Interleukin-1 Receptor Antagonist (IL-1Ra) is a naturally occurring protein that plays a crucial role in regulating the immune response by inhibiting the activity of interleukin-1 (IL-1). IL-1 is a pro-inflammatory cytokine involved in various inflammatory and autoimmune conditions. Recombinant forms of IL-1Ra, including those derived from rats, have been developed for research and therapeutic purposes.
IL-1Ra was first discovered in 1984 in the urine and serum of patients with leukemia and in the supernatant of cultured monocytes . The protein was named for its ability to competitively bind to the IL-1 receptor, thereby antagonizing the effects of IL-1. This discovery paved the way for the development of recombinant forms of IL-1Ra for clinical and research applications.
IL-1Ra functions by binding to the IL-1 receptor without eliciting a signal, effectively blocking the binding of IL-1 and preventing its pro-inflammatory effects. This mechanism is crucial in controlling the inflammatory response and has therapeutic implications for various inflammatory diseases.
Recombinant IL-1Ra, such as anakinra (Kineret™), has been approved for clinical use in the treatment of rheumatoid arthritis (RA) and other inflammatory conditions . Anakinra is a recombinant form of human IL-1Ra that differs from the native protein by the addition of an N-terminal methionine . It is administered daily by subcutaneous injection and has shown efficacy in reducing the signs and symptoms of RA .
Rat recombinant IL-1Ra is widely used in preclinical research to study the role of IL-1 in various disease models. It helps in understanding the pathophysiology of inflammatory diseases and in developing new therapeutic strategies. Studies have demonstrated the efficacy of IL-1Ra in animal models of arthritis, providing insights into its potential therapeutic benefits .
Clinical trials have shown that anakinra is relatively safe and modestly efficacious in treating RA . However, it is associated with an increased incidence of injection site reactions and serious infections . More studies are needed to evaluate the long-term safety and efficacy of IL-1Ra, especially in comparison to other biologic therapies.