Etanercept

Identification

Name
Etanercept
Accession Number
DB00005  (BTD00052, BIOD00052)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Fusion proteins
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.

Protein structure
Db00005
Protein chemical formula
C2224H3475N621O698S36
Protein average weight
51234.9 Da
Sequences
> Etanercept Sequence
LPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSDTVCDSCEDST
YTQLWNWVPECLSCGSRCSSDQVETQACTREQNRICTCRPGWYCALSKQEGCRLCAPLRK
CRPGFGVARPGTETSDVVCKPCAPGTFSNTTSSTDICRPHQICNVVAIPGNASMDAVCTS
TSPTRSMAPGAVHLPQPVSTRSQHTQPTPEPSTAPSTSFLLPMGPSPPAEGSTGDEPKSC
DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVD
GVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK
GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Download FASTA Format
Synonyms
  • Etanercept-szzs
  • 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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BrenzysSolution50 mgSubcutaneousSamsung Bioepis Co., Ltd.2016-09-13Not applicableCanada
BrenzysSolution50 mgSubcutaneousSamsung Bioepis Co., Ltd.2016-09-23Not applicableCanada
EnbrelInjection, powder, for solution25 mgSubcutaneousPfizer2000-02-03Not applicableEu
EnbrelInjection, solution50 mgSubcutaneousPfizer2000-02-03Not applicableEu
EnbrelSolution50 mg/1mLSubcutaneousImmunex Corporation2005-11-10Not applicableUs
EnbrelSolution50 mgSubcutaneousImmunex Corporation2005-12-21Not applicableCanada
EnbrelInjection, solution25 mgSubcutaneousPfizer2000-02-03Not applicableEu
EnbrelInjection, powder, for solution50 mgSubcutaneousPfizer2000-02-03Not applicableEu
EnbrelInjection, powder, for solution50 mgSubcutaneousPfizer2000-02-03Not applicableEu
EnbrelInjection, powder, for solution10 mgSubcutaneousPfizer2000-02-03Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
EnbrelEtanercept (25 mg) + Water (1 ml)Kit; Liquid; Powder, for solutionSubcutaneousImmunex Corporation2001-03-14Not applicableCanada
EnbrelEtanercept (25 mg/1mL) + Benzyl alcohol (9.93 mg/1mL)KitPhysicians Total Care, Inc.2003-04-302012-06-30Us
International/Other Brands
Davictrel / Enbrel Sureclick / Tunex
Categories
UNII
OP401G7OJC
CAS number
185243-69-0

Pharmacology

Indication

Etanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and chronic moderate to severe plaque psoriasis in adults. It is also used to manage signs and symptoms of polyarticular idiopathic arthritis in those aged 4 to 17 after insufficient response to one or more disease-modifying anti-rheumatic drugs. Etanercept is also used to improve psoriatic arthritis and ankylosing spondylitis.

Associated Conditions
Pharmacodynamics

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 metalloproteinase-3, also known as stromelysin. In animal models, etanarcept has been demonstrated to affect inflammation, such as in murine collagen-induced arthritis.

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). Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation.

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 (AS), and plaque psoriasis.

TargetActionsOrganism
ATumor necrosis factor
antibody
Human
UTumor necrosis factor receptor superfamily member 1BNot AvailableHuman
UHigh affinity immunoglobulin gamma Fc receptor INot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor III-ANot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor II-aNot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor II-bNot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor II-cNot AvailableHuman
ULymphotoxin-alphaNot AvailableHuman
ULow affinity immunoglobulin gamma Fc region receptor III-BNot AvailableHuman
UComplement C1s subcomponentNot AvailableHuman
UComplement C1r subcomponentNot AvailableHuman
UComplement C1q subcomponent subunit ANot AvailableHuman
UComplement C1q subcomponent subunit BNot AvailableHuman
UComplement C1q subcomponent subunit CNot AvailableHuman
Absorption

Bioavailability following sub-Q administration is approximately 60%. Peak plasma concentrations achieved within 69 hours.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

102 +/- 30 hrs in individuals with rheumatoid arthritis and 68 hours in healthy adults.

