Lihat sumber Etanersept

{{Infobox drug
| image = Enbrel.jpg
| width = 153
| alt =

<!-- Clinical data -->
| pronounce = 
| tradename = Enbrel
| Drugs.com = {{drugs.com|monograph|etanercept}}
| MedlinePlus = a602013
| DailyMedID = Etanercept
| pregnancy_AU = D
| pregnancy_AU_comment = <ref name="AusPAR: Etanercept" /><ref name="Drugs.com pregnancy">{{cite web | title=Etanercept Use During Pregnancy | website=Drugs.com | date=24 January 2020 | url=https://www.drugs.com/pregnancy/etanercept.html | access-date=13 August 2020}}</ref>
| pregnancy_category =
| routes_of_administration = Subkutan
| class = 
| ATC_prefix = L04
| ATC_suffix = AB01
| ATC_supplemental =
| biosimilars = etanercept-szzs, etanercept-ykro, Benepali,<ref name="Benepali EPAR" /> Brenzys,<ref>{{cite web | title=Health Canada New Drug Authorizations: 2016 Highlights | website=[[Health Canada]] | date=14 March 2017 | url=https://www.canada.ca/en/health-canada/services/publications/drugs-health-products/health-canada-new-drug-authorizations-2016-highlights.html | access-date=7 April 2024}}</ref> Erelzi,<ref name="Erelzi EPAR" /><ref>{{cite web | title=Arthritis | website=[[Health Canada]] | date=8 May 2018 | url=https://www.canada.ca/en/services/health/drug-health-products/drug-medical-device-highlights-2017/approved-drugs/arthritis.html | access-date=13 April 2024}}</ref><ref>{{cite web | title=Regulatory Decision Summary for Erelzi | website=Drug and Health Products Portal | date=6 April 2017 | url=https://dhpp.hpfb-dgpsa.ca/review-documents/resource/RDS00226 | access-date=13 April 2024}}</ref> Etacept, Etera,<ref name="Etera ARTG" /> Eticovo, Lifmior, Nepexto,<ref name="Nepexto EPAR" /> Rymti<ref name="Rymti ARTG" />

<!-- Legal status -->
| legal_AU = S4
| legal_AU_comment = <ref name="Rymti ARTG" /><ref name="Etera ARTG" />
| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F -->
| legal_BR_comment = 
| legal_CA = Rx-only
| legal_CA_comment = /&nbsp;Schedule D<ref>{{cite web | title=Rymti Summary Basis of Decision | website=[[Health Canada]] | date=23 October 2014 | url=https://hpr-rps.hres.ca/reg-content/summary-basis-decision-detailTwo.php?lang=en&linkID=SBD00623&lang=en | access-date=10 March 2023 | archive-date=27 May 2023 | archive-url=https://web.archive.org/web/20230527235856/https://hpr-rps.hres.ca/reg-content/summary-basis-decision-detailTwo.php?lang=en&linkID=SBD00623&lang=en | url-status=dead }}</ref>
| legal_DE = <!-- Anlage I, II, III or Unscheduled -->
| legal_DE_comment = 
| legal_NZ = <!-- Class A, B, C -->
| legal_NZ_comment = 
| legal_UK = POM
| legal_UK_comment = <ref>{{cite web | title=Benepali 25 mg solution for injection in pre-filled syringe - Summary of Product Characteristics (SmPC) | website=(emc) | date=25 January 2021 | url=https://www.medicines.org.uk/emc/product/2708/smpc | access-date=12 June 2021}}</ref><ref>{{cite web | title=Enbrel 25mg solution for injection in pre-filled pen - Summary of Product Characteristics (SmPC) | website=(emc) | date=8 June 2021 | url=https://www.medicines.org.uk/emc/product/11738/smpc | access-date=12 June 2021}}</ref><ref>{{cite web | title=Erelzi 50 mg solution for injection in pre filled pen - Summary of Product Characteristics (SmPC) | website=(emc) | date=25 May 2021 | url=https://www.medicines.org.uk/emc/product/12517/smpc | access-date=12 June 2021}}</ref>
| legal_US = Rx-only
| legal_US_comment = <ref name="Enbrel FDA label">{{cite web | title=Enbrel- etanercept solution Enbrel- etanercept kit | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a002b40c-097d-47a5-957f-7a7b1807af7f | access-date=17 April 2021}}</ref>
| legal_EU = Rx-only
| legal_EU_comment = <ref name="Enbrel EPAR" /><ref name="Nepexto EPAR">{{cite web | title=Nepexto EPAR | website=European Medicines Agency | date=24 March 2020 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/nepexto | access-date=4 March 2023}}</ref><ref>{{cite web | title=Nepexto Product information | website=Union Register of medicinal products | url=https://ec.europa.eu/health/documents/community-register/html/h1436.htm | access-date=3 March 2023}}</ref>
| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV -->
| legal_UN_comment = 
| legal_status = <!-- For countries not listed above -->

