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Identification
- Summary
Etanercept is a protein therapy based on the binding fragment of the tumour necrosis factor alpha receptor used to treat severe rheumatoid arthritis and moderate to severe plaque psoriasis.
- Brand Names
- Enbrel, Eticovo
- Generic Name
- Etanercept
- DrugBank Accession Number
- DB00005
- Background
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 IgG1.7,5 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).
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Fusion proteins - Protein Structure
- Protein Chemical Formula
- C2224H3475N621O698S36
- Protein Average Weight
- 51234.9 Da (Monomer)
- Sequences
> Etanercept Sequence LPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSDTVCDSCEDST YTQLWNWVPECLSCGSRCSSDQVETQACTREQNRICTCRPGWYCALSKQEGCRLCAPLRK CRPGFGVARPGTETSDVVCKPCAPGTFSNTTSSTDICRPHQICNVVAIPGNASMDAVCTS TSPTRSMAPGAVHLPQPVSTRSQHTQPTPEPSTAPSTSFLLPMGPSPPAEGSTGDEPKSC DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVD GVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Download FASTA Format- Synonyms
- Etanercept
- etanercept-szzs
- etanercept-ykro
- Recombinant human TNF
- rhu TNFR:Fc
- rhu-TNFR:Fc
- TNFR-Immunoadhesin
- External IDs
- CHS-0214
- DWP-422
- ENIA-11
- GP-2015
- GP2015
- GP2015C
- HD-203
- HD203
- LBEC-0101
- LBEC0101
- SB-4
- SB4
Pharmacology
- 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.7,8 It is also used to manage signs and symptoms of polyarticular idiopathic arthritis and Juvenile Psoriatic Arthritis in those aged 2 years and older. Etanercept is also used to manage the symptoms of psoriatic arthritis and ankylosing spondylitis.9
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Active juvenile psoriatic arthritis •••••••••••• ••••••••• ••••••••• Management of Ankylosing spondylitis •••••••••••• ••••••••• Management of Graft-versus-host disease ••• ••••• Management of Plaque psoriasis •••••••••••• ••••• ••••••••• Management of Polyarticular juvenile idiopathic arthritis •••••••••••• •••••••••• •••••••• •• ••• •• •••• •••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF.7,5 Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinases.
- Mechanism of action
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).5 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.6TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses.5 Increased levels of TNF are found in tissues and fluids of those with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and plaque psoriasis.
Target Actions Organism ATumor necrosis factor inhibitorantibodyHumans ALymphotoxin-alpha antibodyHumans UHigh affinity immunoglobulin gamma Fc receptor I ligandHumans ULow affinity immunoglobulin gamma Fc region receptor II-a ligandHumans ULow affinity immunoglobulin gamma Fc region receptor II-b ligandHumans ULow affinity immunoglobulin gamma Fc region receptor II-c ligandHumans ULow affinity immunoglobulin gamma Fc region receptor III-A ligandHumans ULow affinity immunoglobulin gamma Fc region receptor III-B ligandHumans UComplement component 1q (C1q) ligandHumans - Absorption
Population pharmacokinetic modeling in adults with RA, AS, or who were healthy showed a subcutaneous bioavailability of 56.9% with a Ka of 0.0223/h.2 Another model in pediatric JIA patients showed an increased Ka of 0.05/h with a high mean interindividual variability of 215%.3 Cmax after a single 25 mg subcutaneous dose of Enbrel is reported as 1.1 mcg/L with a Tmax of 69 h.7 Cmax after repeated dosing is reported as 2.4 mcg/L in adult RA patients with a dosage of 25 mg twice weekly and 2.1 mcg in pediatric JIA patients with a dosage of 0.4 mg/kg twice weekly.
- Volume of distribution
Population pharmacokinetic modeling predicts a total Vd of 5.49 L with a peripheral compartment of 1.24 L in adults with RA and an apparent Vd with subcutaneous administration in pediatric JIA patients of 7.88 L.2,3
- Protein binding
No significant protein binding has been identified.
