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: Antibody
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:
NameTrade nameCompanyClinical PhaseIndicationsReferences
etanercept-szzsErelziSandozApproved (2016 FDA, 2017 EMA)As per reference agent 
SB4; etanercept-ykroBrenzys; Benepali; Eticovo Samsung BioepisApproved in S Korea (2015), Canada (2016), Europe (EMA 2016), US (FDA 2019) and othersAs per reference agent[1]
 LifmiorPfizerApproved (2017 EMA)As per reference agent 
ENIA11; TuNEX; OpinerceptMycenax BiotechApproved (2018 Taiwan)Rheumatoid arthritisReuters news brief
EtaceptReumatoceptShanghai CP GoujianMarketed in Colombia as Etanar Rheumatoid arthritis 
CHS-0214 Coherus BiosciencesPh 3 (NCT02134210)Plaque psoriasis 
LBEC0101 LG Life SciencesPh 3 (NCT02357069)Rheumatoid arthritis[4-5]
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View more information in the IUPHAR Pharmacology Education Project: etanercept

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).