<!-- Pharmacokinetic data -->
| bioavailability = 58–76% (subkutan)
| protein_bound = 
| metabolism = 
| metabolites = 
| onset = 
| elimination_half-life = 70–132 jam
| duration_of_action = 
| excretion =

<!-- Identifiers -->
| CAS_number = 185243-69-0
| CAS_supplemental = 
| PubChem = 
| PubChemSubstance = 7847807
| IUPHAR_ligand = 
| DrugBank = DB00005
| ChemSpiderID = None
| UNII = OP401G7OJC
| KEGG = D00742
| ChEBI = 
| ChEMBL = 1201572
| NIAID_ChemDB = 
| PDB_ligand = 
| synonyms = 

<!-- Chemical and physical data -->
| IUPAC_name = 
| C=2224 | H=3475 | N=621 | O=698 | S=36
| SMILES = 
| StdInChI = 
| StdInChI_comment = 
| StdInChIKey = 
| density = 
| density_notes = 
| melting_point = 
| melting_high = 
| melting_notes = 
| boiling_point = 
| boiling_notes = 
| solubility = 
| sol_units = 
| specific_rotation = 
}}

'''Etanersept''' adalah [[biofarmasi|produk medis biologis]] yang digunakan untuk mengobati [[penyakit autoimun]] dengan mengganggu [[faktor nekrosis tumor-alfa]] (TNF-α), sitokin [[radang|inflamasi]] yang larut, dengan bertindak sebagai penghambat TNF. Produk ini telah mendapat persetujuan dari [[Badan Pengawas Obat dan Makanan Amerika Serikat]] (FDA) untuk mengobati [[rheumatoid arthritis]], artritis idiopatik juvenil, dan artritis psoriatis, [[psoriasis]] plak, dan [[ankilosing spodilitis]]. Faktor nekrosis tumor alfa (TNFα) adalah "pengatur utama" respons inflamasi (imun) di banyak sistem organ. Penyakit autoimun disebabkan oleh respons imun yang terlalu aktif. Etanersept berpotensi untuk mengobati penyakit ini dengan menghambat TNF-alfa.<ref name="titleTNF defined as a therapeutic target for rheumatoid arthritis and other autoimmune diseases - Nature Medicine">{{cite journal | vauthors = Feldmann M, Maini RN | title = Lasker Clinical Medical Research Award. TNF defined as a therapeutic target for rheumatoid arthritis and other autoimmune diseases | journal = Nature Medicine | volume = 9 | issue = 10 | pages = 1245–1250 | date = October 2003 | pmid = 14520364 | doi = 10.1038/nm939 | s2cid = 52860838 }}</ref>

Etanersept adalah protein fusi yang diproduksi oleh [[DNA rekombinan]]. Protein ini menggabungkan reseptor TNF dengan ujung konstan antibodi IgG1. Pertama, para pengembang mengisolasi urutan DNA yang mengkode gen manusia untuk reseptor TNF 2 yang larut, yaitu reseptor yang mengikat faktor nekrosis tumor-alfa. Kedua, mereka mengisolasi urutan DNA yang mengkode gen manusia untuk ujung Fc [[antibodi G|imunoglobulin G]]1 (IgG1). Ketiga, mereka menghubungkan DNA untuk reseptor TNF 2 dengan DNA untuk Fc IgG1. Terakhir, mereka mengekspresikan DNA yang terhubung untuk menghasilkan protein yang menghubungkan protein untuk reseptor TNF 2 dengan protein untuk Fc IgG1.<ref>{{Cite web|url=https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=103795|title = Drugs@FDA: FDA-Approved Drugs}}</ref>

Protein fusi prototipe pertama kali disintesis dan terbukti sangat aktif dan sangat stabil sebagai modalitas untuk blokade TNF ''[[in vivo]]'' pada awal tahun 1990-an oleh [[Bruce Beutler|Bruce A. Beutler]], seorang peneliti akademis di [[Universitas Pusat Medis Barat Daya Texas]] di Dallas, dan rekan-rekannya.<ref>{{cite journal | vauthors = Peppel K, Crawford D, Beutler B | title = A tumor necrosis factor (TNF) receptor-IgG heavy chain chimeric protein as a bivalent antagonist of TNF activity | journal = The Journal of Experimental Medicine | volume = 174 | issue = 6 | pages = 1483–1489 | date = December 1991 | pmid = 1660525 | pmc = 2119031 | doi = 10.1084/jem.174.6.1483 }}</ref><ref>{{cite journal | vauthors = Peppel K, Poltorak A, Melhado I, Jirik F, Beutler B | title = Expression of a TNF inhibitor in transgenic mice | journal = Journal of Immunology | volume = 151 | issue = 10 | pages = 5699–5703 | date = November 1993 | pmid = 7693816 | doi = 10.4049/jimmunol.151.10.5699 | s2cid = 10859938 }}</ref>

