Etanercept

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
Db00005
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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
ATumor necrosis factor
antibody
Humans
UHigh affinity immunoglobulin gamma Fc receptor I
ligand
Humans
ULow affinity immunoglobulin gamma Fc region receptor II-a
ligand
Humans
ULow affinity immunoglobulin gamma Fc region receptor II-b
ligand
Humans
ULow affinity immunoglobulin gamma Fc region receptor II-c
ligand
Humans
ULow affinity immunoglobulin gamma Fc region receptor III-A
ligand
Humans
ULow affinity immunoglobulin gamma Fc region receptor III-B
ligand
Humans
ALymphotoxin-alpha
antibody
Humans
UComplement component 1q (C1q)
ligand
Humans
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
Adverseeffects
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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.
DrugInteraction
AbataceptThe risk or severity of infection can be increased when Etanercept is combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Etanercept.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Etanercept.
AcebutololThe metabolism of Acebutolol can be increased when combined with Etanercept.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Etanercept.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Etanercept.
AcetohexamideThe metabolism of Acetohexamide can be increased when combined with Etanercept.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be increased when combined with Etanercept.
AcyclovirThe metabolism of Acyclovir can be increased when combined with Etanercept.
AdalimumabThe risk or severity of adverse effects can be increased when Etanercept is combined with Adalimumab.
Interactions
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Food Interactions
No interactions found.

Products

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International/Other Brands
Davictrel / Tunex
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BenepaliInjection, solution50 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BenepaliInjection, solution25 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BenepaliInjection, solution50 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BenepaliInjection, solution50 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BenepaliInjection, solution25 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BenepaliInjection, solution50 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BenepaliInjection, solution25 mgSubcutaneousSamsung Bioepis Nl B.V.2020-12-16Not applicableEU flag
BrenzysSolution50 mg / mLSubcutaneousSamsung Bioepis Co., Ltd.2016-09-13Not applicableCanada flag
BrenzysSolution50 mg / mLSubcutaneousSamsung Bioepis Co., Ltd.2016-09-23Not applicableCanada flag
EnbrelInjection, solution50 mgSubcutaneousPfizer Europe Ma Eeig2016-09-20Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
EnbrelEtanercept (25 mg / kit) + Water (1 mL / kit)Kit; Liquid; Powder, for solutionSubcutaneousImmunex Corporation2001-03-14Not applicableCanada flag
EnbrelEtanercept (25 mg/1mL) + Benzyl alcohol (9.93 mg/1mL)KitSubcutaneousPhysicians Total Care, Inc.2003-04-302012-06-30US flag

Categories

ATC Codes
L04AB01 — Etanercept
Drug Categories
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. FDA Approved Drug Products: Enbrel (etanercept) injection solution [Link]
UniProt
P20333
Genbank
M32315
KEGG Drug
D00742
KEGG Compound
C07897
PubChem Substance
46506732
RxNav
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
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentPancreatitis, Chronic; Diabetes; Transplant1
4Active Not RecruitingTreatmentRheumatoid Arthritis3
4CompletedPreventionAnkylosing Spondylitis (AS) / Recurrences1
4CompletedTreatmentActive Rheumatoid Arthritis; Rheumatoid Arthritis / Rheumatoid Arthritis1
4CompletedTreatmentAnkylosing Spondylitis (AS)8
4CompletedTreatmentAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Spondylarthropathy1
4CompletedTreatmentAxial Spondyloarthritis (AxSpA)1
4CompletedTreatmentCancer, Cancer Nonmelanoma Skin / Malignant Melanoma of Skin / Psoriasis (PsO)1
4CompletedTreatmentInflammatory Arthritis / Rheumatoid Arthritis1
4CompletedTreatmentJuvenile Chronic Polyarthritis / Juvenile Idiopathic Arthritis (JIA) / Rheumatoid Arthritis, Juvenile1

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
FormRouteStrength
Injection, solutionParenteral25 MG
Injection, solutionParenteral50 MG
InjectionSubcutaneous
Injection, powder, for solutionSubcutaneous10 MG
Injection, powder, for solutionSubcutaneous25 MG/ML
Injection, powder, for solutionSubcutaneous50 MG
Injection, solutionSubcutaneous25 MG
Injection, solutionSubcutaneous50 MG
KitSubcutaneous
Kit; liquid; powder, for solutionSubcutaneous
PowderSubcutaneous25 MG
SolutionParenteral; Subcutaneous50 MG
SolutionSubcutaneous25 mg/0.5mL
SolutionSubcutaneous50 mg / mL
SolutionSubcutaneous50 mg/1mL
Solution25 mg/0.5ml
Injection, powder, lyophilized, for solutionSubcutaneous50 mg
PowderParenteral25 MG
Injection, solutionSubcutaneous
InjectionSubcutaneous25 mg
Injection, solutionSubcutaneous50 mg/mL
SolutionSubcutaneous25 mg
SolutionSubcutaneous50 mg
Injection, solutionParenteral; Subcutaneous25 MG
Injection, solutionParenteral; Subcutaneous50 MG
SolutionSubcutaneous25 mg / 0.5 mL
Injection, powder, lyophilized, for solutionSubcutaneous25 mg
Injection, powder, lyophilized, for solutionSubcutaneous
Injection, solutionSubcutaneous25 mg/0.5mL
Injection, solutionSubcutaneous50 mg/1mL
Injection, powder, for solutionSubcutaneous25 mg
Injection, solution50 mg
Powder25 mg/1vial
Prices
Unit descriptionCostUnit
Enbrel (1 Box = 1 Kit = Four 50 mg Syringes) 3.92ml Box2033.14USD 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 syr488.74USD syringe
Enbrel 25 mg kit250.37USD each
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2476934No2009-06-162023-02-27Canada flag
CA2123593No2000-03-142013-09-14Canada flag
US7276477No2007-10-022024-07-29US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)71 °C (whole mAb)Vermeer, A.W.P. & Norde, W., Biophys. J. 78:394-404 (2000)
hydrophobicity-0.529Not Available
isoelectric point7.89Not Available

Targets

Drugtargets2
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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
  1. 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]
  2. 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]
  3. 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]
  4. Moreland LW: Inhibitors of tumor necrosis factor: new treatment options for rheumatoid arthritis. Cleve Clin J Med. 1999 Jun;66(6):367-74. [Article]
  5. 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]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
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
  1. 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]
  2. 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
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
  1. 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]
  2. 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]
  3. 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]
  4. 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
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
  1. 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]
  2. 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
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
  1. 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]
  2. 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]
  3. 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
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
  1. 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]
  2. 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]
  3. 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]
  4. 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
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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
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
  1. Johnson CJ, Reilly KM, Murray KM: Etanercept in juvenile rheumatoid arthritis. Ann Pharmacother. 2001 Apr;35(4):464-71. [Article]
  2. 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]
  3. 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]
  4. 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:
References
  1. 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 on June 13, 2005 13:24 / Updated on October 22, 2021 23:18