pegpleranib   Click here for help

GtoPdb Ligand ID: 13532

Synonyms: E-01AJ | E-10030 | E01AJ | E10030 | Fovista® | X-01E | X01E
Compound class: Nucleic acid
Comment: Pegpleranib (E10030) is a 32-mer pegylated DNA aptamer that selectively binds to PDGF-BB and PDGF-AB homo- and hetero-dimers. It prevents PDGF binding to its cognate PDGF receptors. Blocking receptor activation leads to the death of capillary pericytes. This mechanism was investigated as a disruptor of vessel formation in neovascular age related macular degeneration. Pegpleranib is formulated as a sodium adduct for therapeutic administration (see DBSALT002614).
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Summary of Clinical Use Click here for help
Phase 3 studies of E10030 were terminated when analyses showed that the combination of E10030 and ranibizumab (an anti-VEGFA mAb) failed to demonstrate enhanced efficacy (superiority) compared to ranibizumab alone.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01940900 A Phase 3 Safety and Efficacy Study of Fovista® (E10030) Intravitreous Administration in Combination With Lucentis® Compared to Lucentis® Monotherapy Phase 3 Interventional Astellas Pharma Inc The OPH1003 study
NCT01940887 A Phase 3 Safety and Efficacy Study of Fovista® (E10030) Intravitreous Administration in Combination With Either Avastin® or Eylea® Compared to Avastin® or Eylea® Monotherapy Phase 3 Interventional Astellas Pharma Inc The OPH1002 study