Eyepoint, Inc. · NASDAQ:EYPT
Eyepoint — EyePoint Pharmaceuticals — Retina Society 2023
8 slides from Eyepoint's conference presentation, October 2023
Slide 1: Comparison of the Antiangiogenic Profile of Tyrosine Kinase Inhibitors Vorolanib, Axitinib, and Sunitinib
Comparison of the FINANCIAL DISCLOSURES Antiangiogenic Profile Consultant – Abbvie, Adverum, Apellis, Aviceda, Eyepoint, ilumen, Iveric Bio, Genentech, Neurotech, Novartis, Outlook Therapeutics, Pixium, Revana, Regenxbio, Regeneron, Rejuvitas, Roche, Voxel, of Tyrosine Kinase Zeiss Inhibitors Vorola
Slide 2: Current treatment targets for wAMD and the unmet need
Current treatment targets for wAMD and the unmet need - Several ligands, receptors, and pathways beyond VEGF ligands contribute to wAMD Receptor abbreviations: FGFR, fibroblast growth factor receptor; PDGFR, platelet-derived growth factor receptor; TIE2, tyrosine-protein kinase receptor TIE-2; VEGFR
Slide 3: Anti-VEGF therapy: Acute treatment for wAMD, a chronic disease
Anti-VEGF therapy: Acute treatment for wAMD, a chronic disease Anti-VEGFs and bispecific antibody Pan-VEGF receptor inhibitors • Quench VEGF, ANG2 or PLGF in a ligand “trap” • Block all VEGF receptors 1, 2, and 3, PDGFRβ and other receptors involved in wAMD • Time to elimination is rapid, requiring
Slide 4: Vorolanib and other TKIs inhibited angiogenesis more effectively in the CAM assay
In vivo, vorolanib and other TKIs inhibited angiogenesis more effectively in the gelatin sponge- choriallantoic membrane (CAM) assay than the anti-VEGF (bevacizumab) positive control - IC50 concentration is sufficient for VEGFR2 inhibition as demonstrated by 200x IC50 results Experimental design usi
Slide 5: All three tested TKIs have potent pan-VEGFR inhibition and only axitinib is a strong inhibitor of TIE2
All three tested TKIs have potent pan-VEGFR inhibition and only axitinib is a strong inhibitor of TIE2 Control Enlarged and labeled Receptors of interest for angiogenesis (dot size represents 100% inhibition) Antibody and Trap inhibitor (assuming 100% binding of ligand) TKIs (10µM) Aflibercept OPT-3
Slide 6: IC50 measurements confirm kinase screening results as all TKIs are strong pan-VEGFR inhibitors
IC50 measurements confirm kinase screening results as all 3 TKIs are strong pan-VEGFR inhibitors - The TKIs are similar, but also differ because only axitinib potently binds TIE2 receptor Compound IC50 Data for VEGFR1 Compound IC50 Data for VEGFR2 Compound IC50 Data for VEGFR3 120 120 120 VOROLANIB
Slide 7: Vorolanib does not bind melanin
Vorolanib does not bind melanin - Accumulation in a melanin-containing tissue by any drug would need to be studied to determine impact Only sunitinib was found by LC/MS analysis to bind melanin. Vorolanib Compound Kd Bmax Mean % bound (µM) (nmol/mg (across all melanin) concentrations) Vorolanib ND N
Slide 8: Vorolanib is a pan-VEGF receptor inhibitor that will effectively block all known pathways of pathological angiogenesis
Vorolanib is a pan-VEGF receptor inhibitor that will effectively block all known pathways of pathological angiogenesis while not impacting TIE2 function Vorolanib binding • All TKIs effectively inhibit several receptors involved in to VEGFR2 pathological angiogenesis • TKIs offer pan–VEGFR inhibitio