Clearance
  • 160 +/- 80 mL/hr [RA patients]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Etanercept is combined with 2-Methoxyethanol.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Etanercept is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
AbataceptThe risk or severity of infection can be increased when Etanercept is combined with Abatacept.
AbetimusThe risk or severity of adverse effects can be increased when Etanercept is combined with Abetimus.
ActeosideThe risk or severity of adverse effects can be increased when Etanercept is combined with Acteoside.
AdalimumabThe risk or severity of adverse effects can be increased when Etanercept is combined with Adalimumab.
AfelimomabThe risk or severity of adverse effects can be increased when Etanercept is combined with Afelimomab.
AlclometasoneThe risk or severity of adverse effects can be increased when Etanercept is combined with Alclometasone.
AldesleukinThe risk or severity of adverse effects can be increased when Etanercept is combined with Aldesleukin.
AldosteroneThe risk or severity of adverse effects can be increased when Etanercept is combined with Aldosterone.
Food Interactions
Not Available

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. Link [Link]
  2. Link [Link]
External Links
UniProt
P20333
Genbank
M32315
KEGG Drug
D00742
KEGG Compound
C07897
PubChem Substance
46506732
ChEMBL
CHEMBL1201572
Therapeutic Targets Database
DNC000605
PharmGKB
PA449515
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Etanercept
ATC Codes
L04AB01 — Etanercept
AHFS Codes
  • 92:36.00 — Disease-modifying Antirheumatic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentInclusion Body Myositis (IBM)1
1Active Not RecruitingTreatmentRheumatoid Arthritis1
1CompletedNot AvailableHealthy Volunteers2
1CompletedBasic ScienceBioequivalence / Phase 11
1CompletedBasic ScienceHealthy Volunteers2
1CompletedHealth Services ResearchAlzheimer's Disease (AD)1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentAcute and Chronic Inflammation / Autoimmune Diseases / Disorder of Pleura and Pleural Cavity / Disorder of Synovium / Felty's Syndrome / Rheumatoid Arthritis / Rheumatoid Nodules / Sjögren's Syndrome1
1CompletedTreatmentDermatomyositis1
1CompletedTreatmentHealthy Men and Women1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1CompletedTreatmentPsoriasis1
1CompletedTreatmentRheumatoid Arthritis1
1CompletedTreatmentTumors1
1Not Yet RecruitingPreventionSubarachnoid Hemorrhage, Aneurysmal1
1RecruitingTreatmentPsoriatic plaque1
1TerminatedTreatmentBone destruction / One to five years postmenopausal / Osteopenia / Rheumatoid Arthritis1
1Unknown StatusNot AvailableRheumatoid Arthritis1
1, 2Active Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
1, 2CompletedTreatmentAdenocarcinomas / Neoplasms, Pancreatic1
1, 2CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Small Lymphocytic Lymphoma (SLL)1
1, 2CompletedTreatmentDe Novo Myelodysplastic Syndromes / Previously Treated Myelodysplastic Syndromes / Secondary Myelodysplastic Syndromes1
1, 2CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
1, 2CompletedTreatmentLeukemias / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Diseases1
