Anti-angiogenic Compounds for Ocular Delivery
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Solution Overview
Problem
Current treatments for diseases characterized by inappropriate growth of new blood vessels, such as diabetic retinopathy, age-related macular degeneration, and cancer, are limited by the need for frequent injections, high costs, and the development of resistance to anti-angiogenic therapies, necessitating the development of more effective and safer anti-angiogenic compounds.
Innovation Solution
Development of specific anti-angiogenic compounds, including those from the 11B and 11F series, which are administered topically or systemically, inhibiting angiogenesis by targeting key pathways involved in blood vessel formation and tumor growth, offering a potential alternative to costly antibodies and invasive injections.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If monoclonal antibodies targeted to VEGF are used for anti-angiogenic therapy, then new leaky blood vessels stop developing, but treatment cost increases and requires frequent intravitreal injections
Solution Approach 1:
The patent replaces the mechanical injection system (intravitreal injections by retinal specialists) with a topical administration system (eye drops). The anti-angiogenic compound is delivered through the tear film, eliminating the need for invasive injections and specialized medical procedures while maintaining therapeutic effectiveness.
Solution Approach 2:
The patent uses a small molecule compound that can be administered via inexpensive eye drops, replacing expensive monoclonal antibodies. The compound provides sustained anti-angiogenic activity through repeated topical applications, reducing the need for costly intravitreal injections every six weeks.
2Reliability
If laser ablation is performed to treat diabetic retinopathy, then new vessels are destroyed, but healthy retinal tissue is also damaged
Solution Approach 1:
The patent applies anti-angiogenic compound specifically to the ocular surface through eye drops, creating a localized therapeutic effect. The compound concentrates on the corneal and conjunctival surfaces where it inhibits VEGF-mediated angiogenesis without penetrating deep into the retina, thus protecting healthy retinal tissue while targeting abnormal vascular growth.
Solution Approach 2:
The patent converts the natural protective barrier of the eye (tear film and corneal epithelium) from a limitation into a delivery advantage. By utilizing the ocular surface as the route of administration, the compound achieves high local concentration at the site of action without requiring invasive procedures, thereby avoiding tissue damage while maintaining therapeutic efficacy.
3Reliability
If anti-angiogenic therapy is used for cancer treatment, then tumour growth is inhibited, but resistance develops over time
Solution Approach 1:
The patent modifies the pharmacological parameters of anti-angiogenic therapy by using a small molecule compound with different mechanism and pharmacokinetic properties compared to monoclonal antibodies. The compound exhibits sustained inhibition of VEGF signaling through repeated topical applications, potentially delaying or preventing resistance development through continuous suppression of angiogenic pathways.
Data Source
AI summary
(E)-2-(2-Quinolin-2-yl-propenyl)-phenol, 2-Quinolin-2-yl-ylethynyl-phenol and salts thereof are useful as medicaments, especially for treatment of an angiogenesis-related disease or disorder.