Para peneliti ini juga mematenkan protein tersebut,<ref>U.S. Patent number: 5,447,851</ref> dan menjual semua hak atas penggunaannya kepada Immunex, sebuah perusahaan bioteknologi Seattle yang diakuisisi oleh [[Amgen]] pada tahun 2002.<ref name="DukeMedNews">{{cite web |url=http://www.dukemednews.org/news/article.php?id=9419 |title=Arthritis Drug Effective for Depression in Psoriasis Sufferers |access-date=10 January 2008 |archive-url=https://web.archive.org/web/20071020205003/http://www.dukemednews.org/news/article.php?id=9419 |archive-date=20 October 2007 |url-status=dead }}</ref>

Protein ini merupakan molekul besar, dengan berat molekul 150 [[dalton (satuan)|dalton]], yang mengikat TNFα dan mengurangi perannya dalam gangguan yang melibatkan peradangan berlebih pada manusia dan hewan lainnya, termasuk penyakit autoimun seperti ankilosing spondilitis,<ref name="pmid17389658">{{cite journal | vauthors = Braun J, McHugh N, Singh A, Wajdula JS, Sato R | title = Improvement in patient-reported outcomes for patients with ankylosing spondylitis treated with etanercept 50 mg once-weekly and 25 mg twice-weekly | journal = Rheumatology | volume = 46 | issue = 6 | pages = 999–1004 | date = June 2007 | pmid = 17389658 | doi = 10.1093/rheumatology/kem069 | doi-access = free }}</ref> rheumatoid arthritis juvenil, psoriasis, arthritis psoriasis, rheumatoid arthritis, dan berpotensi dalam berbagai gangguan lain yang dimediasi oleh kelebihan TNFα. Protein ini tercantum dalam [[Daftar Obat Esensial Organisasi Kesehatan Dunia]].<ref name="WHO21st">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 21st list 2019 | year = 2019 | hdl = 10665/325771 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO | hdl-access=free }}</ref>

==Sejarah==
Paten pertama yang terkait dengan etanersept diajukan oleh Immunex pada bulan September 1989.<ref>{{cite journal | vauthors = Norman P | title = Enbrel and etanercept biosimilars: a tale of two patent systems | journal = Pharmaceutical Patent Analyst | volume = 6 | issue = 1 | pages = 5–7 | date = January 2017 | pmid = 28201948 | doi = 10.4155/ppa-2016-0043 }}</ref> Protein fusi tersebut dikembangkan oleh Bruce A. Beutler, seorang peneliti akademis di Universitas Pusat Medis Barat Daya Texas di Dallas, dan rekan-rekannya, yang mematenkannya dan melisensikan haknya pada tahun 1995 kepada Immunex.<ref>{{cite web | title=A three-decade monopoly: How Amgen built a patent thicket around its top-selling drug | date=1 November 2021 | vauthors = Gardner J | url=https://www.biopharmadive.com/news/amgen-enbrel-patent-thicket-monopoly-biosimilar/609042/}}</ref> Paten lain untuk teknologi protein fusi tersebut dari Brian Seed di [[Rumah Sakit Umum Massachusetts]] dilisensikan kepada Immmunex pada tahun 1997.<ref>{{cite web| vauthors = Kowalczyk L | date=24 March 2002 |title= Lucrative Licensing Deals With Drug, Biotech Firms Are Raising Ethics Issues For Hospitals| url=https://www.sskrplaw.com/lucrative-licensing-deals-with-drug-biotech-firms-are-raising-et.html}}</ref>

Etanersept disetujui untuk digunakan di Amerika Serikat pada bulan November 1998.<ref name="Enbrel FDA label">{{cite web | title=Enbrel- etanercept solution Enbrel- etanercept kit | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a002b40c-097d-47a5-957f-7a7b1807af7f | access-date=17 April 2021}}</ref><ref>{{cite web | title=Etanercept Product Approval Information - Licensing Action 12/2/98 | website=U.S. [[Food and Drug Administration]] (FDA) | date=1 April 2016 | url=https://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/TherapeuticBiologicApplications/ucm080536.htm | archive-url=https://web.archive.org/web/20170118085127/https://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/TherapeuticBiologicApplications/ucm080536.htm | archive-date=18 January 2017 | url-status=dead | access-date=4 June 2020}}</ref>

Etanersept disetujui untuk digunakan di Uni Eropa pada bulan Februari 2000.<ref name="Enbrel EPAR">{{cite web | title=Enbrel EPAR | website=[[European Medicines Agency]] (EMA) | url=https://www.ema.europa.eu/en/medicines/human/EPAR/enbrel | access-date=2 April 2020}} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.</ref>

==Kegunaan dalam medis==
Di Amerika Serikat, etanersept diindikasikan untuk:

*[[Rheumatoid arthritis]] (RA) Sedang hingga Berat (November 1998)<ref name="Enbrel FDA label" /><ref>{{cite letter | vauthors = Siegel YP | recipient = Sally Gould | subject = Approval of Etanercept for treatment of rheumatoid arthritis | date = 2 November 1998 | access-date = 14 April 2015 | url = https://www.fda.gov/downloads/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/TherapeuticBiologicApplications/ucm088659.pdf | publisher = U.S. [[Food and Drug Administration]] (FDA)}}</ref>
*Rheumatoid arthritis juvenil Poliartikular Sedang hingga Berat (Mei 1999)<ref name="Enbrel FDA label" /><ref>{{cite letter | vauthors = Weiss KD | recipient = Sally Gould | subject = Approval of Etanercept for treatment of polyarticular course juvenile rheumatoid arthritis (JRA) | date = 27 May 1999 | access-date = 14 April 2015 | url = https://www.fda.gov/downloads/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/TherapeuticBiologicApplications/ucm088844.pdf | publisher = U.S. [[Food and Drug Administration]] (FDA)}}</ref>
*Arthritis Psoriasis (Januari 2002)<ref name="Enbrel FDA label" /><ref>{{cite letter | vauthors = Weiss KD | recipient = Sally Gould | subject = Approval of Etanercept for treatment of psoriatic arthritis | date = 15 January 2002 | access-date = 14 April 2015 | url = http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2002/etanimm011502L.htm | publisher = U.S. [[Food and Drug Administration]] (FDA)}}</ref>
*[[Ankilosing spodilitis]] (AS) (Juli 2003)<ref name="Enbrel FDA label" /><ref>{{cite letter | vauthors = Keegan P | recipient = Douglas Hunt | subject = Approval of Etanercept for treatment of ankylosing spondylitis | date = 24 July 2003 | access-date = 14 April 2015 | url = http://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/103795-5123_Enbrel_approv.pdf | publisher = U.S. [[Food and Drug Administration]] (FDA)}}</ref><ref>{{cite journal | vauthors = Maxwell LJ, Zochling J, Boonen A, Singh JA, Veras MM, Tanjong Ghogomu E, Benkhalti Jandu M, Tugwell P, Wells GA | display-authors = 6 | title = TNF-alpha inhibitors for ankylosing spondylitis | journal = The Cochrane Database of Systematic Reviews | volume = 2015 | issue = 4 | pages = CD005468 | date = April 2015 | pmid = 25887212 | doi = 10.1002/14651858.CD005468.pub2 | pmc = 11200207 }}</ref>
*[[Psoriasis]] Plak Sedang hingga Berat (April 2004)<ref name="Enbrel FDA label" /><ref>{{cite letter | vauthors = Walton M | recipient = Douglas Hunt | subject = Approval of Etanercept for treatment of moderate to severe plaque psoriasis | date = 30 April 2004 | access-date = 14 April 2015 | url = http://www.accessdata.fda.gov/drugsatfda_docs/appletter/biologics/2004/103795_5149ltr.pdf | publisher = U.S. [[Food and Drug Administration]] (FDA)}}</ref>

Di Uni Eropa, etanersept diindikasikan untuk mengobati:

*Rheumatoid arthritis aktif sedang hingga berat<ref name="Enbrel EPAR" />
*Rheumatoid arthritis berat, aktif, dan progresif<ref name="Enbrel EPAR" />
*Artritis idiopatik juvenil<ref name="Enbrel EPAR" />
*Poliartritis (faktor rheumatoid positif atau negatif) dan oligoartritis yang meluas pada anak-anak dan remaja<ref name="Enbrel EPAR" />
*artritis psoriatis aktif dan progresif<ref name="Enbrel EPAR" />
*artritis terkait entesitis
*spondiloartritis aksial<ref name="Enbrel EPAR" />
*spondilitis ankilosa aktif yang parah<ref name="Enbrel EPAR" />
*spondiloartritis aksial non-radiografik yang parah<ref name="Enbrel EPAR" />
*psoriasis plak sedang hingga parah<ref name="Enbrel EPAR" />
*psoriasis plak kronis parah psoriasis plak pediatrik<ref name="Enbrel EPAR" />