- Metabolism
As etanercept is a fusion protein antibody, it is assumed to be metabolized via proteinases similarly to endogenous proteins.
- Route of elimination
Not Available
- Half-life
Etanercept has a mean half-life of elimination of 102 hours in RA patients.7 Population models have shown a mean half-life of 68 hours in healthy adults and 70.7-94.8 hours in pediatric JIA patients.4,3
- Clearance
Etanercept has a mean apparent clearance of 160 mL/h in RA patients.7 Population models predict a mean apparent clearance of 132 mL/h in healthy adults and 0.0576 L/h in pediatric JIA patients.4,3
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of infection can be increased when Etanercept is combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Etanercept. Abrocitinib The metabolism of Abrocitinib can be increased when combined with Etanercept. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Etanercept. Acebutolol The metabolism of Acebutolol can be increased when combined with Etanercept. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Davictrel / Tunex
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Benepali Injection, solution 25 mg Subcutaneous Samsung Bioepis Nl B.V. 2020-12-16 Not applicable EU 
Benepali Injection, solution 50 mg Subcutaneous Samsung Bioepis Nl B.V. 2020-12-16 Not applicable EU Benepali Injection, solution 50 mg Subcutaneous Samsung Bioepis Nl B.V. 2020-12-16 Not applicable EU Benepali Injection, solution 25 mg Subcutaneous Samsung Bioepis Nl B.V. 2020-12-16 Not applicable EU Benepali Injection, solution 50 mg Subcutaneous Samsung Bioepis Nl B.V. 2020-12-16 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Enbrel Etanercept (25 mg / kit) + Water (1 mL / kit) Kit; Liquid; Powder, for solution Subcutaneous Immunex Corporation 2001-03-14 2023-01-31 Canada 
Enbrel Etanercept (25 mg/1mL) + Benzyl alcohol (9.93 mg/1mL) Kit Subcutaneous Physicians Total Care, Inc. 2003-04-30 2012-06-30 US 
Categories
- ATC Codes
- L04AB01 — Etanercept
- Drug Categories
- Agents reducing cytokine levels
- Amino Acids, Peptides, and Proteins
- Anti-Inflammatory Agents
- Antibodies
- Antirheumatic Agents
- Biological Products
- Biologics for Rheumatoid Arthritis Treatment
- Dermatologicals
- Disease-modifying Antirheumatic Agents
- Immunoglobulin Constant Regions
- Immunoglobulin Fc Fragments
- Immunoglobulin Fragments
- Immunoglobulin Isotypes
- Immunologic Factors
- Immunoproteins
- Immunosuppressive Agents
- Membrane Proteins
- Peptides
- Proteins
- Tumor necrosis factor alpha (TNF-alpha) inhibitors
- Tumor Necrosis Factor Blockers
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- OP401G7OJC
- CAS number
- 185243-69-0
References
- Synthesis Reference
Timothy D. Osslund, Christi L. Clogston, Shon Lee Crampton, Randal B. Bass, "Crystals of etanercept and methods of making thereof." U.S. Patent US07276477, issued October 02, 2007.
