APLNR and VEGF Antagonist Combination Therapy for Eye Disorders
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Solution Overview
Problem
Current treatments for vascular eye diseases, such as diabetic retinopathy and age-related macular degeneration, have limitations in effectively inhibiting abnormal neovascularization and vascular permeability, with anti-VEGF therapies showing partial efficacy and potential side effects like proliferative retinopathy.
Innovation Solution
Administering a combination of an apelin receptor antagonist and a vascular endothelial growth factor (VEGF) antagonist to inhibit pathological angiogenesis and promote revascularization, using pharmaceutical compositions that include antibodies or small molecule inhibitors targeting the apelin/APLNR pathway in conjunction with VEGF inhibitors.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If anti-VEGF therapy is administered alone, then vascular permeability is reduced, but abnormal neovascularization is not effectively inhibited and proliferative retinopathy may occur
Solution Approach 1:
The patent combines apelin receptor antagonist and VEGF antagonist into a dual-target therapy regimen. The apelin antagonist (e.g., A182454 or A182455) inhibits pathological angiogenesis through the apelin/APLNR pathway, while the VEGF antagonist (e.g., aflibercept, ranibizumab, or bevacizumab) blocks VEGF-mediated vascular permeability and neovascularization. This merged approach addresses both mechanisms simultaneously, improving treatment reliability while reducing side effects through complementary action.
2Object-generated harmful factors
If apelin receptor antagonist is used alone, then pathological angiogenesis is inhibited, but vascular permeability control is insufficient
Solution Approach 1:
The patent merges apelin receptor antagonist therapy with VEGF antagonist therapy to achieve comprehensive control. The apelin antagonist targets angiogenesis pathways, while the VEGF antagonist specifically controls vascular permeability. Together, they provide both anti-angiogenic and anti-permeability effects, resolving the insufficiency of single-target therapy.
3Reliability
If combination therapy with apelin receptor antagonist and VEGF antagonist is administered, then treatment efficacy is improved, but device complexity increases
Solution Approach 1:
The patent combines two biologic agents into a unified therapy regimen that targets complementary pathways. While the regimen involves two medications, they address distinct mechanisms (apelin-mediated angiogenesis and VEGF-mediated permeability) that work synergistically, improving overall efficacy without requiring complex delivery systems or procedures.
Data Source
AI summary
The present disclosure provides methods for treating, preventing or reducing the severity of an eye disease. The methods of the present disclosure comprise administering to a subject in need thereof a therapeutic composition comprising an APLNR antagonist such as an anti-APLNR antibody in combination with a vascular endothelial growth factor (VEGF) antagonist (for example, aflibercept).