Mechanisms of Action
Sirolimus has been shown to possess multiple mechanisms of action, positioning the compound as a potentially highly-efficacious therapeutic for a wide range of ocular diseases and conditions.
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Sirolimus' Mechanism of Action |
Relevance to Ocular Disease |
Anti-angiogenesis |
Inhibits formation of new blood vessels linked to vision-impairing diseases such as AMD and diabetic retinopathy |
Anti-proliferation |
Prevents proliferation of key cells required for formation of new blood vessels in the angiogenic process that is implicated in a number of ocular diseases including wet AMD and diabetic retinopathy |
Anti-migration |
Inhibits migration of endothelial cells in response to cytokines. Cellular migration is a necessary step in the angiogenic process associated with such ocular diseases as wet AMD and proliferative diabetic retinopathy |
Anti-fibrosis |
Inhibits formation of scar tissue. Scarring results from the tissue disruption and damage associated with AMD and other ocular diseases |
Immunosuppression |
Inhibits T- and B-cell activity and down-regulates multiple pro-inflammatory factors tied to ocular diseases |
Anti-permeability |
Inhibits blood vessel leakage (permeability) associated with the angiogenic process in wet AMD, diabetic retinopathy and other diseases and conditions that affect central vision |
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In addition to inhibiting the synthesis and activity of numerous signaling factors (e.g., VEGF) involved in the above processes, sirolimus also inhibits the response of endothelial cells to these signaling factors.
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