| Primary information |
|---|
| ThPP ID | Th1023 |
| Therapeutic Peptide/Protein Name | Anakinra |
| Sequence | MRPSGRKSSKMQAFRIWDVNQKTFYLRNNQLVAGYLQGPNVNLEEKIDVV view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 17257.6 |
| Chemical Formula | C759H1186N208O232S10 |
| Isoelectric Point | 5.46 |
| Hydrophobicity | -0.412 |
| Melting Point (℃) | N.A. |
| Half Life | Healthy subjects = 4 - 6 hours |
| Description | 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. |
| Indication/Disease | To treat adult rheumatoid arthritis and Neonatal-Onset Multisystem Inflammatory Disease (NOMID). |
| Pharmacodynamics | 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. |
| 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 |
| Metabolism | N.A. |
| 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 dail |
| Volume of Distribution | N.A. |
| Clearance | Clearance is variable and increases with increasing creatinine clearance and body weight. |
| Categories | Antirheumatic Agents |
| Patents Number | CA2141953 |
| Date of Issue | 08/04/08 |
| Date of Expiry | 17/09/13 |
| Drug Interaction | Canakinumab results in increased immunosuppressive effects; increases the risk of infection. |
| Target | Interleukin-1 receptor type 1 |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Kineret |
| Company | Amgen Inc |
| Brand Discription | Kineret is a recombinant, nonglycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra). Kineret differs from native human IL-1Ra in that it has the addition of a single methionine residue at its amino terminus. Kineret consists of 153 amin |
| Prescribed for | To treat the symptoms of moderate to severe rheumatoid arthritis in adults. Anakinra may also help slow the progress of the disease. |
| Chemical Name | N.A. |
| Formulation | The solution may contain trace amounts of small, translucent-to-white amorphous proteinaceous particles. Each prefilled glass syringe contains: 0.67 mL (100 mg) of anakinra in a solution (pH 6.5) containing disodium EDTA (0.12 mg), sodium chloride (5.48 m |
| Physcial Appearnce | Sterile, clear, colorless-to-white, preservative free solution |
| Route of Administration | Subcutaneous (Subcutaneous) administration |
| Recommended Dosage | 100 mg/day administered daily |
| Contraindication | Contraindicated in patients with known hypersensitivity to E coli-derived proteins, Kineret, or any components of the product |
| Side Effects | Nausea, diarrhea, stomach pain; headache; cold symptoms such as stuffy nose, sneezing, sore throat; or redness, bruising, pain, or swelling where the injection was given. |
| Useful Link | http://www.rxlist.com/kineret-drug.htm |
| PubMed ID | 17947302, 18251718, 23553601, 23319019, 19169963 |
| 3-D Structure | Th1023 (View) or (Download) |