etanercept

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Ligands
etanercept

GtoPdb Ligand ID: 6789

Synonyms: Enbrel® | Rhu Tnfr:Fc | TNFR-Fc | TNR 001

etanercept is an approved drug (FDA (1998), EMA (2000))

Compound class: Peptide or derivative

Comment: Etanercept is a TNFα inhibitor. It is a dimeric recombinant protein fusing the TNF receptor 2 (TNFRSF1B) to the Fc region of the human IgG1 antibody. Etanercept is used as a disease-modifying anti-rheumatic drug (DMARD).

Biosimilars:

Name	Trade name	Company	Clinical Phase	Indications	References
etanercept-szzs	Erelzi	Sandoz	Approved (2016 FDA, 2017 EMA)	As per reference agent
SB4; etanercept-ykro	Brenzys; Benepali; Eticovo	Samsung Bioepis	Approved in S Korea (2015), Canada (2016), Europe (EMA 2016), US (FDA 2019) and others	As per reference agent	[1]
	Lifmior	Pfizer	Approved (2017 EMA)	As per reference agent
ENIA11;	TuNEX; Opinercept	Mycenax Biotech	Approved (2018 Taiwan)	Rheumatoid arthritis	Reuters news brief
YLB113	Nepexto	Mylan	Approved (2020 EMA)	As per reference agent
Etacept	Reumatocept	Shanghai CP Goujian	Marketed in Colombia as Etanar	Rheumatoid arthritis
CHS-0214		Coherus Biosciences	Ph 3 (NCT02134210)	Plaque psoriasis
LBEC0101		LG Life Sciences	Ph 3 (NCT02357069)	Rheumatoid arthritis	[4-5]

View more information in the IUPHAR Pharmacology Education Project: etanercept

Peptide Sequence
LPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSDTVCDSCEDSTYTQLWNWVPECLSCGSRCSS DQVETQACTREQNRICTCRPGWYCALSKQEGCRLCAPLRKCRPGFGVARPGTETSDVVCKPCAPGTFSNTTSSTDICRPH QICNVVAIPGNASMDAVCTSTSPTRSMAPGAVHLPQPVSTRSQHTQPTPEPSTAPSTSFLLPMGPSPPAEGSTGDEPKSC DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPQVKFNWYVDGVQVHNAKTKPREQQYNSTY RVVSVLTVLHQNWLDGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVE WESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK

Peptide Sequence

LPAQVAFTPYAPEPGSTCRLREYYDQTAQMCCSKCSPGQHAKVFCTKTSDTVCDSCEDSTYTQLWNWVPECLSCGSRCSS
DQVETQACTREQNRICTCRPGWYCALSKQEGCRLCAPLRKCRPGFGVARPGTETSDVVCKPCAPGTFSNTTSSTDICRPH
QICNVVAIPGNASMDAVCTSTSPTRSMAPGAVHLPQPVSTRSQHTQPTPEPSTAPSTSFLLPMGPSPPAEGSTGDEPKSC
DKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPQVKFNWYVDGVQVHNAKTKPREQQYNSTY
RVVSVLTVLHQNWLDGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVE
WESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK

Chemical Modification
This is a recombinant fusion protein combining the extracellular ligand-binding portion of the human tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1 (CH2 and CH3 domains and hinge region).