US07276477- General References
- Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16. [Article]
- Zhou SY, Shu C, Korth-Bradley J, Raible D, Palmisano M, Wadjula J, Fatenejad S, Bjornsson T: Integrated population pharmacokinetics of etanercept in healthy subjects and in patients with rheumatoid arthritis and ankylosing spondylitis. J Clin Pharmacol. 2011 Jun;51(6):864-75. doi: 10.1177/0091270010375961. Epub 2010 Sep 17. [Article]
- Yim DS, Zhou H, Buckwalter M, Nestorov I, Peck CC, Lee H: Population pharmacokinetic analysis and simulation of the time-concentration profile of etanercept in pediatric patients with juvenile rheumatoid arthritis. J Clin Pharmacol. 2005 Mar;45(3):246-56. doi: 10.1177/0091270004271945. [Article]
- Korth-Bradley JM, Rubin AS, Hanna RK, Simcoe DK, Lebsack ME: The pharmacokinetics of etanercept in healthy volunteers. Ann Pharmacother. 2000 Feb;34(2):161-4. doi: 10.1345/aph.19126. [Article]
- Wong M, Ziring D, Korin Y, Desai S, Kim S, Lin J, Gjertson D, Braun J, Reed E, Singh RR: TNFalpha blockade in human diseases: mechanisms and future directions. Clin Immunol. 2008 Feb;126(2):121-36. doi: 10.1016/j.clim.2007.08.013. Epub 2007 Oct 3. [Article]
- Banner DW, D'Arcy A, Janes W, Gentz R, Schoenfeld HJ, Broger C, Loetscher H, Lesslauer W: Crystal structure of the soluble human 55 kd TNF receptor-human TNF beta complex: implications for TNF receptor activation. Cell. 1993 May 7;73(3):431-45. [Article]
- FDA Approved Drug Products: Enbrel (etanercept) injection solution [Link]
- Health Canada Approved Drug Products: RYMTI (etanercept) solution for injection (August 2022) [Link]
- FDA Approved Drug Products: ENBREL® (etanercept) injection, for subcutaneous use (October 2023) [Link]
- FDA Approved Drug Products: Erelzi (etanercept) injection [Link]
- External Links
- UniProt
- P20333
- Genbank
- M32315
- KEGG Drug
- D00742
- KEGG Compound
- C07897
- PubChem Substance
- 46506732
- 214555
- ChEMBL
- CHEMBL1201572
- Therapeutic Targets Database
- DNC000605
- PharmGKB
- PA449515
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Etanercept
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Treatment Brain Disorders / Decline, Cognitive / Depression / Fatigue / Hand Rheumatism / Pain / Rheumatoid Arthritis 1 somestatus stop reason just information to hide Not Available Completed Not Available Ankylosing Spondylitis (AS) 8 somestatus stop reason just information to hide Not Available Completed Not Available Ankylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis 2 somestatus stop reason just information to hide Not Available Completed Not Available Arthritis / Rheumatoid 1 somestatus stop reason just information to hide Not Available Completed Not Available Atherosclerosis / Atopic Dermatitis / Psoriasis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Amgen Inc. + Wyeth + Takeda
- Packagers
- Amgen Inc.
- Boehringer Ingelheim Ltd.
- DSM Corp.
- Immunex Corp.
- Physicians Total Care Inc.
- Vetter Pharma Fertigung GmbH and Co. KG
- Dosage Forms
Form Route Strength Injection, solution Parenteral 25 MG Injection, solution Parenteral 50 MG Injection Subcutaneous 50 MG/ML Injection, powder, for solution Subcutaneous 10 MG Injection, powder, for solution Subcutaneous 25 MG/ML Injection, powder, for solution Subcutaneous 50 MG Injection, powder, lyophilized, for solution; kit Subcutaneous 25 mg/1mL Injection, solution Subcutaneous 25 MG Injection, solution Subcutaneous 50 MG Kit Subcutaneous Kit; liquid; powder, for solution Subcutaneous Powder Subcutaneous 25 MG Solution Parenteral; Subcutaneous 50 MG Solution Subcutaneous 25 mg/0.5mL Solution Subcutaneous 25.000 mg Solution Subcutaneous 50 mg/1mL Solution Subcutaneous 50 mg / mL Solution 25 mg/0.5ml Injection, powder, lyophilized, for solution Subcutaneous 50 mg Injection Subcutaneous 25 mg/0.5ml Powder Parenteral 