Fusion Proteins

• Abat­cept
• Afliber­cept
• Etan­er­cept

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