An anti-proliferative and anti-angiogenic compound. IMS2186 is a novel synthetic compound developed as an anti-CNV drug. The proposed mechanism of action under investigation, is blocking the cell cycle at G2 and inhibiting the production of PGE2/TNF-α. The latter contributing to anti-angiogenic and antiinflammatory effects. IMS2186 inhibits cell growth in vitro in tumor cells, non-transformed fibroblasts, and retinal pigment epithelial cells. IMS2186 inhibits angiogenesis (IC50= 0.1 µM) and cell migration, which plays a role in many biological processes: inflammation, angiogenesis, and scar formation. The physicochemical structure of IMS2186 showed also that the free drug concentration in a physiological media (e.g., vitreous or saline) is 8-10 µM above the IC50 for all these activities (0.1-3.0 µM). Intraocular injection of IMS2186 could be a long-lasting effective treatment for CNV (choroidal neovascularization) in AMD (age-related macular degeneration) with a reduction in scarring and related visual loss.
Falkenstein, I.A., et al., Toxicity and intraocular properties of a novel long-acting anti-proliferative and anti-angiogenic compound IMS2186. Curr. Eye Res. 33, 599-609, (2008)
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