|Accession Number||DB00026 (BIOD00060, BTD00060) |
Anakinra is a recombinant, nonglycosylated human interleukin-1 receptor antagonist (IL-1Ra). The difference between anakinra and the native human IL-1Ra is that anakinra has an extra methionine residue at the amino terminus. It is manufactured by using the E. coli expression system. Anakinra is composed of 153 amino acid residues. FDA approved on November 14, 2001.
|Protein chemical formula||C759H1186N208O232S10|
|Protein average weight||17257.6000|
FLCTAMEADQPVSLTNMPDEGVMVTKFYFQEDEDownload FASTA Format
|ICIL-1RA||Not Available||Not Available|
|IL-1ra||Not Available||Not Available|
|IL-1RN||Not Available||Not Available|
|IL1 inhibitor||Not Available||Not Available|
|Interleukin-1 receptor antagonist protein precursor||Not Available||Not Available|
|IRAP||Not Available||Not Available|
|Name||Dosage||Strength||Route||Labeller||Marketing Start||Marketing End|
|Kineret||injection, solution||100 mg/.67mL||subcutaneous||SWEDISH ORPHAN BIOVITRUM AB (PUBL)||2009-12-15||Not Available|
|Kineret||solution||150 mg||subcutaneous||SWEDISH ORPHAN BIOVITRUM AB (PUBL)||Not Available||Not Available|
|Generic Prescription Products||Not Available|
|Over the Counter Products||Not Available|
|International Brands||Not Available|
|Brand mixtures||Not Available|
|Super Class||Organic Acids|
|Class||Carboxylic Acids and Derivatives|
|Sub Class||Amino Acids, Peptides, and Analogues|
|Alternative Parents||Not Available|
|Molecular Framework||Not Available|
|External Descriptors||Not Available|
|Indication||For the treatment of adult rheumatoid arthritis and treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID). |
|Pharmacodynamics||Used to treat rheumatoid arthritis, Anakinra 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. 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||Anakinra binds competitively to the Interleukin-1 type I receptor (IL-1RI), thereby inhibiting the action of elevated levels IL-1 which normally can lead to cartilage degradation and bone resorption.|
|Absorption||When a 70 mg subcutaneous bolus injection is given to healthy subjects, the absolute bioavailability is 95%. Accumulation does not occur following daily subcutaneous doses.
Tmax, SubQ, 1-2 mg/kg, healthy subjects = 3-7 hours;
Cmax, SubQ, 3 mg/kg once daily, NOMID patients = 3628 ng/mL.
|Volume of distribution||Not Available|
|Protein binding||Not Available|
|Route of elimination||Not Available|
|Half life||Healthy subjects = 4 - 6 hours;
NOMID patients = 5.7 hours (range of 3.1 - 28.2 hours). |
Clearance is variable and increases with increasing creatinine clearance and body weight. However, gender and age were not significant factors.
|Toxicity||Most common adverse reactions (incidence ≥ 5%) are injection site reaction, worsening of rheumatoid arthritis, upper respiratory tract infection, headache, nausea, diarrhea, sinusitis, arthralgia, flu like-symptoms, and abdominal pain when anakinra is used in RA patients. In NOMID patients, the most common AEs during the first 6 months of treatment (incidence >10%) are injection site reaction, headache, vomiting, arthralgia, pyrexia, and nasopharyngitis. |
|SNP Mediated Effects||Not Available|
|SNP Mediated Adverse Drug Reactions||Not Available|
|Injection, solution||subcutaneous||100 mg/.67mL|
|Kineret 1 Box = 7 Syringes, 4.69ml Box||449.9USD ||box|
|Kineret 100 mg/0.67 ml syr||61.8USD ||syringe|
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
|Country||Patent Number||Approved||Expires (estimated)|
|isoelectric point||5.46||Not Available|
|Synthesis Reference||Not Available|
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
- Lequerré T, Quartier P, Rosellini D, Alaoui F, De Bandt M, Mejjad O, Kone-Paut I, Michel M, Dernis E, Khellaf M, Limal N, Job-Deslandre C, Fautrel B, Le Loët X, Sibilia J; Société Francophone pour la Rhumatologie et les Maladies Inflammatoires en Pédiatrie (SOFREMIP); Club Rhumatismes et Inflammation (CRI): Interleukin-1 receptor antagonist (anakinra) treatment in patients with systemic-onset juvenile idiopathic arthritis or adult onset Still disease: preliminary experience in France. Ann Rheum Dis. 2008 Mar;67(3):281-2.
- FDA label
|FDA label||Download (62.3 KB) |
|Abatacept||Avoid combination due to enhanced adverse effects of abatacept|
|Canakinumab||results in increased immunosuppressive effects; increases the risk of infection. |
|Certolizumab pegol||Co-administration with other TNF-blocking agents may increase the risk of serious infections. Concomitant therapy is not recommended. |
|Etanercept||Avoid combination due to increased adverse effects of anakinra and increased risk of infections.|
|golimumab||Avoid combination with anakinra due to the increased chance of serious infection.
|Infliximab||Combination may enhance the toxic effect of Anakinra and should be avoided otherwise there may be an increased risk of infection|
|Rilonacept||results in increased immunosuppressive effects; increases the risk of infection. |
|Thalidomide||Thalidomide may increase the adverse effects of Anakinra. Increased risk of serious infection. Concomitant therapy should be avoided. |
|Tofacitinib||Avoid combination due to the potential increase in tofacitinib related adverse effects.
|Trastuzumab||Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
|Food Interactions||Not Available|