Oral CD73 Inhibitor Formulations with Chelating Agents
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Solution Overview
Problem
Current CD73 inhibitors face challenges due to less than ideal metabolic stability and the lack of effective oral formulations, limiting their availability for medical practitioners in treating various disorders, including cancer and inflammatory conditions.
Innovation Solution
Development of oral formulations comprising a compound of Formula (I) in combination with a chelating agent, which enhances the bioavailability of CD73 inhibitors, allowing for the treatment and prevention of a range of diseases mediated by CD73, such as cancer, fibrosis, and immune-related disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If CD73 inhibitors are developed as small molecules, then oral administration is enabled, but metabolic stability is compromised
Solution Approach 1:
The patent introduces a chelating agent as an intermediary substance that forms a stable complex with the CD73 inhibitor small molecule. This complex acts as a protective carrier that shields the drug from metabolic degradation while maintaining oral bioavailability, thus resolving the contradiction between oral administration capability and metabolic stability.
Solution Approach 2:
The invention creates a composite formulation combining the small molecule CD73 inhibitor with a chelating agent. This composite structure leverages the oral bioavailability properties of small molecules while the chelating agent provides metabolic stability through chelation, achieving both goals simultaneously.
2Quantity of substance
If CD73 inhibitors are formulated for oral use, then bioavailability is improved, but formulation complexity increases
Solution Approach 1:
The chelating agent serves as a simple intermediary that enhances bioavailability through a straightforward chelation mechanism. Rather than creating a complex multi-component formulation, the patent uses a single chelating agent that binds to the drug molecule, simplifying the overall formulation while improving absorption and bioavailability.
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 oral formulations effectively inhibit CD73 activity, providing therapeutic benefits in treating diverse conditions by improving bioavailability and stability, thus offering a promising approach for managing diseases like cancer and inflammatory disorders.
Implementation Method 1
oral formulations comprising a compound of Formula (I) and a chelating agent
Data Source
AI summary
Oral formulations comprising a compound of Formula (I) and a chelating agent are provided, wherein compounds of Formula (I) have the structure:wherein, W, X, Y, Z, Ra, Rc, and each Rg are as defined herein. Also provided are methods of preparation, methods of use, and specific dosage forms.