A fluorescent fundus contrast agent that allows monitoring of hypoxic regions


  • Useful in determining the continued use of expensive VEGF inhibitors
  • Topical administration reduces the risk of side effects
  • Fixed-dose combination with VEGF inhibitors to differentiate it from biotech generics

Background & Technology

Ophthalmic anti-VEGF products inhibit VEGF-induced angiogenesis caused by hypoxia and are used to treat age-related macular degeneration with neovascularization and macular edema associated with retinal vein occlusion, among others. In particular, it is almost the only drug that has been shown to restore vision for age-related macular degeneration, creating a market of about $4 billion. As for VEGF antibody products, the development of bio-generics is in progress, and price competition is expected to intensify in the future.
The therapeutic efficacy of anti-VEGF products is thought to be judged by the resolution of hypoxia. However, existing methods of fundus examination (ICGA/FA) with fluorescein/indocyanine green or vascular and tissue monitoring with OCT do not measure the presence or absence of the causative hypoxia. This makes it difficult to determine when to end treatment, which may lead to unnecessary long-term administration and, conversely, to numerous cases of recurrence after completion.
The inventors have developed a probe (GPU-327) that emits near-infrared fluorescence when the patient becomes hypoxic, which can be measured by existing fundus cameras, and have successfully visualized the intraocular hypoxic region in mouse and rabbit pathological models. We are now planning to examine the joint development and the use of the monkey model.


A-H) Fluorescence probe detection of hypoxic regions produced by the retinal artery occlusion model.


University of Tsukuba, Associate Professor of Ophthalmology, Shin-ichi Fukuda


Article: Graefes Arch Clin Exp Ophthalmol (2016) 254:2373-2385
Patent: JPB6505408 (Granted)


Demonstrated detection of hypoxic regions using animal models. Fixed-dose combination studies with VEGF inhibitors and pre-clinical studies in monkeys are planned.
We are looking for companies to collaborate on joint grant applications and the pre-clinical trials.

Product No.WL-03724

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