Brands, Medical Use, Clinical Data
- Antirheumatic Agents
- Immunomodulatory Agents
Brands / Synonyms
ICIL-1RA; IL-1ra; IL-1RN; IL1 inhibitor; Interleukin-1 receptor antagonist protein precursor; IRAP; Kineret; Kineret (Amgen Inc)
Recombinant human interleukin-1 receptor antagonist. Has an extra Met at N-terminus, expressed in E. coli. 153 residues, MW=17.3 kD
For treatment of adult rheumatoid arthritis
Used to treat rheumatoid arthritis, Kineret blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI), which is expressed in a wide variety of tissues and organs.1 IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic responses including inflammatory and immunological responses. Patients with rheumatoid arthritis have elevated levels of IL-1. The levels of the naturally occurring IL-1Ra in synovium and synovial fluid from rheumatoid arthritis (RA) patients are not sufficient to compete with the elevated amount of locally produced IL-1. Increasing the levels of IL-1Ra by artificial means reduces the negative effects (cartilage degradation, bone resorption) of IL-1.
Mechanism of Action
Kineret binds to the Interleukin-1 type I receptor (IL-1RI), thereby inhibiting the action of elevated levels IL-1 leading to cartilage degradation and bone resorption.
Biotrnasformation / Drug Metabolism