has not increased clinical benefit and the manufacturers say that concurrent use is not recommended. ... 

The interleukin-l-receptor-antagonist Anakinra (Kineret ) with its sequence of 153 amino acids was patented in 1989 by the company Synergen, and later developed to the market by Amgen (Fig. 5.92). It is produced using recombinant Escherichia coli strains, and is applied as a combination product for the treatment of severe rheumatoid arthritis. [209]... 

Fleischmann RM, Tesser J, Schiff MH, et al. Safety of extended treatment with anakinra in patients with rheumatoid arthritis. Ann Rheum Dis. 2006 65 6-12. 

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