9alpha-Fluoromedroxyprogesterone acetate (FMPA) is a synthetic analog of
medroxyprogesterone acetate (MPA). FMPA exhibited more potent anti-
tumor and anti-angiogenic activities in some assay systems than the parent agent, MPA. Exudative
age-related macular degeneration (AMD) is characterized by
choroidal neovascularization (CNV).
Anecortave acetate, an angiostatic
steroid, is clinically efficacious in patients with exudative AMD.
Betamethasone is an anti-angiogenic
steroid. Therefore, we examined the effects of FMPA,
anecortave acetate and
betamethasone on
laser-induced CNV in rats.
Anecortave acetate and
betamethasone were included as positive controls. Crypton
laser was applied to the fundus in Brown Norway rats.
Laser photocoagulations were performed in each eye between the major retinal vessels of the superior retina. Subconjunctival injection of FMPA,
anecortave acetate or
betamethasone was performed once just after the
photocoagulation (on day 0). The incidence of CNV formation was evaluated by
fluorescein angiography (FAG) on day 14. On the next day, examination of the
retinal function was performed by electro retinogram (ERG). Subconjunctival injection of FMPA at doses of 300, 1000 and 3000 microg/eye dose-dependently inhibited the incidence of CNV formation. Significant differences were observed at doses of 1000 and 3000 microg/eye of FMPA as compared with the control group.
Anecortave acetate and
betamethasone significantly inhibited the incidence of CNV formation. FMPA at the doses used in this study did not affect the
retinal function in rats, as determined by ERG. FMPA appeared to be effective in a rat model of CNV, so it was demonstrated that FMPA might be useful in the treatment of AMD.