25 MG Injection Subcutaneous 25 mg Injection Subcutaneous Injection Subcutaneous 50 mg Injection, solution Subcutaneous 50 mg/mL Solution Subcutaneous 25 mg Solution Subcutaneous 50 mg Injection, solution Parenteral; Subcutaneous 25 MG Injection, solution Parenteral; Subcutaneous 50 MG Solution Subcutaneous 25 mg / 0.5 mL Solution Subcutaneous 25.00 mg Injection, powder, lyophilized, for solution Subcutaneous 25 mg Injection, solution Subcutaneous 25 mg/0.5mL Injection, solution Subcutaneous 50 mg/1mL Injection, powder, for solution Subcutaneous 25 mg Solution 25 mg Solution 50 mg Solution 50 mg/ml Solution Subcutaneous 50 mg / 1 mL Injection, powder, for solution Intramuscular 25 mg/25mg Injection, solution 50 mg Powder 25 mg/1vial - Prices
Unit description Cost Unit Enbrel (1 Box = 1 Kit = Four 50 mg Syringes) 3.92ml Box 2033.14USD box Enbrel SureClick (1 Box Contains Four 50 mg Prefilled Autoinjectors) 2033.14USD box Enbrel 4 25 mg Kit (1 Box = 1 Kit = Four 25 mg Vials) 1016.57USD box Enbrel 50 mg/ml sureclick syr 488.74USD syringe Enbrel 25 mg kit 250.37USD each DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2476934 No 2009-06-16 2023-02-27 Canada CA2123593 No 2000-03-14 2013-09-14 Canada US7276477 No 2007-10-02 2024-07-29 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 71 °C (whole mAb) Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000) hydrophobicity -0.529 Not Available isoelectric point 7.89 Not Available
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- InhibitorAntibody
- General Function
- Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs regulatory T-cells (Treg) function in individuals with rheumatoid arthritis via FOXP3 dephosphorylation. Up-regulates the expression of protein phosphatase 1 (PP1), which dephosphorylates the key 'Ser-418' residue of FOXP3, thereby inactivating FOXP3 and rendering Treg cells functionally defective (PubMed:23396208). Key mediator of cell death in the anticancer action of BCG-stimulated neutrophils in combination with DIABLO/SMAC mimetic in the RT4v6 bladder cancer cell line (PubMed:16829952, PubMed:22517918, PubMed:23396208). Induces insulin resistance in adipocytes via inhibition of insulin-induced IRS1 tyrosine phosphorylation and insulin-induced glucose uptake. Induces GKAP42 protein degradation in adipocytes which is partially responsible for TNF-induced insulin resistance (By similarity). Plays a role in angiogenesis by inducing VEGF production synergistically with IL1B and IL6 (PubMed:12794819). Promotes osteoclastogenesis and therefore mediates bone resorption (By similarity)
- Specific Function
- cytokine activity
- Gene Name
- TNF
- Uniprot ID
- P01375
- Uniprot Name
- Tumor necrosis factor
- Molecular Weight
- 25644.15 Da
References
- Park YC, Burkitt V, Villa AR, Tong L, Wu H: Structural basis for self-association and receptor recognition of human TRAF2. Nature. 1999 Apr 8;398(6727):533-8. [Article]
- Sandborn WJ, Hanauer SB: Antitumor necrosis factor therapy for inflammatory bowel disease: a review of agents, pharmacology, clinical results, and safety. Inflamm Bowel Dis. 1999 May;5(2):119-33. [Article]
- Grell M, Zimmermann G, Gottfried E, Chen CM, Grunwald U, Huang DC, Wu Lee YH, Durkop H, Engelmann H, Scheurich P, Wajant H, Strasser A: Induction of cell death by tumour necrosis factor (TNF) receptor 2, CD40 and CD30: a role for TNF-R1 activation by endogenous membrane-anchored TNF. EMBO J. 1999 Jun 1;18(11):3034-43. [Article]
- Moreland LW: Inhibitors of tumor necrosis factor: new treatment options for rheumatoid arthritis. Cleve Clin J Med. 1999 Jun;66(6):367-74. [Article]
