Anakinra

Manufacturer Amgen Inc., Thousand Oaks, CA Indications Reduction of signs and symptoms of rheumatoid arthritis Type of submission Biologics license application A. General description Anakinra is a recombinant nonglycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra). It differs from native human IL-1Ra by the addition of a methionine residue at its amino terminus. Anakinra consists of 153 amino acids and has a molecular weight of 17.3 kDa. It is produced by recombinant DNA...

Clinical pharmacology Anakinra

Blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukine-1 type I receptor IL-1RI , which is expressed in a variety of tissues and organs. IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic and immuno-logical responses. IL-1 has a broad range of activity, including cartilage degradation, through rapid loss of proteoglycans, as well as stimulation of bone resorption. The levels of naturally occurring IL-1Ra in...

BOX 45 Modulation Of The Clearance Of Therapeutic Proteins By Addition Of Fc Domain Sequences

In the early 1970s, when recombinant proteins in large quantity first became available in pharmaceutical grade, it was recognized that most proteins less than 50kDa are readily cleared from the circulation if they are not bound to a receptor or do not contain unique amino-acid sequences that provide prolonged residence time in blood. Studies of immunoglobulin biosynthesis and metabolism mapped the important determinants of the half-life of these molecules in plasma, regardless of their antigen...