Anakinra is an interleukin-1 (IL-1) receptor antagonist and is common;y used for treatment of rheumatoid arthritis. Anakinra blocks the biologic activity of naturally occurring IL-1 by competitively inhibiting the binding of IL-1 to the Interleukin-1 type receptor.
IL-1 is produced in response to inflammatory stimuli and mediates various physiologic responses, including inflammatory and immunologic reactions. IL-1 stimulates bone resorption and induces tissue damage like cartilage degradation as a result of loss of proteoglycans.
The anakinra molecule is a recombinant, non-glycosylated version of human IL-1 receptor antagonist prepared from cultures of genetically modified Escherichia coli using recombinant DNA technology.
The drug is used as biological response modifier.
A recent study conducted trial to check the efficacy of drug {intraartcular single injection} in osteoarthritis. It concluded that single intraarticular injection of the interleukin-1 receptor antagonist anakinra for treatment of knee osteoarthritis has no effect on knee pain, function, stiffness, or cartilage turnover.
Interleukin-1 is believed to stimulate the synthesis of mediators and effectors of tissue inflammation and destruction in osteoarthritis. In preclinical studies, intraarticular anakinra was associated with reductions in the number and size of osteophytes and cartilage lesions.
In their randomized, double-blind trial conducted at 20 study centers in 3 countries, 34 patients were assigned to receive anakinra 50 mg, 67 to receive anakinra 150 mg, and 69 to receive a placebo injection. the results of the study have ben published in Arthritis and Rheumatism journal.
the patients were assesed by the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) and there was no significant difference between groups at periodic evaluations through week 12. The three groups also were similar in the amount of rescue analgesic used and in measures of cartilage degradation.
Serum anakinra levels were below the level of quantification within 24 hours after administration, an indication that there is no depot effect from intraarticular injection.
Dr. Chevalier’s who was part of the team that conducted trial suggests that a higher dose or repeated injections of anakinra, or else use of longer acting and more potent interleukin-1 antagonists, may be more effective.
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