Repositioning Candidate Details
| Candidate ID: | R0003 |
| Source ID: | DB00005 |
| Source Type: | approved; investigational |
| Compound Type: | biotech |
| Compound Name: | Etanercept |
| Synonyms: | Etanercept; etanercept-szzs; etanercept-ykro; Recombinant human TNF; rhu TNFR:Fc; rhu-TNFR:Fc; TNFR-Immunoadhesin |
| Molecular Formula: | -- |
| SMILES: | -- |
| DrugBank Description: | Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids. It is used to treat or manage a variety of inflammatory conditions including rheumatoid arthritis (RA), ankylosing spondylitis (AS), and juvenile idiopathic poly-articular arthritis (JIA). |
| CAS Number: | 185243-69-0 |
| Molecular Weight: | |
| DrugBank Indication: | Etanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and in chronic moderate to severe plaque psoriasis in patients 4 years of age and older. It is also used to manage signs and symptoms of polyarticular idiopathic arthritis in those aged 2 years and older. Etanercept is also used to manage the symptoms of psoriatic arthritis and ankylosing spondylitis. |
| DrugBank Pharmacology: | Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF. Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinases. |
| DrugBank MoA: | There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (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. Notably, etancerpt is only capable of binding to the active trimeric form of TNF as its binding site is located in the cleft between subunits.TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Increased levels of TNF are found in tissues and fluids of those with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and plaque psoriasis. |
| Targets: | Tumor necrosis factor antibody; High affinity immunoglobulin gamma Fc receptor I ligand; Low affinity immunoglobulin gamma Fc region receptor II-a ligand; Low affinity immunoglobulin gamma Fc region receptor II-b ligand; Low affinity immunoglobulin gamma Fc region receptor II-c ligand; Low affinity immunoglobulin gamma Fc region receptor III-A ligand; Low affinity immunoglobulin gamma Fc region receptor III-B ligand; Lymphotoxin-alpha antibody; Complement component 1q (C1q) ligand |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I15 | 1290 | Bone disease | A connective tissue disease that affects the structure or development of bone or causes an impairment of normal bone function. http://en.wikipedia.org/wiki/Bone_disease | disease of anatomical entity/ musculoskeletal system disease/connective tissue disease | Details |