===Penggunaan yang tidak diketahui===
Seorang dokter Amerika Serikat, Edward Tobinick, telah mencoba menggunakan etanersept untuk mengobati disfungsi neurologis kronis setelah [[strok]] dan cedera otak<ref>{{cite news |publisher=Springer Select |date=31 October 2012 |title=New hope for survivors of stroke and traumatic brain injury | url=https://www.springer.com/about+springer/media/springer+select?SGWID=0-11001-6-1394543-0 |access-date=17 November 2018 }}</ref> dan telah mengeluarkan paten AS<ref>{{Cite patent|country=US|number=8900583|title=Methods for treatment of brain injury utilizing biologics|inventor = Tobinick EL |pubdate=2014-12-02}}</ref> dan asing. Dalam tulisannya untuk ''Science-Based Medicine'', Steven Novella mengatakan bahwa "tidak etis bagi dokter untuk berpraktik di luar area kompetensi dan keahlian mereka". Tobinick menggugat Novella sebagai tanggapan, dan kalah.<ref>{{Cite web |date=24 February 2017 |title=Another Free Speech Win In Libel Lawsuit Disguised As A Trademark Complaint |url=https://abovethelaw.com/2017/02/another-free-speech-win-in-libel-lawsuit-disguised-as-a-trademark-complaint/ |access-date=27 June 2022 |website=Above the Law |language=en-US}}</ref> Mengenai pengobatan ini, ''American Academy of Neurology'' menyarankan "tidak ada cukup bukti untuk menentukan efektivitasnya dan bahwa pengobatan tersebut mungkin dikaitkan dengan hasil yang buruk dan biaya yang tinggi".<ref name=aan>{{cite web |publisher=American Academy of Neurology |title=Practice Advisory: Etanercept for Poststroke Disability |url=https://www.aan.com/Guidelines/home/GetGuidelineContent/747 |date=6 June 2016 |format=pdf}}</ref>

==Efek samping==
Pada tanggal 2 Mei 2008, [[Badan Pengawas Obat dan Makanan Amerika Serikat]] (FDA) memberikan peringatan kotak hitam pada etanersept karena sejumlah infeksi serius yang terkait dengan obat tersebut.<ref name="Wyeth and Amgen">{{cite web|url=https://money.cnn.com/news/newsfeeds/articles/apwire/21965cf0a650a8b5897142bfcbccb427.htm |title=Wyeth and Amgen heighten warning of life-threatening infections on skin drug Enbrel |access-date=2 May 2008 |archive-url=https://web.archive.org/web/20080505133653/https://money.cnn.com/news/newsfeeds/articles/apwire/21965cf0a650a8b5897142bfcbccb427.htm |archive-date=5 May 2008 |url-status=dead }}</ref> Infeksi serius dan [[sepsis]] termasuk kematian, telah dilaporkan akibat penggunaan etanersept termasuk reaktivasi infeksi tuberkulosis laten dan [[hepatitis B]].<ref name="Enbrel FDA label" /><ref name="FDAReport">{{cite conference | url=https://www.fda.gov/ohrms/dockets/ac/01/briefing/3779b2_01_cber_safety%20_revision2.pdf | title=Safety Update on TNF- α Antagonists: Infliximab and Etanercept | publisher=U.S. [[Food and Drug Administration]] (FDA) | access-date=20 December 2013 | pages=13–14 | conference= | archive-date=24 September 2015 | archive-url=https://web.archive.org/web/20150924170456/http://www.fda.gov/ohrms/dockets/ac/01/briefing/3779b2_01_cber_safety%20_revision2.pdf | url-status=dead }}</ref>

Reaksi di tempat suntikan seperti kemerahan dan nyeri adalah hal yang umum, terjadi pada sekitar 11,4% kasus.<ref name="PMID37533141">{{cite journal | vauthors = Kim PJ, Lansang RP, Vender R | title = A Systematic Review and Meta-Analysis of Injection Site Reactions in Randomized-Controlled Trials of Biologic Injections | journal = Journal of Cutaneous Medicine and Surgery | volume = 27 | issue = 4 | pages = 358–367 | date = July 2023 | pmid = 37533141 | doi = 10.1177/12034754231188444 | pmc = 10486173 }}</ref>

==Mekanisme kerja==
Etanersept mengurangi efek TNF yang ada secara alami, dan karenanya merupakan penghambat TNF, yang berfungsi sebagai reseptor umpan yang mengikat TNF.<ref>{{cite journal | vauthors = Zalevsky J, Secher T, Ezhevsky SA, Janot L, Steed PM, O'Brien C, Eivazi A, Kung J, Nguyen DH, Doberstein SK, Erard F, Ryffel B, Szymkowski DE | display-authors = 6 | title = Dominant-negative inhibitors of soluble TNF attenuate experimental arthritis without suppressing innate immunity to infection | journal = Journal of Immunology | volume = 179 | issue = 3 | pages = 1872–1883 | date = August 2007 | pmid = 17641054 | doi = 10.4049/jimmunol.179.3.1872 | doi-access = free }}</ref>

Faktor nekrosis tumor-alfa (TNFα) adalah [[sitokin]] yang diproduksi oleh [[limfosit]] dan [[makrofag]], dua jenis [[sel darah putih]]. Ia memediasi respons imun dengan menarik sel darah putih tambahan ke lokasi peradangan dan melalui mekanisme molekuler tambahan yang memulai dan memperkuat peradangan. Penghambatan aksinya oleh etanersept mengurangi respons peradangan, yang sangat berguna untuk mengobati penyakit autoimun.