- Calabrese LH: Rheumatoid arthritis and primary care: the case for early diagnosis and treatment. J Am Osteopath Assoc. 1999 Jun;99(6):313-21. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Clark IA, Vissel B: Neurodegenerative disease treatments by direct TNF reduction, SB623 cells, maraviroc and irisin and MCC950, from an inflammatory perspective - a Commentary. Expert Rev Neurother. 2019 Jun;19(6):535-543. doi: 10.1080/14737175.2019.1618710. Epub 2019 May 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Cytokine that in its homotrimeric form binds to TNFRSF1A/TNFR1, TNFRSF1B/TNFBR and TNFRSF14/HVEM (PubMed:9462508). In its heterotrimeric form with LTB binds to TNFRSF3/LTBR (PubMed:24248355). Lymphotoxin is produced by lymphocytes and is cytotoxic for a wide range of tumor cells in vitro and in vivo
- Specific Function
- cytokine activity
- Gene Name
- LTA
- Uniprot ID
- P01374
- Uniprot Name
- Lymphotoxin-alpha
- Molecular Weight
- 22296.57 Da
References
- Johnson CJ, Reilly KM, Murray KM: Etanercept in juvenile rheumatoid arthritis. Ann Pharmacother. 2001 Apr;35(4):464-71. [Article]
- Gudbrandsdottir S, Larsen R, Sorensen LK, Nielsen S, Hansen MB, Svenson M, Bendtzen K, Muller K: TNF and LT binding capacities in the plasma of arthritis patients: effect of etanercept treatment in juvenile idiopathic arthritis. Clin Exp Rheumatol. 2004 Jan-Feb;22(1):118-24. [Article]
- Buch MH, Conaghan PG, Quinn MA, Bingham SJ, Veale D, Emery P: True infliximab resistance in rheumatoid arthritis: a role for lymphotoxin alpha? Ann Rheum Dis. 2004 Oct;63(10):1344-6. Epub 2004 Mar 19. [Article]
- Enbrel (Etanercept) FDA Label [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses. Mediates IgG effector functions on monocytes triggering antibody-dependent cellular cytotoxicity (ADCC) of virus-infected cells
- Specific Function
- high-affinity IgG receptor activity
- Gene Name
- FCGR1A
- Uniprot ID
- P12314
- Uniprot Name
- High affinity immunoglobulin gamma Fc receptor I
- Molecular Weight
- 42631.525 Da
References
- Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16. [Article]
- Arora T, Padaki R, Liu L, Hamburger AE, Ellison AR, Stevens SR, Louie JS, Kohno T: Differences in binding and effector functions between classes of TNF antagonists. Cytokine. 2009 Feb;45(2):124-31. doi: 10.1016/j.cyto.2008.11.008. Epub 2009 Jan 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Binds to the Fc region of immunoglobulins gamma. Low affinity receptor. By binding to IgG it initiates cellular responses against pathogens and soluble antigens. Promotes phagocytosis of opsonized antigens
- Specific Function
- IgG binding
- Gene Name
- FCGR2A
- Uniprot ID
- P12318
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor II-a
- Molecular Weight
- 35000.42 Da
References
- Criswell LA, Lum RF, Turner KN, Woehl B, Zhu Y, Wang J, Tiwari HK, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL Jr: The influence of genetic variation in the HLA-DRB1 and LTA-TNF regions on the response to treatment of early rheumatoid arthritis with methotrexate or etanercept. Arthritis Rheum. 2004 Sep;50(9):2750-6. [Article]
- Hughes LB, Criswell LA, Beasley TM, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL: Genetic risk factors for infection in patients with early rheumatoid arthritis. Genes Immun. 2004 Dec;5(8):641-7. [Article]
- Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16. [Article]
- Arora T, Padaki R, Liu L, Hamburger AE, Ellison AR, Stevens SR, Louie JS, Kohno T: Differences in binding and effector functions between classes of TNF antagonists. Cytokine. 2009 Feb;45(2):124-31. doi: 10.1016/j.cyto.2008.11.008. Epub 2009 Jan 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Receptor for the Fc region of complexed or aggregated immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells. Binding to this receptor results in down-modulation of previous state of cell activation triggered via antigen receptors on B-cells (BCR), T-cells (TCR) or via another Fc receptor. Isoform IIB1 fails to mediate endocytosis or phagocytosis. Isoform IIB2 does not trigger phagocytosis