1, 2CompletedTreatmentObliterative Bronchiolitis / Pneumonia / Respiratory Distress Syndrome, Adult1
1, 2CompletedTreatmentPsoriasis1
1, 2Not Yet RecruitingTreatmentAutoimmune Diseases / Diabetes Mellitus (DM) / Diabetes, Diabetes Mellitus Type 1 / Hypoglycemia1
1, 2Not Yet RecruitingTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
1, 2RecruitingOtherRheumatoid Arthritis1
1, 2RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
1, 2WithdrawnTreatmentDiabetes, Diabetes Mellitus Type 11
2Active Not RecruitingPreventionGraft Versus Host Disease (GVHD)1
2Active Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
2Active Not RecruitingTreatmentLichen Planus (LP)1
2Active Not RecruitingTreatmentLupus Erythematosus, Chronic Cutaneous / Lupus Erythematosus, Cutaneous / Lupus Erythematosus, Discoid1
2Active Not RecruitingTreatmentMucocutaneous Lymph Node Syndrome1
2CompletedOtherRheumatoid Arthritis1
2CompletedTreatmentAccelerated Phase Chronic Myelogenous Leukemia / Acute, secondary Myeloid Leukemia / Blastic Phase Chronic Myelogenous Leukemia / Childhood Acute Lymphoblastic Leukemia in Remission / Childhood Acute Myeloid Leukemia in Remission / Childhood Chronic Myelogenous Leukemia / Childhood Myelodysplastic Syndromes / Chronic Phase Chronic Myelogenous Leukemia / De Novo Myelodysplastic Syndromes / Disseminated Neuroblastoma / Juvenile Myelomonocytic Leukemia / Previously Treated Childhood Rhabdomyosarcoma / Previously Treated Myelodysplastic Syndromes / Pulmonary Complications / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Myeloid Leukemia / Recurrent Childhood Large Cell Lymphoma / Recurrent Childhood Lymphoblastic Lymphoma / Recurrent Childhood Rhabdomyosarcoma / Recurrent Childhood Small Noncleaved Cell Lymphoma / Recurrent Neuroblastoma / Recurrent Wilms Tumor and Other Childhood Kidney Tumors / Recurrent/Refractory Childhood Hodgkin Lymphoma / Relapsing Chronic Myelogenous Leukemia / Secondary Myelodysplastic Syndromes1
2CompletedTreatmentAcute Lung Injury (ALI) / Obliterative Bronchiolitis / Respiratory Distress Syndrome, Adult1
2CompletedTreatmentAlzheimer's Disease (AD)1
2CompletedTreatmentAsthma Bronchial1
2CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
2CompletedTreatmentGraft Versus Host Disease (GVHD)2
2CompletedTreatmentGraft Versus Host Disease (GVHD) / Immune System Disorders1
2CompletedTreatmentGranulomatosis With Polyangiitis / Vasculitis1
2CompletedTreatmentHealthy Volunteers / Inflammatory Reaction1
2CompletedTreatmentHealthy Volunteers / Rheumatoid Arthritis1
2CompletedTreatmentHidradenitis Suppurativa (HS)1
2CompletedTreatmentHistiocytosis, Langerhans-Cell1
2CompletedTreatmentLeukemias / Myelodysplastic Syndromes1
2CompletedTreatmentLeukemias / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Diseases1
2CompletedTreatmentPemphigus Vulgaris (PV)1
2CompletedTreatmentPersistent Knee Joint Synovitis1
2CompletedTreatmentPsoriasis1
2CompletedTreatmentPulmonary Fibrosis1
2CompletedTreatmentRheumatoid Arthritis2
2CompletedTreatmentRheumatoid Arthritis, Juvenile / Uveitis1
2CompletedTreatmentSjögren's Syndrome1
2CompletedTreatmentTemporomandibular Joint Disorders1
2CompletedTreatmentTransplanted Kidney Ischemia Reperfusion Injury1