Ada dua jenis [[reseptor (biokimia)|reseptor]] TNF: yang ditemukan tertanam dalam sel darah putih yang merespons TNF dengan melepaskan sitokin lain, dan reseptor TNF terlarut yang digunakan untuk menonaktifkan TNF dan menumpulkan respons imun. Selain itu, reseptor TNF ditemukan pada permukaan hampir semua sel berinti (sel darah merah, yang tidak berinti, tidak mengandung reseptor TNF pada permukaannya). Etanersept meniru efek penghambatan reseptor TNF terlarut yang terjadi secara alami, perbedaannya adalah etanersept, karena merupakan protein fusi dan bukan reseptor TNF sederhana, memiliki waktu paruh yang jauh lebih lama di aliran darah, dan oleh karena itu efek biologisnya lebih mendalam dan tahan lama daripada reseptor TNF terlarut yang terjadi secara alami.<ref name="pmid16135466">{{cite journal | vauthors = Madhusudan S, Muthuramalingam SR, Braybrooke JP, Wilner S, Kaur K, Han C, Hoare S, Balkwill F, Ganesan TS | display-authors = 6 | title = Study of etanercept, a tumor necrosis factor-alpha inhibitor, in recurrent ovarian cancer | journal = Journal of Clinical Oncology | volume = 23 | issue = 25 | pages = 5950–5959 | date = September 2005 | pmid = 16135466 | doi = 10.1200/JCO.2005.04.127 }}</ref>

==Struktur==
Etanersept dibuat dari kombinasi dua reseptor TNF manusia 75 kilodalton yang larut secara alami yang dihubungkan ke bagian Fc dari IgG1.<ref name="pmid1936291">{{cite journal | vauthors = Smola MG, Soyer HP, Scharnagl E | title = Surgical treatment of dermatofibrosarcoma protuberans. A retrospective study of 20 cases with review of literature | journal = European Journal of Surgical Oncology | volume = 17 | issue = 5 | pages = 447–453 | date = October 1991 | pmid = 1936291 }}</ref> Efeknya adalah protein fusi dimerik yang direkayasa secara artifisial.<ref name="pmid1936291" /> Etanersept adalah molekul kompleks yang mengandung 6 N-glikana, hingga 14 O-glikana dan 29 struktur jembatan disulfida.<ref>{{cite journal | vauthors = Houel S, Hilliard M, Yu YQ, McLoughlin N, Martin SM, Rudd PM, Williams JP, Chen W | display-authors = 6 | title = N- and O-glycosylation analysis of etanercept using liquid chromatography and quadrupole time-of-flight mass spectrometry equipped with electron-transfer dissociation functionality | journal = Analytical Chemistry | volume = 86 | issue = 1 | pages = 576–584 | date = January 2014 | pmid = 24308717 | doi = 10.1021/ac402726h }}</ref><ref>{{cite journal | vauthors = Mukai Y, Nakamura T, Yoshikawa M, Yoshioka Y, Tsunoda S, Nakagawa S, Yamagata Y, Tsutsumi Y | display-authors = 6 | title = Solution of the structure of the TNF-TNFR2 complex | journal = Science Signaling | volume = 3 | issue = 148 | pages = ra83 | date = November 2010 | pmid = 21081755 | doi = 10.1126/scisignal.2000954 | s2cid = 24226117 }}</ref><ref name=":0">{{cite journal | vauthors = Lamanna WC, Mayer RE, Rupprechter A, Fuchs M, Higel F, Fritsch C, Vogelsang C, Seidl A, Toll H, Schiestl M, Holzmann J | display-authors = 6 | title = The structure-function relationship of disulfide bonds in etanercept | journal = Scientific Reports | volume = 7 | issue = 1 | pages = 3951 | date = June 2017 | pmid = 28638112 | pmc = 5479810 | doi = 10.1038/s41598-017-04320-5 | bibcode = 2017NatSR...7.3951L }}</ref>

