Limus Compounds Inhibit Choroidal Neovascularization
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Solution Overview
Problem
Current treatments for choroidal neovascularization (CNV) associated with ocular diseases like age-related macular degeneration (AMD) are inadequate, as they often result in significant visual loss and recurrence of neovascularization, with limited effectiveness and adverse effects from laser photocoagulation.
Innovation Solution
The use of 'limus' compounds, such as sirolimus and tacrolimus, which bind to immunophilin proteins to inhibit angiogenesis in choroidal membranes, offering a therapeutic approach to prevent or significantly inhibit CNV by administering these compounds via various routes to treat ocular neovascular diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If laser photocoagulation is used to treat choroidal neovascularization, then neovascular lesions can be ablated and vision preserved in selected cases, but neovascularization recurs in about 50-70% of eyes and treatment is limited to only about 10% of cases
Solution Approach 1:
The invention changes the therapeutic approach from physical ablation (laser) to pharmacological inhibition (limus compounds). By administering limus compounds systemically or locally, the treatment mechanism shifts from destroying existing vessels to inhibiting new vessel formation, thereby expanding applicability to all CNV cases regardless of location or size while maintaining treatment effectiveness through targeted anti-angiogenic action
2Reliability
If laser photocoagulation is used to treat CNV, then vision can be preserved in selected cases, but visual acuity immediately worsens after surgery and only marginally better outcomes are achieved at two years
Solution Approach 1:
The limus compound treatment can be administered before CNV fully develops or progresses, preventing neovascularization before it occurs. By inhibiting angiogenesis proactively through mTOR pathway blockade, the treatment avoids the need for corrective procedures that cause temporary vision loss, thereby preserving vision without the delayed recovery period associated with laser surgery
3Reliability
If limus compounds are administered to inhibit angiogenesis, then unwanted neovascularization is inhibited and vision preserved, but long-term safety and optimal dosing requirements need to be determined
Solution Approach 1:
The limus compounds target the mTOR pathway, which is a central regulatory node in cell growth and angiogenesis. By inhibiting this master regulator, the treatment achieves broad anti-angiogenic effects through a single molecular target, simplifying the treatment protocol compared to multi-target approaches while maintaining effectiveness against various angiogenic stimuli
Data Source
AI summary
The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents.