Etanercept

DB00005

biotech approved investigational

Deskripsi

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.L14862,A216522 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. It is used to treat or manage a variety of inflammatory conditions including rheumatoid arthritis (RA), ankylosing spondylitis (AS), and juvenile idiopathic poly-articular arthritis (JIA).

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Etanercept has a mean half-life of elimination of 102 hours in RA patients.[L14862] Population models have shown a mean half-life of 68 hours in healthy adults and 70.7-94.8 hours in pediatric JIA patients.[A215657,A215357]
Volume Distribusi Population pharmacokinetic modeling predicts a total Vd of 5.49 L with a peripheral compartment of 1.24 L in adults with RA and an apparent Vd with subcutaneous administration in pediatric JIA patients of 7.88 L.[A215352,A215357]
Klirens (Clearance) Etanercept has a mean apparent clearance of 160 mL/h in RA patients.[L14862] Population models predict a mean apparent clearance of 132 mL/h in healthy adults and 0.0576 L/h in pediatric JIA patients.[A215657,A215357]

Absorpsi

Population pharmacokinetic modeling in adults with RA, AS, or who were healthy showed a subcutaneous bioavailability of 56.9% with a Ka of 0.0223/h.A215352 Another model in pediatric JIA patients showed an increased Ka of 0.05/h with a high mean interindividual variability of 215%.A215357 Cmax after a single 25 mg subcutaneous dose of Enbrel is reported as 1.1 mcg/L with a Tmax of 69 h.L14862 Cmax after repeated dosing is reported as 2.4 mcg/L in adult RA patients with a dosage of 25 mg twice weekly and 2.1 mcg in pediatric JIA patients with a dosage of 0.4 mg/kg twice weekly.

Metabolisme

As etanercept is a fusion protein antibody, it is assumed to be metabolized via proteinases similarly to endogenous proteins.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

