First time available for research use

TNF-α-inhibitor

Etanercept inhibitor from Enbrel®

Therapeutic TNF-α-inhibitor from the original Enbrel® commercial drug targeting the TNF-α-antigen, also referred to as Enbrel® or etanercept. Research-relevant quantities are available as licence-free consumable in aliquoted or diluted variant. This therapeutic monoclonal inhibitor can be used from researchers in in vitro and in vivo experiments, biosimilar developers can order different batches at the same time.

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Easy Access

Easy Access

Easy to order as license-free research consumable
Multiple batches

Multiple batches

Up to 10 batches of original drugs for examining batch-to-batch variations
Reduce costs

Reduce costs

Up to 80% less compared to the original pharmaceutical price
Prompt delivery

Prompt delivery

Shipment within days worldwide according to GDP-standards
Documented origin

Documented origin

Information on batch, registration number, expiry date, GDP-compliant pedigree

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Etanercept / Enbrel

Product Reference

Drug nameEnbrel®
INNEtanercept
API typeEtanercept is a human tumour necrosis factor receptor p75 Fc fusion protein produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian expression system. Etanercept is a dimer of a chimeric protein genetically engineered by fusing the extracellular ligand binding domain of human tumour necrosis factor receptor-2 (TNFR2/p75) to the Fc domain of human IgG1. This Fc component contains the hinge, CH2and CH3regions, but not the CH1region of IgG1. Etanercept contains 934amino acids and has an apparent molecular weight of approximately 150 kilodaltons. The specific activity of etanercept is 1.7x 106units/mg.
Pharmacotherapeutic group
Immunosuppressants, Tumour Necrosis Factor alpha (TNF-α) inhibitors
ATC code
L04AB01
Target of antibody
TNF-α; Synonyms: DIF, TNF-alpha, TNFA, TNFSF2, RATTNF, Tnfa, tnf, TNF-a, TNFalpha, Tnfsf1a, TNFa, cTNF, Tnf-alpha, tnfa-like, TNF-ALPHA, dif, tnfa, xtnf, tnfsf2, tnf-alpha, Cachectin
General function
Short descriptionTumour necrosis factor (TNF) is a dominant cytokine in the inflammatory process of rheumatoid arthritis. Elevated levels of TNF are also found in the synovium and psoriatic plaques of patients with psoriatic arthritis and in serum and synovial tissue of patients with ankylosing spondylitis. In plaque psoriasis, infiltration by inflammatory cells, including T-cells, leads to increased TNF levels in psoriatic lesions compared with levels in uninvolved skin. Etanercept is a competitive inhibitor of TNF binding to its cell surface receptors, and thereby inhibits the biological activity of TNF. TNF and lymphotoxin are pro-inflammatory cytokines that bind to two distinct cell surface receptors: the 55- kilodalton (p55) and 75-kilodalton (p75) tumour necrosis factor receptors (TNFRs). Both TNFRs exist naturally in membrane-bound and soluble forms. Soluble TNFRs are thought to regulate TNF biological activity.
TNF and lymphotoxin exist predominantly as homotrimers, with their biological activity dependent on cross-linking of cell surface TNFRs. Dimeric soluble receptors, such as etanercept, possess a higher affinity for TNF than monomeric receptors and are considerably more potent competitive inhibitors of TNF binding to its cellular receptors. In addition, use of an immunoglobulin Fc region as a fusion element in the construction of a dimeric receptor imparts a longer serum half-life.
Pharmacodynamic properties
(Mechanism of action; Source EMA document)
Much of the joint pathology in rheumatoid arthritis and ankylosing spondylitis and skin pathology in plaque psoriasis is mediated by pro-inflammatory molecules that are linked in a network controlled by TNF. The mechanism of action of etanercept is thought to be its competitive inhibition of TNF binding to cell surface TNFR, preventing TNF-mediated cellular responses by rendering TNF biologically inactive. Etanercept may also modulate biologic responses controlled by additional downstream molecules (e.g., cytokines, adhesion molecules, or proteinases) that are induced or regulated by TNF.
Pharmacodynamic properties (Pharmacodynamic effects; Source EMA document)
Original license holder
Marketing authorisation numbers
EU/1/99/126/001 - 022
Marketing authorisation holder
Pfizer Limited
Ramsgate Road
Sandwich
Kent CT13 9NJ
United Kingdom
Name of the manufacturer of the biological active substance
Boehringer Ingelheim Pharma KG
Birkendorfer Strasse 65
D-88397 Biberach an der Riss
Germany

Pfizer Ireland Pharmaceuticals
Grange Castle Business Park
Clondalkin
Dublin 22
Ireland
Name and address of the manufacturer(s) responsible for batch releaseWyeth Pharmaceuticals
New Lane
Havant
Hampshire, PO9 2NG
United Kingdom
Max shelf life
48 months
Storage conditions
2°C – 8°C
List of excipients
Powder: Mannitol (E421) Sucrose
Trometamol
Solvent: Water for injections