2CompletedTreatmentVitiligo1
2RecruitingTreatmentAnkylosing Spondylitis (AS)1
2RecruitingTreatmentDiabetes, Diabetes Mellitus Type 1 / Transplant, Kidney1
2SuspendedTreatmentPrimary Systemic Amyloidosis1
2TerminatedTreatmentEnd Stage Renal Disease (ESRD)1
2TerminatedTreatmentLeukemias1
2TerminatedTreatmentLichen Planus (LP)1
2TerminatedTreatmentMyalgic Encephalomyelitis (ME)1
2TerminatedTreatmentNephritis, Lupus1
2TerminatedTreatmentRheumatoid Arthritis1
2TerminatedTreatmentVesicular Stomatitis1
2Unknown StatusTreatmentAnkylosing Spondylitis (AS)1
2Unknown StatusTreatmentDiscoid Lupus Erythematosus (DLE)1
2Unknown StatusTreatmentModerate to Severe Active Axial Spondyloarthritis1
2Unknown StatusTreatmentSpondyloarthritis1
2, 3CompletedTreatmentAcute Exacerbation of Chronic Obstructive Pulmonary Disease1
2, 3CompletedTreatmentGranulomatosis With Polyangiitis1
2, 3CompletedTreatmentLumbosacral Radiculopathy1
2, 3CompletedTreatmentMetabolic Syndromes1
2, 3RecruitingTreatmentAnkylosing Spondylitis (AS) / Arthritis / Bone Diseases / Joint ankylosis / Musculoskeletal Disorders / Spinal Diseases / Spondylarthritis / Spondylarthropathy / Spondylitis1
2, 3TerminatedDiagnosticBone Cancer / Lung Cancers / Neoplasms Metastasis / Prostate Cancer1
2, 3TerminatedTreatmentDermatomyositis1
2, 3WithdrawnTreatmentChronic Idiopathic Urticaria1
3Active Not RecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
3Active Not RecruitingTreatmentJuvenile Idiopahtic Arthritis1
3Active Not RecruitingTreatmentPsoriasis2
3Active Not RecruitingTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
3Active Not RecruitingTreatmentPsoriasis / Psoriasis Vulgaris (Plaque Psoriasis)1
3Active Not RecruitingTreatmentRheumatoid Arthritis3
3CompletedPreventionPsoriasis / Psoriatic Arthritis1
3CompletedSupportive CareAnorexic / Cachexia / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentActive Rheumatoid Arthritis1
3CompletedTreatmentAnkylosing Spondylitis (AS)6
3CompletedTreatmentChronic Plaque Psoriasis1
3CompletedTreatmentDiabetes, Diabetes Mellitus Type 12
3CompletedTreatmentGraft Versus Host Disease, Acute1
3CompletedTreatmentIdiopathic Pneumonia Syndrome / Pneumonia1
3CompletedTreatmentInflammatory Reaction / Psoriasis1
3CompletedTreatmentJuvenile Idiopathic Arthritis (JIA)1
3CompletedTreatmentModerate to Severe Plaque Psoriasis1
3CompletedTreatmentPalmoplantaris Pustulosis1
3CompletedTreatmentPediatric Plaque Psoriasis1
3CompletedTreatmentPolymyalgia Rheumatica1
3CompletedTreatmentPsoriasis11
3CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)2
3CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis) / Rheumatoid Arthritis1
3CompletedTreatmentPsoriasis / Psoriatic Arthritis1
3CompletedTreatmentPsoriatic Arthritis1
3CompletedTreatmentPsoriatic Arthritis / Rheumatoid Arthritis1
3CompletedTreatmentProphylaxis of Rheumatic fever / Psoriatic Arthritis / Rheumatoid Arthritis1
3CompletedTreatmentRheumatoid Arthritis17
3Not Yet RecruitingTreatmentStevens Johnson Syndrome / Toxic Epidermal Necrolyses1
3RecruitingTreatmentChronic Severe Plaque-type Psoriasis1
3RecruitingTreatmentJuvenile Idiopathic Arthritis (JIA)1
3RecruitingTreatmentPsoriasis1