1028 Data
Belimumab The risk or severity of adverse effects can be increased when Etanercept is combined with Belimumab.
Cyclophosphamide The risk or severity of adverse effects can be increased when Etanercept is combined with Cyclophosphamide.
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Etanercept.
Infliximab Etanercept may increase the immunosuppressive activities of Infliximab.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Etanercept is combined with Peginterferon alfa-2a.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon alfa-n1.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon alfa-n3.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Etanercept is combined with Peginterferon alfa-2b.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon gamma-1b.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon alfa-2a.
Aldesleukin The risk or severity of adverse effects can be increased when Etanercept is combined with Aldesleukin.
Adalimumab The risk or severity of infection can be increased when Adalimumab is combined with Etanercept.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Etanercept is combined with Gemtuzumab ozogamicin.
Pegaspargase The risk or severity of adverse effects can be increased when Etanercept is combined with Pegaspargase.
Interferon beta-1b The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon beta-1b.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon alfacon-1.
Rituximab The risk or severity of adverse effects can be increased when Etanercept is combined with Rituximab.
Basiliximab The risk or severity of adverse effects can be increased when Etanercept is combined with Basiliximab.
Muromonab The risk or severity of adverse effects can be increased when Etanercept is combined with Muromonab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Etanercept is combined with Ibritumomab tiuxetan.
Tositumomab The risk or severity of adverse effects can be increased when Etanercept is combined with Tositumomab.
Alemtuzumab The risk or severity of adverse effects can be increased when Etanercept is combined with Alemtuzumab.
Alefacept The risk or severity of adverse effects can be increased when Etanercept is combined with Alefacept.
Efalizumab The risk or severity of adverse effects can be increased when Etanercept is combined with Efalizumab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Etanercept is combined with Antithymocyte immunoglobulin (rabbit).
Interferon alfa-2b The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon alfa-2b.
Daclizumab The risk or severity of adverse effects can be increased when Etanercept is combined with Daclizumab.
Phenylalanine The risk or severity of adverse effects can be increased when Etanercept is combined with Phenylalanine.
Cladribine Etanercept may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Etanercept is combined with Amsacrine.
Bleomycin The risk or severity of adverse effects can be increased when Etanercept is combined with Bleomycin.
Chlorambucil The risk or severity of adverse effects can be increased when Etanercept is combined with Chlorambucil.
Raltitrexed The risk or severity of adverse effects can be increased when Etanercept is combined with Raltitrexed.
Mitomycin The risk or severity of adverse effects can be increased when Etanercept is combined with Mitomycin.
Floxuridine The risk or severity of adverse effects can be increased when Etanercept is combined with Floxuridine.
Tioguanine The risk or severity of adverse effects can be increased when Etanercept is combined with Tioguanine.
Dexrazoxane The risk or severity of adverse effects can be increased when Etanercept is combined with Dexrazoxane.
Streptozocin The risk or severity of adverse effects can be increased when Etanercept is combined with Streptozocin.
Trifluridine The risk or severity of adverse effects can be increased when Etanercept is combined with Trifluridine.
Gemcitabine The risk or severity of adverse effects can be increased when Etanercept is combined with Gemcitabine.
Epirubicin The risk or severity of adverse effects can be increased when Etanercept is combined with Epirubicin.
Chloramphenicol The risk or severity of adverse effects can be increased when Etanercept is combined with Chloramphenicol.
Lenalidomide The risk or severity of adverse effects can be increased when Etanercept is combined with Lenalidomide.
Altretamine The risk or severity of adverse effects can be increased when Etanercept is combined with Altretamine.
Cisplatin The risk or severity of adverse effects can be increased when Etanercept is combined with Cisplatin.
Oxaliplatin The risk or severity of adverse effects can be increased when Etanercept is combined with Oxaliplatin.
Propylthiouracil The risk or severity of adverse effects can be increased when Etanercept is combined with Propylthiouracil.
Pentostatin The risk or severity of adverse effects can be increased when Etanercept is combined with Pentostatin.
Linezolid The risk or severity of adverse effects can be increased when Etanercept is combined with Linezolid.
Clofarabine The risk or severity of adverse effects can be increased when Etanercept is combined with Clofarabine.
Methimazole The risk or severity of adverse effects can be increased when Etanercept is combined with Methimazole.
Temozolomide The risk or severity of adverse effects can be increased when Etanercept is combined with Temozolomide.
Penicillamine The risk or severity of adverse effects can be increased when Etanercept is combined with Penicillamine.
Mechlorethamine The risk or severity of adverse effects can be increased when Etanercept is combined with Mechlorethamine.
Azacitidine The risk or severity of adverse effects can be increased when Etanercept is combined with Azacitidine.
Carboplatin The risk or severity of adverse effects can be increased when Etanercept is combined with Carboplatin.
Dactinomycin The risk or severity of adverse effects can be increased when Etanercept is combined with Dactinomycin.
Hydroxyurea The risk or severity of adverse effects can be increased when Etanercept is combined with Hydroxyurea.
Mycophenolic acid The risk or severity of adverse effects can be increased when Etanercept is combined with Mycophenolic acid.
Topotecan The risk or severity of adverse effects can be increased when Etanercept is combined with Topotecan.
Mercaptopurine The risk or severity of adverse effects can be increased when Etanercept is combined with Mercaptopurine.
Melphalan The risk or severity of adverse effects can be increased when Etanercept is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Etanercept is combined with Fludarabine.
Flucytosine The risk or severity of adverse effects can be increased when Etanercept is combined with Flucytosine.
Procarbazine The risk or severity of adverse effects can be increased when Etanercept is combined with Procarbazine.
Arsenic trioxide The risk or severity of adverse effects can be increased when Etanercept is combined with Arsenic trioxide.
Mitoxantrone The risk or severity of adverse effects can be increased when Etanercept is combined with Mitoxantrone.
Lomustine The risk or severity of adverse effects can be increased when Etanercept is combined with Lomustine.
Eculizumab The risk or severity of adverse effects can be increased when Etanercept is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Etanercept is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Etanercept is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Etanercept is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Etanercept is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Etanercept is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Etanercept is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Etanercept is combined with Brequinar.
Afelimomab The risk or severity of adverse effects can be increased when Etanercept is combined with Afelimomab.
Interferon alfa The risk or severity of adverse effects can be increased when Etanercept is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Etanercept is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Etanercept is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Etanercept is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Etanercept is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Etanercept is combined with Abetimus.
Golimumab The risk or severity of adverse effects can be increased when Etanercept is combined with Golimumab.
Belatacept The risk or severity of adverse effects can be increased when Etanercept is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Etanercept is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Etanercept is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Etanercept is combined with Eribulin.
Teriflunomide The risk or severity of adverse effects can be increased when Etanercept is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Etanercept is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Etanercept is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Etanercept is combined with Obinutuzumab.
Secukinumab The risk or severity of adverse effects can be increased when Etanercept is combined with Secukinumab.
Siltuximab The risk or severity of adverse effects can be increased when Etanercept is combined with Siltuximab.
Blinatumomab The risk or severity of adverse effects can be increased when Etanercept is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Etanercept is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Etanercept is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Etanercept is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Etanercept is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Etanercept is combined with Tepoxalin.

