Kineret Anakinra

Kineret is a human IL-1 receptor antagonist and is produced by recombinant DNA technology. It is nonglycosylated and is made up of 153 amino acids. With the exception of an additional methionine residue, it is similar to native human IL-lRa. Human IL-lRa is a naturally occurring IL-1 receptor antagonist, a 17-kDa protein, which competes with IL-1 for receptor binding and blocks the activity of IL-1. 

The most serious side effects of Kineret are infections and neutropenia. Injection site reactions are also common. Other side effects may include headache, nausea, diarrhea, flu-like symptoms and abdominal pain. The increased risk of malignancies has also been observed. 

The IL-2 receptor occurs in three forms with different affinities for IL-2 the three distinct subunits are the a, (3 and y chains. The monomeric IL-2Ra possesses low affinity, the dimeric IL-2R(3y has intermediate affinity and the trimeric IL-2R (3y has high affinity (Table 2.2). The a chain is not expressed on resting T cells but 

When IL-2 binds to high-affinity receptors, it becomes internalized following receptor-mediated endocytosis. After high-affinity binding, there is an increase in the stimulation of phosphoinositol turnover, redistribution of protein kinase C from the cytoplasm to the cell membrane, and an increased expression of IL-2 receptors, with low-affinity receptors being preferentially increased. 

---

Kepivance, Palifermin, KSA-2 Kineret , Anakinra IL-IRa Amgen, Inc Amgen, Inc... 

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

KINERET (Anakinra) [E. coli expressed recombinant, Amgen Liquid 100 mg prefilled single dose syringe 100 mg per 0.67 mL (pH 6.5) Per Syringe 1.29 mg sodium citrate 5.48 mg sodium chloride 0.12 mg disodium EDTA... 

Recombinant human DL-1 receptor antagonist (Anakinra, Kineret ) blocks the biological activity of interleukin-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. Thereby it reduces the pro-inflammatory activities of IL-1 including cartilage destiuction and bone resorption. Side effects include an increased risk of infections and neutropenia. 

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 (Kineret) 100-150 mg daily SC injection 2-4 weeks HA, N, V, D, ISR Monitor for infection ... 

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. 

Dosage form Kineret is supplied in single-use, 1 ml prefilled glass syringes with needles. Each prefilled syringe contains anakinra 100 mg. 

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. 

Interferons and cytokines Anakinra, human IL-lRa Kineret 1 ml in solution vial -100 mg anakinra SC... 

Abatacept (Orencia) Aclalimumab (Humira) Anakinra (Kineret)... 

Anakinra (Kineret) Gold sodium thiomalate (Myochrysine)... 

Drug Anakinra Trade Name Kineret Usual Dosage Subcutaneous injection 100 mg/d. Special Considerations Can be used alone or with other antiarthritic agents, but should not be used with tumor necrosis factor inhibitors. 

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... 

FDA Pharmacology/Toxicology review (anakinra) Kineret. http //www.fda.gov/ cder/foi/nda/2001/103950-0 Kineret Pharmr.PDF12... 

USA anakinra protein Kineret Antril A recombinant non-glycosylated human lL-1 receptor antagonist isolated from monocytes and expressed in E. coli Anti-arthritic... 

---