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