- Specific Function
- amyloid-beta binding
- Gene Name
- FCGR2B
- Uniprot ID
- P31994
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor II-b
- Molecular Weight
- 34043.355 Da
References
- Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16. [Article]
- Arora T, Padaki R, Liu L, Hamburger AE, Ellison AR, Stevens SR, Louie JS, Kohno T: Differences in binding and effector functions between classes of TNF antagonists. Cytokine. 2009 Feb;45(2):124-31. doi: 10.1016/j.cyto.2008.11.008. Epub 2009 Jan 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Receptor for the Fc region of complexed immunoglobulins gamma. Low affinity receptor. Involved in a variety of effector and regulatory functions such as phagocytosis of immune complexes and modulation of antibody production by B-cells
- Specific Function
- IgG binding
- Gene Name
- FCGR2C
- Uniprot ID
- P31995
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor II-c
- Molecular Weight
- 35577.96 Da
References
- Hart SP, Ross JA, Ross K, Haslett C, Dransfield I: Molecular characterization of the surface of apoptotic neutrophils: implications for functional downregulation and recognition by phagocytes. Cell Death Differ. 2000 May;7(5):493-503. [Article]
- Ranheim EA, Kipps TJ: Tumor necrosis factor-alpha facilitates induction of CD80 (B7-1) and CD54 on human B cells by activated T cells: complex regulation by IL-4, IL-10, and CD40L. Cell Immunol. 1995 Apr 1;161(2):226-35. [Article]
- Arora T, Padaki R, Liu L, Hamburger AE, Ellison AR, Stevens SR, Louie JS, Kohno T: Differences in binding and effector functions between classes of TNF antagonists. Cytokine. 2009 Feb;45(2):124-31. doi: 10.1016/j.cyto.2008.11.008. Epub 2009 Jan 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Receptor for the invariable Fc fragment of immunoglobulin gamma (IgG). Optimally activated upon binding of clustered antigen-IgG complexes displayed on cell surfaces, triggers lysis of antibody-coated cells, a process known as antibody-dependent cellular cytotoxicity (ADCC). Does not bind free monomeric IgG, thus avoiding inappropriate effector cell activation in the absence of antigenic trigger (PubMed:11711607, PubMed:21768335, PubMed:22023369, PubMed:24412922, PubMed:25786175, PubMed:25816339, PubMed:28652325, PubMed:8609432, PubMed:9242542). Mediates IgG effector functions on natural killer (NK) cells. Binds antigen-IgG complexes generated upon infection and triggers NK cell-dependent cytokine production and degranulation to limit viral load and propagation. Involved in the generation of memory-like adaptive NK cells capable to produce high amounts of IFNG and to efficiently eliminate virus-infected cells via ADCC (PubMed:24412922, PubMed:25786175). Regulates NK cell survival and proliferation, in particular by preventing NK cell progenitor apoptosis (PubMed:29967280, PubMed:9916693). Fc-binding subunit that associates with CD247 and/or FCER1G adapters to form functional signaling complexes. Following the engagement of antigen-IgG complexes, triggers phosphorylation of immunoreceptor tyrosine-based activation motif (ITAM)-containing adapters with subsequent activation of phosphatidylinositol 3-kinase signaling and sustained elevation of intracellular calcium that ultimately drive NK cell activation. The ITAM-dependent signaling coupled to receptor phosphorylation by PKC mediates robust intracellular calcium flux that leads to production of pro-inflammatory cytokines, whereas in the absence of receptor phosphorylation it mainly activates phosphatidylinositol 3-kinase signaling leading to cell degranulation (PubMed:1825220, PubMed:23024279, PubMed:2532305). Costimulates NK cells and trigger lysis of target cells independently of IgG binding (PubMed:10318937, PubMed:23006327). Mediates the antitumor activities of therapeutic antibodies. Upon ligation on monocytes triggers TNFA-dependent ADCC of IgG-coated tumor cells (PubMed:27670158). Mediates enhanced ADCC in response to afucosylated IgGs (PubMed:34485821)