==Dalam budaya masyarakat==
===Ekonomi===
Harga eceran etanersept di AS telah meningkat dari waktu ke waktu. Pada tahun 2008, biaya etanersept adalah $1.500 per bulan atau $18.000 per tahun.<ref>[http://seattletimes.com/html/health/2008120449_drugs18m.html "What's behind the whopping price tags on the newest generation of drugs:] The story behind the production of Enbrel, Amgen's popular rheumatoid arthritis drug, provides insights as to why bioengineered drugs are so expensive."  Carol M. Ostrom, Seattle Times, 18 August 2008</ref> Pada tahun 2011, biaya tersebut telah melampaui $20.000 per tahun.<ref name="NYTAmgen2011">{{cite news | title=Amgen's New Enbrel Patent May Undercut Health Care Plan | website=The New York Times | date=23 November 2011 | url=https://www.nytimes.com/2011/11/23/business/amgens-new-enbrel-patent-may-undercut-health-care-plan.html | access-date=10 March 2023 | vauthors = Pollock A }}</ref><ref>[http://bostonherald.com/news/columnists/view/2011_1103painful_reality "Co-pay hike a painful reality; Miracle drug monthly cost jumps from $42 to $600"] {{Webarchive|url=https://archive.today/20130118110008/http://bostonherald.com/news/columnists/view/2011_1103painful_reality |date=18 January 2013 }}, Margery Eagan, Boston Herald, 3 November 2011</ref> Pada tahun 2013, sebuah survei oleh ''International Federation of Health Plans'' (IFHP) menemukan bahwa biaya rata-rata etanersept di AS adalah $2.225 per bulan, atau $26.700 per tahun. Laporan IFHP juga menemukan variasi yang luas dalam harga yang dikenakan pada berbagai rencana kesehatan AS, antara $1.946 per bulan pada persentil ke-25 dan $4.006 per bulan pada persentil ke-95.<ref name="IFHP2013">{{cite web |url=https://static1.squarespace.com/static/518a3cfee4b0a77d03a62c98/t/534fc9ebe4b05a88e5fbab70/1397737963288/2013+iFHP+FINAL+4+14+14.pdf |title=2013 Comparative Price Report |publisher=International Federation of Health Plans |access-date=24 November 2017 |archive-date=22 October 2017 |archive-url=https://web.archive.org/web/20171022020959/http://static1.squarespace.com/static/518a3cfee4b0a77d03a62c98/t/534fc9ebe4b05a88e5fbab70/1397737963288/2013+iFHP+FINAL+4+14+14.pdf |url-status=dead }}</ref>

Etanersept lebih mahal di AS dibandingkan di negara lain. Pada tahun 2013, biaya bulanan rata-rata di negara-negara yang disurvei berkisar antara $1.017 di Swiss hingga $1.646 di Kanada, dibandingkan dengan biaya bulanan rata-rata $2.225 per bulan di AS.<ref name="IFHP2013"/>

Amgen menjual etanersept di AS dan Kanada; sementara [[Pfizer]], Inc. menjual obat tersebut di luar AS dan Kanada. Penjualan di AS dan Kanada mencapai $3,5 miliar pada tahun 2010.<ref name="NYTAmgen2011" /> Penjualan etanersept di luar AS dan Kanada mencapai $3,3 miliar pada tahun 2010.<ref>{{cite web|url=https://www.sec.gov/Archives/edgar/data/78003/000119312511048877/dex13.htm |title=Portions of the 2010 Financial Report |publisher=Sec.gov |access-date=5 June 2019}}</ref>

===Paten===
Paten etanersept akan berakhir pada bulan Oktober 2012,<ref>{{cite web | url=http://www.uspto.gov/patents/resources/terms/156.html | title=Patent Terms Extended Under 35 USC §156 | access-date=9 December 2009 | archive-date=24 February 2010 | archive-url=https://web.archive.org/web/20100224023842/http://www.uspto.gov/patents/resources/terms/156.html | url-status=dead }}</ref> tetapi di Amerika Serikat, paten kedua yang memberikan eksklusivitas selama 16 tahun lagi, telah diberikan.<ref>{{cite web | url=http://www.gabionline.net/Biosimilars/News/New-Amgen-Enbrel-patent-could-block-biosimilars-until-2028 | title=New Amgen Enbrel patent could block biosimilars until 2028 | date=25 November 2011 | access-date=14 July 2019}}</ref>

Sebelum perpanjangan, tampaknya tidak mungkin obat generik akan tersedia. Sebagai obat biologis, etanersept tunduk pada hukum yang berbeda dari yang berlaku untuk formulasi kimia. Banyak negara tidak mengizinkan pembuatan biologika generik. Akan tetapi, Uni Eropa dan Amerika Serikat (''[https://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/TherapeuticBiologicApplications/Biosimilars/ Biologics Price Competition and Innovation Act of 2009]'') memiliki sistem untuk menyetujui biologika generik (biosimilar) yang "memerlukan pengujian klinis wajib dan tinjauan berkala".<ref>{{cite web|url=https://scholarship.law.duke.edu/cgi/viewcontent.cgi?referer=https://en.wiki-indonesia.club/&httpsredir=1&article=1184&context=dltr |title=The Future of Generic Biologics: Should the United States "Follow-On" the European Pathway? | vauthors = Kaldre I |date=2008 |website=www.law.duke.edu |access-date=5 June 2019}}</ref>

