Abstract
Etanercept is a tumor necrosis factor-α (TNF-α) antagonist used in the treatment of adult and juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, and ankylosing spondylitis. It is a recombinant, fully human, soluble, dimeric fusion protein that consists of two copies of the extracellular ligand-binding domain of the human 75-kDa TNF-α receptor linked to the Fc portion of human immunoglobulin (Ig) G1 (European Medicines Agency 2005). It is produced by recombinant DNA technology in a Chinese hamster ovary mammalian cell expression system (European Medicines Agency 2005; Enbrel: US Full Prescribing Information 2006). A simplified structure of etanercept is provided in Fig. 4.1. The CH2 and CH3 domains and the hinge region of the Fc portion of IgG1 are included but not the CH1 domain. It consists of 934 amino acids (fully human amino acid sequences) with an apparent molecular weight of 150 kDa (European Medicines Agency 2005; Enbrel: US Full Prescribing Information 2006).
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Key References
Choy EH, Panayi GS (2001) Cytokine pathways and joint inflammation in rheumatoid arthritis. N Engl J Med 344:907–916
Goffe B, Cather JC (2003) Etanercept: An overview. J Am Acad Dermatol 49:S105–111
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Zhou H (2005) Clinical pharmacokinetics of etanercept: a fully humanized soluble recombinant tumor necrosis factor receptor fusion protein. J Clin Pharmacol 45:490–497
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Molta, C.T. (2007). Etanercept. In: Boehncke, WH., Radeke, H.H. (eds) Biologics in General Medicine. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-29018-6_4
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DOI: https://doi.org/10.1007/978-3-540-29018-6_4
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