3RecruitingTreatmentPsoriasis / Psoriasis Vulgaris (Plaque Psoriasis)1
3SuspendedTreatmentRheumatoid Arthritis1
3TerminatedTreatmentRheumatoid Arthritis1
3TerminatedTreatmentRheumatoid Arthritis, Juvenile1
3WithdrawnTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
4Active Not RecruitingTreatmentAnkylosing Spondylitis (AS)2
4Active Not RecruitingTreatmentSpondyloarthritis1
4CompletedNot AvailableAnkylosing Spondylitis (AS)3
4CompletedNot AvailableArthritis / Rheumatoid1
4CompletedNot AvailableInflammatory Reaction / Rheumatoid Arthritis1
4CompletedNot AvailablePsoriasis1
4CompletedNot AvailablePsoriatic Arthritis / Rheumatoid Arthritis1
4CompletedNot AvailableRheumatoid Arthritis2
4CompletedPreventionAnkylosing Spondylitis (AS) / Recurrences1
4CompletedTreatmentActive Rheumatoid Arthritis / Rheumatoid Arthritis1
4CompletedTreatmentAnkylosing Spondylitis (AS)6
4CompletedTreatmentAnkylosing Spondylitis (AS) / Inflammatory Reaction1
4CompletedTreatmentAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Spondylarthropathy1
4CompletedTreatmentCardiovascular Disease, Rheumatoid Arthritis / Rheumatoid Arthritis1
4CompletedTreatmentJuvenile Chronic Polyarthritis / Juvenile Idiopathic Arthritis (JIA) / Rheumatoid Arthritis, Juvenile1
4CompletedTreatmentMelanoma / Non-Melanoma Skin Cancer (NMSC) / Psoriasis1
4CompletedTreatmentNail Psoriasis / Psoriasis Vulgaris (Plaque Psoriasis)1
4CompletedTreatmentPsoriasis10
4CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)4
4CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis) / Rheumatoid Arthritis1
4CompletedTreatmentPsoriasis, Moderate to Severe1
4CompletedTreatmentPsoriasis / Psoriasis Vulgaris (Plaque Psoriasis)1
4CompletedTreatmentPsoriasis / Psoriatic Arthritis1
4CompletedTreatmentPsoriatic Arthritis3
4CompletedTreatmentRheumatoid Arthritis20
4CompletedTreatmentSpondylarthropathies, Enthesitis1
4CompletedTreatmentSpondyloarthritis, Axial1
4CompletedTreatmentSpondyloarthropathies1
4Enrolling by InvitationBasic ScienceRheumatoid Arthritis1
4Not Yet RecruitingTreatmentAcute Gouty Arthritis1
4Not Yet RecruitingTreatmentAnkylosing Spondylitis (AS)1
4RecruitingBasic ScienceRheumatoid Arthritis1
4RecruitingPreventionSpondyloarthritis1
4RecruitingTreatmentPancreatitis, Chronic; Diabetes; Transplant1
4RecruitingTreatmentRheumatoid Arthritis8
4TerminatedTreatmentAnkylosing Spondylitis (AS)1
4TerminatedTreatmentModerate to Severe Rheumatoid Arthritis1
4TerminatedTreatmentPsoriasis1
4TerminatedTreatmentRheumatoid Arthritis3
4TerminatedTreatmentRheumatoid Arthritis / Vascular Inflammation1
4Unknown StatusBasic ScienceAbsolute Number, Density of Immune Infiltrate and Dendritic Cells and Inflammatory Cytokines Expression Pattern / Psoriasis, Moderate to Severe1
4Unknown StatusScreeningAnkylosing Spondylitis (AS) / Rheumatoid Arthritis1
4Unknown StatusTreatmentAnkylosing Spondylitis (AS) / High Blood Pressure (Hypertension) / Psoriatic Arthritis / Rheumatoid Arthritis1
4Unknown StatusTreatmentArthritis / Rheumatoid Arthritis1
4Unknown StatusTreatmentJuvenile Idiopathic Arthritis (JIA)1
4Unknown StatusTreatmentMyocardial Infarction1
4Unknown StatusTreatmentPsoriasis2
4Unknown StatusTreatmentRheumatoid Arthritis2
