June 2017
Volume 58, Issue 8
Open Access
ARVO Annual Meeting Abstract  |   June 2017
Novel Glycosylated VEGF Decoy Receptor Fusion Protein, VEGF-Grab3 showed superior anti-angiogenic efficacy to Aflibercept (Eylea): a potential therapeutic agent for exudative Age-related macular degeneration (AMD)
Author Affiliations & Notes
  • Hye kyoung Hong
    Department of Ophthalmology,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Eun jin Lim
    Graduate School of Medical Science and Engineering,, Korea Advanced Institute of Science and Technology, Daejeon, Korea (the Republic of)
  • Na-Kyung Ryoo
    Department of Ophthalmology,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Sang Jun Park
    Department of Ophthalmology,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Young Mi Na
    Department of Ophthalmology,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Jae Yong Chung
    Department of Clinical Pharmacology and Therapeutics,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Ho Min Kim
    Graduate School of Medical Science and Engineering,, Korea Advanced Institute of Science and Technology, Daejeon, Korea (the Republic of)
  • Kyu Hyung Park
    Department of Ophthalmology,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Se Joon Woo
    Department of Ophthalmology,, Seoul National University College of Medicine, Seoul National University Bundang, Seongnam-si, Korea (the Republic of)
  • Footnotes
    Commercial Relationships   Hye kyoung Hong, None; Eun jin Lim, None; Na-Kyung Ryoo, None; Sang Jun Park, None; Young Mi Na, None; Jae Yong Chung, None; Ho Min Kim, None; Kyu Hyung Park, None; Se Joon Woo, None
  • Footnotes
    Support  None
Investigative Ophthalmology & Visual Science June 2017, Vol.58, 1951. doi:
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      Hye kyoung Hong, Eun jin Lim, Na-Kyung Ryoo, Sang Jun Park, Young Mi Na, Jae Yong Chung, Ho Min Kim, Kyu Hyung Park, Se Joon Woo; Novel Glycosylated VEGF Decoy Receptor Fusion Protein, VEGF-Grab3 showed superior anti-angiogenic efficacy to Aflibercept (Eylea): a potential therapeutic agent for exudative Age-related macular degeneration (AMD). Invest. Ophthalmol. Vis. Sci. 2017;58(8):1951.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

Purpose : To investigate the therapeutic potential for AMD, in vitro and in vivo efficacy, safety, and intraocular pharmacokinetics of a novel Glycosylated VEGF Decoy Receptor Fusion Protein, VEGF-Grab3 were compared with those of Aflibercept (Eylea, VEGF-Trap-Eye).

Methods : The binding affinity of drugs to VEGF and PlGF were assessed using a biacore assay. For the evaluation of in vivo anti-angiogenic efficacy, choroidal neovascularization (CNV) and oxygen induced retinopathy (OIR) mouse models were used. High dose (25µg/1µL) and low dose (2µg/1µL) of VEGF-Grab3 and Aflibercept were injected intravitreally in the right eyes. Ocular toxicity was evaluated up to 30 days and was compared between two drugs with histopathologic and electromicroscopic analysis of mouse eyeballs. Intraocular pharmacokinetics were also investigated using rabbit eyes.

Results : Affinity of VEGF-Grab3 to VEGF and PlGF was about 3-fold higher than Aflibercept. In vivo anti-angiogenic efficacy of VEGF-Grab3 was superior than Aflibercept for low dose administration while it was comparable for high dose administration. The mouse retina treated with the two drugs showed mildly increased müller cell activation and senescence of retinal pigment epithelial cells. However, no discernible ocular toxicity was observed. Intraocular pharmacokinetic profiles were similar between two drugs.

Conclusions : The new anti-VEGFR decoy protein, VEGF-Grab3 showed a superior therapeutic efficacy to Aflibercept with similar safety and pharmacokinetic profiles. Up to now, VEGF-grab3 is the most potent anti-VEGF agents that can be used for neovascular retinal diseases such as exudative AMD.

This is an abstract that was submitted for the 2017 ARVO Annual Meeting, held in Baltimore, MD, May 7-11, 2017.

 

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