CD73 Inhibitor Compounds Counteract Adenosine Immunosuppression
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current cancer treatments are inadequate in addressing the role of CD73 in tumor immune evasion, as CD73-generated adenosine suppresses adaptive anti-tumor immune responses, promoting tumor growth and metastasis.
Innovation Solution
Development of compounds that inhibit CD73 activity, including specific pharmaceutical compositions and methods for administering these compounds to effectively target and inhibit CD73 in subjects with cancer, thereby modulating adenosine metabolism and enhancing anti-tumor immunity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current cancer treatments are used, then tumor growth is addressed through conventional methods, but they fail to counteract the immunosuppressive effects of CD73-generated adenosine
Solution Approach 1:
The patent converts the harmful immunosuppressive effect of CD73-generated adenosine into a therapeutic opportunity by developing CD73 inhibitors that block adenosine production, thereby transforming the tumor's immune evasion mechanism into a target for immune activation and tumor suppression
Solution Approach 2:
The patent changes the biochemical parameter of adenosine metabolism by inhibiting CD73 enzyme activity, which alters the balance of extracellular nucleotides and reduces immunosuppressive adenosine accumulation, thereby enhancing anti-tumor immune responses
2Productivity
If CD73 activity is inhibited, then anti-tumor adaptive immunity is promoted and tumor growth is suppressed, but new therapeutic agents and compositions must be developed
Solution Approach 1:
The patent segments the therapeutic approach into distinct chemical compounds with specific structures (Formula I) that can be individually optimized for CD73 inhibition, allowing for systematic development of inhibitor variants with improved potency and selectivity
Solution Approach 2:
The patent creates composite pharmaceutical compositions that combine CD73 inhibitor compounds with other therapeutic agents, forming multi-component formulations that synergistically enhance anti-tumor immunity while managing the complexity through structured combination therapies
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The inhibition of CD73 activity leads to suppressed tumor growth and prolonged survival by promoting anti-tumor adaptive immunity, providing a therapeutic approach to counteract the immunosuppressive effects of CD73 in cancerous tissues.
Implementation Method 1
CD73 catalyzes the conversion of AMP to adenosine (Ado)
Data Source
AI summary
The present disclosure provides pyrimidine dione compounds of Formula Iand pharmaceutical compositions thereof, for treating cancer, including solid tumors either-used alone or in combination with other anti-cancer agents.