Fusion Proteins
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Fusion Proteins
Abatacept
Abatacept (Orencia®) is a fusion protein composed of the Fc region of the immunoglobulin IgG1 linked to the extracellular domain of cytotoxic T-lymphocyte-associated protein 4 (CTLA-4). It is down-regulating the activation of T-cells by binding to the CD80 and CD86 ligand proteins. Orencia® is indicated for reducing symptoms in adult patients with moderately to severely active rheumatoid arthritis. It is also indicated for juvenile idiopathic arthritis and adult psoriatic arthritis. Patents on Orencia® expired in US in October 2019 and in Europe in December 2017. Learn more
Aflibercept
Aflibercept (Eylea®, Zaltrap®) is a recombinant fusion protein consisting of vascular endothelial growth factor (VEGF) – binding portion from the extracellular domains of human VEGF receptors 1 and 2 fused to the Fc portion of a human IgG1 immunoglobulin. Like ranibizumab, aflibercept is an inhibitor of VEGF. It binds to the receptor binding site of active forms of VEGF-A, including the biologically active, cleaved form of this molecule, VEGF-110. Eylea® (aflibercept) is indicated for the treatment of neovascular (wet) age-related macular degeneration, macular edema following retinal vein occlusion, diabetic macular edema, and diabetic retinopathy. Zaltrap® (ziv-aflibercept) is indicated in combination with 5-fluorouracil, leucovorin, irinotecan (cytostatic medication) for metastatic colorectal cancer that is resistant to or has progressed after an oxaliplatin-containing therapy. The basic US patent for aflibercept will expire in 2020, European patents will expire in 2021. Learn more
Etanercept
Etanercept (Enbrel®) is a dimeric human receptor fusion protein consisting of the extracellular ligand-binding domain of human 75 kDa (p75) tumor necrosis factor receptor (TNFR) linked to the Fc-part of human IgG1. The Fc-part of etanercept contains CH2 domain, CH3 domain and the hinge region. Etanercept competitively inhibits binding of TNF-α to TNFRs, rendering TNF-α biologically inactive. Etanercept also modulates indirectly different biological functions such as expression of adhesion molecule E-selectin, production of interleukin-6 (IL-6) and matrix metalloproteinase 3 (MMP-3), as well as IL-1. Etanercept is indicated for the treatment of rheumatoid arthritis, polyarticular juvenile idiopathic arthritis, psoriatic arthritis, ankylosing spondylitis and plaque psoriasis. Enbrel® patents expired in 2012 in US and in 2015 in Europe. Learn more