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Topical nepafenac inhibits ocular neovascularization
Kyoichi Takahashi1, Yoshitsugu Saishin, Yumiko Saishin
1Departments of Ophthalmology and Neuroscience, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287-9277, USA.
Investigative Ophthalmology & Visual Science
|December 31, 2002
Summary
Topical nepafenac effectively reduces ocular neovascularization by inhibiting VEGF production. This non-steroidal anti-inflammatory drug shows promise as a new treatment for conditions like choroidal neovascularization and retinopathy.
Area of Science:
- Ophthalmology
- Pharmacology
- Molecular Biology
Background:
- Topical nepafenac is metabolized to amfenac, a potent cyclooxygenase (COX)-1 and COX-2 inhibitor.
- Ocular neovascularization (NV) is a significant cause of vision loss.
- Understanding the efficacy of topical anti-inflammatory agents in ocular NV is crucial.
Purpose of the Study:
- To evaluate the effect of topical nepafenac on three distinct murine models of ocular neovascularization.
- To investigate the mechanism of action, specifically the role of vascular endothelial growth factor (VEGF).
Main Methods:
- A masked trial comparing vehicle with varying concentrations of topical nepafenac, diclofenac, and ketorolac tromethamine.
- Murine models included oxygen-induced ischemic retinopathy, laser-induced choroidal neovascularization (CNV), and rho/VEGF transgenic mice.
- VEGF mRNA levels in the retina were assessed.
Main Results:
- Topical nepafenac (0.1% and 0.5%) significantly reduced CNV and ischemia-induced retinal NV.
- Nepafenac treatment blunted the ischemia-induced increase in retinal VEGF mRNA.
- No significant inhibition of neovascularization was observed in rho/VEGF transgenic mice.
Conclusions:
- Topical nepafenac effectively inhibits CNV and ischemia-induced retinal neovascularization, likely by decreasing VEGF production.
- The results suggest topical nepafenac as a potential new treatment for ocular neovascularization.
- The study highlights the potential of topical delivery for antiangiogenic agents, warranting further formulation research.