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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. |
| No information available. |
Summary of Clinical Use  |
| Aflibercept is used in the treatment of macular edema following central retinal vein occlusion (CRVO), diabetic macular edema and neovascular age-related macular degeneration (AMD, wet macular degeneration). In 2015 the FDA expanded the approved use of aflibercept to include the treatment of diabetic retinopathy in patients with diabetic macular edema. The Zaltrap® brand is used to treat metastatic colorectal cancer. |
| Mechanism Of Action and Pharmacodynamic Effects |
| Alfibercept binds with high affinity to vascular endothelial growth factor (VEGF-A and -B) and placenta growth factor (PIGF-1 and -2), thereby inhibiting the neovascularization and vascular permeability actions of these peptides. This results in antitumour effects. |
| External links |
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For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |
