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Etanercept
Identification
- Name
- Etanercept
- Accession Number
- DB00005
- 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 IgG1.7,5 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 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.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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 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 ALymphotoxin-alpha antibodyHumans 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
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- 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 Unlock Additional DataAbatacept The risk or severity of infection can be increased when Etanercept is combined with Abatacept. Abiraterone The metabolism of Abiraterone 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. Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Etanercept. Acetaminophen The metabolism of Acetaminophen can be increased when combined with Etanercept. Acetohexamide The metabolism of Acetohexamide can be increased when combined with Etanercept. Acetylsalicylic acid The metabolism of Acetylsalicylic acid can be increased when combined with Etanercept. Acyclovir The metabolism of Acyclovir can be increased when combined with Etanercept. Adalimumab The risk or severity of adverse effects can be increased when Etanercept is combined with Adalimumab. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
- International/Other Brands
- Davictrel / Tunex
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBrenzys Solution Subcutaneous Samsung Bioepis Co., Ltd. 2016-09-13 Not applicable Canada 
Brenzys Solution Subcutaneous Samsung Bioepis Co., Ltd. 2016-09-23 Not applicable Canada Enbrel Injection, solution 50 mg Subcutaneous Pfizer 2000-02-03 Not applicable EU 
Enbrel 25 mg/1mL Subcutaneous Immunex Corporation 2003-01-02 Not applicable US 
Enbrel Injection, solution 25 mg Subcutaneous Pfizer 2000-02-03 Not applicable EU Enbrel Injection, powder, for solution 25 mg Subcutaneous Pfizer 2000-02-03 Not applicable EU Enbrel Injection, powder, for solution 50 mg Subcutaneous Pfizer 2000-02-03 Not applicable EU Enbrel Solution 50 mg/1mL Subcutaneous Immunex Corporation 2017-10-20 Not applicable US Enbrel Injection, solution 50 mg Subcutaneous Pfizer 2000-02-03 Not applicable EU Enbrel Solution 25 mg/0.5mL Subcutaneous Immunex Corporation 2019-06-07 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Enbrel Etanercept (25 mg) + Water (1 ml) Kit; Liquid; Powder, for solution Subcutaneous Immunex Corporation 2001-03-14 Not applicable 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
- Receptors, Cell Surface
- Receptors, Cytokine
- Receptors, Immunologic
- Receptors, Tumor Necrosis Factor
- Serum Globulins
- Tumor Necrosis Factor Alpha (TNF-α) Inhibitors
- Tumor Necrosis Factor Blocker
- 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
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. [PubMed:27463856]
- 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. [PubMed:20852002]
- 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. [PubMed:15703360]
- 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. [PubMed:10676822]
- 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. [PubMed:17916444]
- 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. [PubMed:8387891]
- FDA Approved Drug Products: Enbrel (etanercept) injection solution [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
- AHFS Codes
- 92:36.00 — Disease-modifying Antirheumatic Agents
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Rheumatoid Arthritis 1 4 Active Not Recruiting Treatment Ankylosing Spondylitis (AS) 1 4 Active Not Recruiting Treatment Rheumatoid Arthritis 1 4 Completed Not Available Ankylosing Spondylitis (AS) 3 4 Completed Not Available Arthritis / Rheumatoid 1 4 Completed Not Available Inflammatory Reaction / Rheumatoid Arthritis 1 4 Completed Not Available Psoriasis 1 4 Completed Not Available Psoriatic Arthritis / Rheumatoid Arthritis 1 4 Completed Not Available Rheumatoid Arthritis 2 4 Completed Prevention Ankylosing Spondylitis (AS) / Recurrences 1
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 Solution Subcutaneous Injection, powder, for solution Subcutaneous 10 mg Injection, powder, for solution Subcutaneous 25 mg Injection, powder, for solution Subcutaneous 50 mg Injection, solution Subcutaneous 25 mg Injection, solution Subcutaneous 50 mg Kit Subcutaneous Kit; liquid; powder, for solution Subcutaneous Solution Subcutaneous 25 mg/0.5mL Solution Subcutaneous 50 mg/1mL Powder Parenteral 25 MG - 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 Unlock Additional DataCA2476934 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 Additional Data Available- Filed On
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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Tumor necrosis factor receptor binding
- Specific 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 ac...
- 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. [PubMed:10206649]
- 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. [PubMed:10338381]
- 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. [PubMed:10357816]
- Moreland LW: Inhibitors of tumor necrosis factor: new treatment options for rheumatoid arthritis. Cleve Clin J Med. 1999 Jun;66(6):367-74. [PubMed:10375846]
- Calabrese LH: Rheumatoid arthritis and primary care: the case for early diagnosis and treatment. J Am Osteopath Assoc. 1999 Jun;99(6):313-21. [PubMed:10405518]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Receptor signaling protein activity
- Specific Function
- High affinity receptor for the Fc region of immunoglobulins gamma. Functions in both innate and adaptive immune responses.
- 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. [PubMed:27463856]
- 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. [PubMed:19128982]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Not Available
- Specific 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 ...
- 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. [PubMed:15457442]
- 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. [PubMed:15526004]
- 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. [PubMed:27463856]
- 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. [PubMed:19128982]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Not Available
- Specific 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 complex...
- 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. [PubMed:27463856]
- 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. [PubMed:19128982]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Transmembrane signaling receptor activity
- Specific 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 modulat...
- 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. [PubMed:10800083]
- 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. [PubMed:7535196]
- 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. [PubMed:19128982]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Not Available
- Specific Function
- Receptor for the Fc region of IgG. Binds complexed or aggregated IgG and also monomeric IgG. Mediates antibody-dependent cellular cytotoxicity (ADCC) and other antibody-dependent responses, such as...
- 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. [PubMed:15457442]
- 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. [PubMed:15526004]
- 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. [PubMed:27463856]
- 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. [PubMed:19128982]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Not Available
- Specific 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...
- Gene Name
- FCGR3B
- Uniprot ID
- O75015
- Uniprot Name
- Low affinity immunoglobulin gamma Fc region receptor III-B
- Molecular Weight
- 26215.64 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. [PubMed:10800083]
- 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. [PubMed:17387033]
- 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. [PubMed:15457442]
- 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. [PubMed:15526004]
- 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. [PubMed:19128982]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antibody
- General Function
- Receptor binding
- Specific Function
- Cytokine that in its homotrimeric form binds to TNFRSF1A/TNFR1, TNFRSF1B/TNFBR and TNFRSF14/HVEM. In its heterotrimeric form with LTB binds to TNFRSF3/LTBR. Lymphotoxin is produced by lymphocytes a...
- 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. [PubMed:11302411]
- 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. [PubMed:15005015]
- 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. [PubMed:15033655]
- Enbrel (Etanercept) FDA Label [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Ligand
- General Function
- Not Available
- Specific 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) proe...
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. [PubMed:27463856]
Drug created on June 13, 2005 07:24 / Updated on August 04, 2020 17:13
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