Target Protein

Tumor necrosis factor TNF
Lymphotoxin-alpha LTA
High affinity immunoglobulin gamma Fc receptor I FCGR1A
Low affinity immunoglobulin gamma Fc region receptor II-a FCGR2A
Low affinity immunoglobulin gamma Fc region receptor II-b FCGR2B
Low affinity immunoglobulin gamma Fc region receptor II-c FCGR2C
Low affinity immunoglobulin gamma Fc region receptor III-A FCGR3A
Low affinity immunoglobulin gamma Fc region receptor III-B FCGR3B
Complement component 1q (C1q) C1QA

Referensi & Sumber

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.
Artikel (PubMed)
  • PMID: 27463856
    Hofmann HP, Kronthaler U, Fritsch C, Grau R, Muller SO, Mayer R, Seidl A, Da Silva A: Characterization and non-clinical assessment of the proposed etanercept biosimilar GP2015 with originator etanercept (Enbrel((R))). Expert Opin Biol Ther. 2016 Oct;16(10):1185-95. doi: 10.1080/14712598.2016.1217329. Epub 2016 Aug 16.
  • PMID: 20852002
    Zhou SY, Shu C, Korth-Bradley J, Raible D, Palmisano M, Wadjula J, Fatenejad S, Bjornsson T: Integrated population pharmacokinetics of etanercept in healthy subjects and in patients with rheumatoid arthritis and ankylosing spondylitis. J Clin Pharmacol. 2011 Jun;51(6):864-75. doi: 10.1177/0091270010375961. Epub 2010 Sep 17.
  • PMID: 15703360
    Yim DS, Zhou H, Buckwalter M, Nestorov I, Peck CC, Lee H: Population pharmacokinetic analysis and simulation of the time-concentration profile of etanercept in pediatric patients with juvenile rheumatoid arthritis. J Clin Pharmacol. 2005 Mar;45(3):246-56. doi: 10.1177/0091270004271945.
  • PMID: 10676822
    Korth-Bradley JM, Rubin AS, Hanna RK, Simcoe DK, Lebsack ME: The pharmacokinetics of etanercept in healthy volunteers. Ann Pharmacother. 2000 Feb;34(2):161-4. doi: 10.1345/aph.19126.
  • PMID: 17916444
    Wong M, Ziring D, Korin Y, Desai S, Kim S, Lin J, Gjertson D, Braun J, Reed E, Singh RR: TNFalpha blockade in human diseases: mechanisms and future directions. Clin Immunol. 2008 Feb;126(2):121-36. doi: 10.1016/j.clim.2007.08.013. Epub 2007 Oct 3.
  • PMID: 8387891
    Banner DW, D'Arcy A, Janes W, Gentz R, Schoenfeld HJ, Broger C, Loetscher H, Lesslauer W: Crystal structure of the soluble human 55 kd TNF receptor-human TNF beta complex: implications for TNF receptor activation. Cell. 1993 May 7;73(3):431-45.

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