Pada bulan April 2013, perusahaan farmasi besar asal India, [[Cipla]], mengumumkan peluncuran biosimilar pertama Etanersept di India dengan nama merek Etacept untuk pengobatan gangguan rematik.<ref>{{cite web |url=http://www.cipla.com/CiplaSite/Media/PDF/News-Archives/Press-Release-Launch-of-first-biosimilar-of-Etanercept-in-India.pdf?ext=.pdf |title=Cipla - Home |publisher=Cipla.com |access-date=5 June 2019 |archive-date=1 May 2013 |archive-url=https://web.archive.org/web/20130501202841/http://www.cipla.com/CiplaSite/Media/PDF/News-Archives/Press-Release-Launch-of-first-biosimilar-of-Etanercept-in-India.pdf?ext=.pdf |url-status=dead }}</ref>

===Biosimilar===
Pada bulan Januari 2016, Benepali disetujui untuk digunakan di Uni Eropa.<ref name="Benepali EPAR">{{cite web | title=Benepali EPAR | website=[[European Medicines Agency]] (EMA) | url=https://www.ema.europa.eu/en/medicines/human/EPAR/benepali | access-date=2 April 2020}}</ref>

Pada bulan Februari 2017, Lifmior disetujui untuk digunakan di Uni Eropa.<ref>{{cite web | title=Lifmior EPAR | website=[[European Medicines Agency]] (EMA) | url=https://www.ema.europa.eu/en/medicines/human/EPAR/lifmior | access-date=2 April 2020}}</ref> Obat ini ditarik dari pasaran pada bulan Februari 2020.<ref>{{cite web | title=Public statement on Lifmior: Withdrawal of the marketing authorisation in the European Union | url=https://www.ema.europa.eu/documents/public-statement/public-statement-lifmior-withdrawal-marketing-authorisation-european-union_en.pdf | access-date=2 April 2020}}</ref>

Pada bulan Juni 2017, Erelzi disetujui untuk digunakan di Uni Eropa.<ref name="Erelzi EPAR">{{cite web | title=Erelzi EPAR | website=[[European Medicines Agency]] (EMA) | url=https://www.ema.europa.eu/en/medicines/human/EPAR/erelzi | access-date=2 April 2020}}</ref>

Pada bulan Maret 2019, YLB113 (Biosimilar etanersept oleh YL Biologics) disetujui di Jepang.<ref>{{Cite web|title=Japanese approval for Lupin's etanercept biosimilar|url=https://www.gabionline.net/biosimilars/news/Japanese-approval-for-Lupin-s-etanercept-biosimilar}}</ref>

Pada bulan April 2019, Eticovo menerima persetujuan FDA.<ref>{{cite web | title=Drug Approval Package: Eticovo | website=U.S. [[Food and Drug Administration]] (FDA) | date=18 June 2019 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/761066Orig1s000TOC.cfm | access-date=26 September 2024}}</ref><ref>{{Cite web |title=FDA approves etanercept biosimilar Eticovo |url=https://www.gabionline.net/biosimilars/news/FDA-approves-etanercept-biosimilar-Eticovo |access-date=16 July 2024 |website=www.gabionline.net }}</ref>

Pada bulan Mei 2020, Nepexto disetujui untuk digunakan di Uni Eropa.<ref name="Nepexto EPAR">{{cite web | title=Nepexto EPAR | website=European Medicines Agency | date=24 March 2020 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/nepexto | access-date=4 March 2023}}</ref>

Rymti dan Etera disetujui untuk penggunaan medis di Australia pada bulan Oktober 2020.<ref name="AusPAR: Etanercept">{{cite web | title=Australian Public Assessment Report for Etanercept | date= Feb 2021 | url=https://www.tga.gov.au/sites/default/files/auspar-etanercept-210224.pdf }}</ref><ref>{{cite web | title=AusPAR: Etanercept | website=[[Therapeutic Goods Administration]] (TGA) | date=25 February 2021 | url=https://www.tga.gov.au/auspar/auspar-etanercept-3 | access-date=12 June 2021}}</ref><ref name="Rymti ARTG">{{cite web | title=Rymti ARTG | website=[[Therapeutic Goods Administration]] (TGA) | url=https://tga-search.clients.funnelback.com/s/search.html?collection=tga-artg&profile=record&meta_i=309830 | access-date=12 June 2021 | archive-date=13 June 2021 | archive-url=https://web.archive.org/web/20210613063803/https://tga-search.clients.funnelback.com/s/search.html?collection=tga-artg&profile=record&meta_i=309830 | url-status=dead }}</ref><ref name="Etera ARTG">{{cite web | title=Etera ARTG | website=[[Therapeutic Goods Administration]] (TGA) | url=https://tga-search.clients.funnelback.com/s/search.html?collection=tga-artg&profile=record&meta_i=309829 | access-date=12 June 2021 | archive-date=13 June 2021 | archive-url=https://web.archive.org/web/20210613063806/https://tga-search.clients.funnelback.com/s/search.html?collection=tga-artg&profile=record&meta_i=309829 | url-status=dead }}</ref>

==Referensi==
{{reflist}}

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