| Primary information |
|---|
| ThPP ID | Th1005 |
| Therapeutic Peptide/Protein Name | Etanercept |
| Sequence | LPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSD view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 51234.9 |
| Chemical Formula | C2224H3475N621O698S36 |
| Isoelectric Point | 7.89 |
| Hydrophobicity | -0.529 |
| Melting Point (℃) | 71 |
| Half Life | 102 ± 30 hrs |
| Description | It is a dimeric fusion protein (934 amino acids) consisting of extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to Fc portion of human IgG1 produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system.. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. |
| Indication/Disease | Used to treat severe rheumatoid arthritis in adults, severe juvenile idiopathic arthritis, ankylosing spondylitis, and severe plaque psoriasis. |
| Pharmacodynamics | TNF, a naturally occurring cytokine is involved in normal inflammatory and immune responses. Elevated levels of TNF are found in tissues and fluids of patients suffering from rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis (AS), and plaque psoriasis. Etanercept binds specifically to tumor necrosis factor (TNF) and blocks its interaction with cell surface TNF receptors. |
| Mechanism of Action | There are two distinct receptors for TNF (TNFRs), a 55 kilodalton (p55) and a 75 kilodalton receptor (p75). The biological activity of TNF is dependent upon binding to either of the cell surface receptors p75 or p55. Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | 160 ± 80 mL/hr [RA patients] |
| Categories | Immunosuppressive Agents |
| Patents Number | CA2476934 |
| Date of Issue | 16/06/09 |
| Date of Expiry | 27/02/23 |
| Drug Interaction | Rilonacept results in increased immunosuppressive effects; increases the risk of infection. |
| Target | Tumor necrosis factor,Tumor necrosis factor receptor superfamily member 1B,Low affinity immunoglobulin gamma Fc region receptor II-b,Low affinity immunoglobulin gamma Fc region receptor II-c,Lymphotoxin-alpha,Low affinity immunoglobulin gamma Fc region re |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Enbrel |
| Company | Immunex Corp |
| Brand Discription | Enbrel is a 934 amino acid fusion protein (dimeric) weighing approximately 150 kilodaltons and containing the extracellular ligand-binding part of the human 75 kilodalton (p75) tumor necrosis factor receptor linked to the Fc part of human IgG1. The Fc com |
| Prescribed for | Used to treat rheumatoid arthritis, psoriatic arthritis, or ankylosing spondylitis, and prevent joint damage caused by these conditions. Enbrel is also used to treat plaque psoriasis in adults and polyarticular juvenile idiopathic arthritis (in children a |
| Chemical Name | N.A. |
| Formulation | Supplied in a multiple-use vial as a sterile, white, preservative-free, lyophilized powder. Reconstitution with 1 mL of the supplied Sterile Bacteriostatic Water for Injection, USP (containing 0.9% benzyl alcohol) yields a multiple-use, clear, and colorle |
| Physcial Appearnce | Lyophilized powder. |
| Route of Administration | Subcutaneous Injection |
| Recommended Dosage | N.A. |
| Contraindication | N.A. |
| Side Effects | Signs of infection (fever, chills, sore throat, body aches, confusion, neck stiffness, flu symptoms); shortness of breath with swelling, rapid weight gain; chest pain, ongoing cough, coughing up mucus or blood; signs of skin infection such as itching, sw |
| Useful Link | http://www.genome.jp/dbget-bin/www_bget/D00742 |
| PubMed ID | 20080922, 25651776, 23620660, 16713481 |
| 3-D Structure | Th1005 (View) or (Download) |