4WithdrawnNot AvailablePediatric Psoriasis1
4WithdrawnBasic ScienceRheumatoid Arthritis1
4WithdrawnTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
4WithdrawnTreatmentRheumatoid Arthritis1
Not AvailableActive Not RecruitingNot AvailablePsoriasis1
Not AvailableActive Not RecruitingTreatmentPsoriasis1
Not AvailableCompletedNot AvailableAnkylosing Spondylitis (AS)3
Not AvailableCompletedNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis1
Not AvailableCompletedNot AvailableAtherosclerosis / Atopic Dermatitis (AD) / Psoriasis1
Not AvailableCompletedNot AvailableHidradenitis Suppurativa (HS)1
Not AvailableCompletedNot AvailableHuman Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedNot AvailableInflammatory Bowel Diseases (IBD) / Psoriasis1
Not AvailableCompletedNot AvailableInflammatory Reaction / Psoriasis1
Not AvailableCompletedNot AvailableJuvenile Idiopathic Arthritis (JIA)1
Not AvailableCompletedNot AvailablePregnancy1
Not AvailableCompletedNot AvailablePsoriasis3
Not AvailableCompletedNot AvailablePsoriasis Arthritis / Rheumatoid Arthritis1
Not AvailableCompletedNot AvailablePsoriasis Vulgaris (Plaque Psoriasis) / Psoriatic Arthritis / Rheumatoid Arthritis / Spondyloarthritis, Axial1
Not AvailableCompletedNot AvailablePsoriasis / Psoriatic Arthritis / Skin Diseases, Papulosquamous2
Not AvailableCompletedNot AvailablePsoriatic Arthritis1
Not AvailableCompletedNot AvailablePsoriatic Arthritis / Rheumatoid Arthritis / Spondyloarthritis1
Not AvailableCompletedNot AvailableRheumatoid Arthritis12
Not AvailableCompletedNot AvailableRheumatoid Arthritis, Juvenile1
Not AvailableCompletedNot AvailableRhupus Syndrome, Etanercept1
Not AvailableCompletedNot AvailableSpondyloarthritis / Ultrasonography1
Not AvailableCompletedBasic SciencePsoriasis1
Not AvailableCompletedHealth Services ResearchCongenital Hypoplastic Anemia1
Not AvailableCompletedPreventionInguinal Hernias / Postoperative pain1
Not AvailableCompletedScreeningAnkylosing Spondylitis (AS)1
Not AvailableCompletedTreatmentAsthma Bronchial1
Not AvailableCompletedTreatmentDrug hypersensitivity reaction1
Not AvailableCompletedTreatmentMetabolic Syndromes2
Not AvailableCompletedTreatmentPsoriasis1
Not AvailableCompletedTreatmentRheumatoid Arthritis1
Not AvailableRecruitingNot AvailableAnkylosing Spondylitis (AS) / Psoriatic Arthritis / Rheumatoid Arthritis2
Not AvailableRecruitingNot AvailablePsoriasis1
Not AvailableRecruitingNot AvailableRheumatoid Arthritis4
Not AvailableRecruitingNot AvailableRheumatoid Arthritis / Spondyloarthritis, Axial1
Not AvailableRecruitingNot AvailableRheumatoid Arthritis / Spondyloarthropathies1
Not AvailableRecruitingTreatmentKnee Osteoarthritis (Knee OA)2
Not AvailableTerminatedNot AvailableAnkylosing Spondylitis (AS) / Rheumatoid Arthritis1
Not AvailableTerminatedPreventionBMI >30 kg/m2 / High Blood Pressure (Hypertension) / Hyperlipidemias / Metabolic Syndromes / Psoriasis1
Not AvailableUnknown StatusNot AvailableScleritis / Uveitis1
Not AvailableUnknown StatusTreatmentBehcet's Syndrome / Uveal Disease1
Not AvailableUnknown StatusTreatmentPsoriasis1
Not AvailableWithdrawnNot AvailableRheumatoid Arthritis1
Not AvailableWithdrawnTreatmentChronic Regional Pain Syndrome / CRP1