- Specific Function
- IgG binding
- Gene Name
- FCGR3A
- Uniprot ID
- P08637
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor III-A
- Molecular Weight
- 29088.895 Da
References
- Criswell LA, Lum RF, Turner KN, Woehl B, Zhu Y, Wang J, Tiwari HK, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL Jr: The influence of genetic variation in the HLA-DRB1 and LTA-TNF regions on the response to treatment of early rheumatoid arthritis with methotrexate or etanercept. Arthritis Rheum. 2004 Sep;50(9):2750-6. [Article]
- Hughes LB, Criswell LA, Beasley TM, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL: Genetic risk factors for infection in patients with early rheumatoid arthritis. Genes Immun. 2004 Dec;5(8):641-7. [Article]
- Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16. [Article]
- Arora T, Padaki R, Liu L, Hamburger AE, Ellison AR, Stevens SR, Louie JS, Kohno T: Differences in binding and effector functions between classes of TNF antagonists. Cytokine. 2009 Feb;45(2):124-31. doi: 10.1016/j.cyto.2008.11.008. Epub 2009 Jan 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Receptor for the Fc region of immunoglobulins gamma. Low affinity receptor. Binds complexed or aggregated IgG and also monomeric IgG. Contrary to III-A, is not capable to mediate antibody-dependent cytotoxicity and phagocytosis. May serve as a trap for immune complexes in the peripheral circulation which does not activate neutrophils
- Specific Function
- GPI anchor binding
- Gene Name
- FCGR3B
- Uniprot ID
- O75015
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor III-B
- Molecular Weight
- 26242.67 Da
References
- Hart SP, Ross JA, Ross K, Haslett C, Dransfield I: Molecular characterization of the surface of apoptotic neutrophils: implications for functional downregulation and recognition by phagocytes. Cell Death Differ. 2000 May;7(5):493-503. [Article]
- Ozgocmen S, Godekmerdan A, Ozkurt-Zengin F: Acute-phase response, clinical measures and disease activity in ankylosing spondylitis. Joint Bone Spine. 2007 May;74(3):249-53. Epub 2007 Mar 5. [Article]
- Criswell LA, Lum RF, Turner KN, Woehl B, Zhu Y, Wang J, Tiwari HK, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL Jr: The influence of genetic variation in the HLA-DRB1 and LTA-TNF regions on the response to treatment of early rheumatoid arthritis with methotrexate or etanercept. Arthritis Rheum. 2004 Sep;50(9):2750-6. [Article]
- Hughes LB, Criswell LA, Beasley TM, Edberg JC, Kimberly RP, Moreland LW, Seldin MF, Bridges SL: Genetic risk factors for infection in patients with early rheumatoid arthritis. Genes Immun. 2004 Dec;5(8):641-7. [Article]
- Arora T, Padaki R, Liu L, Hamburger AE, Ellison AR, Stevens SR, Louie JS, Kohno T: Differences in binding and effector functions between classes of TNF antagonists. Cytokine. 2009 Feb;45(2):124-31. doi: 10.1016/j.cyto.2008.11.008. Epub 2009 Jan 6. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- C1q associates with the proenzymes C1r and C1s to yield C1, the first component of the serum complement system. The collagen-like regions of C1q interact with the Ca(2+)-dependent C1r(2)C1s(2) proenzyme complex, and efficient activation of C1 takes place on interaction of the globular heads of C1q with the Fc regions of IgG or IgM antibody present in immune complexes
- Specific Function
- amyloid-beta binding
Components:
| Name | UniProt ID |
|---|---|
| Complement C1q subcomponent subunit A | P02745 |
| Complement C1q subcomponent subunit B | P02746 |
| Complement C1q subcomponent subunit C | P02747 |
References
- Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 02, 2024 13:51