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Synonyms: AVE0005 | Eylea® | VEGF Trap | Zaltrap® | ziv-aflibercept
aflibercept is an approved drug (FDA (2011), EMA (2012))
Compound class:
Peptide or derivative
Comment: Alfibercept is a fusion protein combining the Fc portion of human IgG with the ligand binding domains of the VEGRF1 and VEGRF2 receptors.
Biosimilars: Patent protection for originator alfibercept is expected to expire earliest in Japan and China (2022), then in US (2023, if Regeneron's extended patent claims are accepted) and the EU (2025), and biosimilar development is underway [3]. Examples include Momenta Pharmaceuticals/Mylan's M710, Alteogen's ALT-L9 (a heat stabilised formulation with a predicted longer shelf-life than Eylea; NCT04058535), and Formycon/Santo Holdings' FYB203. |
Peptide Sequence  |
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SDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDSRKGFIISNATYKEIGLLTCE ATVNGHLYKTNYLTHRQTNTIIDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSG SEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISR TPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKT ISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKS RWQQGNVFSCSVMHEALHNH YTQKSLSLSPG |
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| Post-translational Modification | |
| This is a recombinant fusion protein comprising vascular endothelial growth factor (VEGF) binding portions from the extracellular domains of human VEGF receptors 1 and 2 fused to the Fc portion of human IgG1. It exists as a dimer, covalently linked by disulphide bridges. | |
| Chemical Modification | |
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Covalent disulphide bonds form between amino acids as follows: Intra peptide disulphide bonds (30-79, 124-185, 246-306, 352-410) Inter peptide disulphide bonds (214-214, 211-211) |
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