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, powder, for solutionSubcutaneous10 mg
Injection, powder, for solutionSubcutaneous25 mg
Injection, powder, for solutionSubcutaneous50 mg
Injection, solutionSubcutaneous25 mg
Injection, solutionSubcutaneous50 mg
Kit
Kit25 mg/1mL
Kit; liquid; powder, for solutionSubcutaneous
SolutionSubcutaneous25 mg/0.5mL
SolutionSubcutaneous50 mg
SolutionSubcutaneous50 mg/1mL
SolutionSubcutaneous25 mg
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)
CA2476934No2009-06-162023-02-27Canada
CA2123593No2000-03-142013-09-14Canada
US7276477No2007-10-022024-07-29Us
US36755No2000-06-272012-10-23Us

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

Taxonomy

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

Targets

Kind
Protein
Organism
Human
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. [PubMed:10206649]
  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. [PubMed:10338381]
  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. [PubMed:10357816]
  4. 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]
  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. [PubMed:10405518]
  6. 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
Human
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Receptor with high affinity for TNFSF2/TNF-alpha and approximately 5-fold lower affinity for homotrimeric TNFSF1/lymphotoxin-alpha. The TRAF1/TRAF2 complex recruits the apoptotic suppressors BIRC2 ...
Gene Name
TNFRSF1B
Uniprot ID
P20333
Uniprot Name
Tumor necrosis factor receptor superfamily member 1B
Molecular Weight
48290.85 Da
References
  1. 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
Human
Pharmacological action
Unknown
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. [PubMed:15457442]
  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. [PubMed:15526004]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. [PubMed:15457442]
  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. [PubMed:15526004]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. [PubMed:10800083]
  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. [PubMed:7535196]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. [PubMed:11302411]
  2. Pennica D, Lam VT, Mize NK, Weber RF, Lewis M, Fendly BM, Lipari MT, Goeddel DV: Biochemical properties of the 75-kDa tumor necrosis factor receptor. Characterization of ligand binding, internalization, and receptor phosphorylation. J Biol Chem. 1992 Oct 15;267(29):21172-8. [PubMed:1328224]
  3. 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]
  4. 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]
  5. Kang CP, Lee KW, Yoo DH, Kang C, Bae SC: The influence of a polymorphism at position -857 of the tumour necrosis factor alpha gene on clinical response to etanercept therapy in rheumatoid arthritis. Rheumatology (Oxford). 2005 Apr;44(4):547-52. Epub 2005 Feb 3. [PubMed:15695296]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. [PubMed:10800083]
  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. [PubMed:17387033]
  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. [PubMed:15457442]
  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. [PubMed:15526004]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
C1s B chain is a serine protease that combines with C1q and C1r to form C1, the first component of the classical pathway of the complement system. C1r activates C1s so that it can, in turn, activat...
Gene Name
C1S
Uniprot ID
P09871
Uniprot Name
Complement C1s subcomponent
Molecular Weight
76683.905 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type peptidase activity
Specific Function
C1r B chain is a serine protease that combines with C1q and C1s to form C1, the first component of the classical pathway of the complement system.
Gene Name
C1R
Uniprot ID
P00736
Uniprot Name
Complement C1r subcomponent
Molecular Weight
80118.04 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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...
Gene Name
C1QA
Uniprot ID
P02745
Uniprot Name
Complement C1q subcomponent subunit A
Molecular Weight
26016.47 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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...
Gene Name
C1QB
Uniprot ID
P02746
Uniprot Name
Complement C1q subcomponent subunit B
Molecular Weight
26721.62 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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...
Gene Name
C1QC
Uniprot ID
P02747
Uniprot Name
Complement C1q subcomponent subunit C
Molecular Weight
25773.56 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]

Drug created on June 13, 2005 07:24 / Updated on September 18, 2018 23:02