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A. Shafiee, K. W. Ward; Efficacy of a Selective Glucocorticoid Receptor Agonist (SEGRA; BOL-303242-X) in a Rodent Model of Laser-Induced Choroidal Neovascularization. Invest. Ophthalmol. Vis. Sci. 2009;50(13):60.
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© ARVO (1962-2015); The Authors (2016-present)
BOL-303242-X is a Selective Glucocorticoid Receptor Agonist (SEGRA) currently of interest for the treatment of a variety of ocular diseases. SEGRAs may offer an improved clinical safety profile compared to corticosteroids. In this study we evaluated the prophylactic effect of posterior sub-tenon injection of the SEGRA BOL-303242-X compared to the steroid triamcinolone acetonide (TA) on laser-induced choroidal neovascularization (CNV) in rats.
Male Long-Evans rats were divided into 4 groups (n=12/group): vehicle, 2 mg TA, and 0.5 and 2 mg BOL-303242-X. 8 laser lesions were placed in the retina between the major retinal vessels in a circular pattern around the optic disc of both eyes. An 810-nm diode laser was utilized with the following settings: 80 µm spot size, 300 mW power, and 0.05 sec duration. Immediately post-laser treatment, 50 µl of the test article were administered bilaterally to the posterior sub-tenon space. The intensity of fluorescein leakage in late-phase fluorescein angiography (FA) was evaluated at 14 and 21 days post-laser by ranking the animals according to their retinal leakage. On days 14 (n=4) and 21 (n=8) rats were sacrificed and eyes were used for histopathological examination.
BOL-303242-X at the lowest dose of 0.5 mg significantly inhibited CNV (fluorescein intensity) when compared to the vehicle control by day 14. A higher dose of 2 mg TA was also effective in reducing fluorescein leakage at the same time point. In contrast to the 14-day data, neither TA nor BOL-303242-X significantly changed CNV on day 21.
These data suggest that the SEGRA BOL-303242-X may have anti-angiogenic activity in the rat CNV model similar to that of the conventional steroid TA. Therefore BOL-303242-X has the potential to be used for the treatment of age-related macular degeneration as a stand-alone therapy or co-administered with other anti-angiogenic agents lacking anti-inflammatory properties to improve patient outcomes.
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