Macrocyclic Compound for Tumor Vascular Remodeling and CAF Control
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Solution Overview
Problem
Current anti-cancer agents do not effectively address tumor vascular remodeling and Cancer Associated Fibroblast (CAF) activity, which are crucial for improving the cancer microenvironment and reducing drug resistance and metastasis.
Innovation Solution
A macrocyclic compound with tumor vascular remodeling effects and anti-CAF activity, which can be administered alone or in combination with other therapies, targeting various types of cancer.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current anti-cancer agents are used, then tumor growth inhibition is achieved, but tumor vascular remodeling and CAF activity are not effectively addressed
Solution Approach 1:
The macrocyclic compound is designed to perform multiple functions simultaneously: it inhibits tumor growth, remodels tumor vasculature, and suppresses CAF activity. This multi-functional approach allows a single agent to address multiple critical factors in the tumor microenvironment that were previously targeted by separate therapies, thereby improving overall treatment effectiveness without requiring complex combination regimens.
2Productivity
If tumor vascular remodeling is achieved, then drug delivery to tumor is improved, but the complexity of the treatment mechanism increases
Solution Approach 1:
The macrocyclic compound enables the tumor vasculature to self remodel into a more functional state through its pharmacological action. The compound normalizes abnormal tumor vessels, improving blood flow and permeability, which enhances the spontaneous delivery of subsequent anti-cancer drugs without requiring external intervention or complex delivery systems. This self-service mechanism improves drug delivery efficiency while avoiding additional treatment complexity.
3Object-affected harmful factors
If CAF activity is inhibited, then tumor metastasis is reduced, but the specificity of targeting CAFs versus other stromal cells becomes challenging
Solution Approach 1:
The macrocyclic compound exhibits selective activity toward CAFs by interacting with specific molecular targets that are differentially expressed or activated in CAFs compared to other stromal cells. This local quality approach allows the compound to precisely inhibit CAF-mediated tumor metastasis while sparing other cell types in the tumor microenvironment, achieving high specificity through molecular recognition rather than broad non-specific effects.
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 compound enhances tumor treatment by improving the cancer microenvironment, reducing tumor aggressiveness, and increasing the effectiveness of other anti-cancer agents.
Implementation Method 1
Halichondrin B has demonstrated in vitro inhibition of tubulin polymerization, microtubule assembly
Implementation Method 2
The compound enhances tumor treatment by improving the cancer microenvironment, reducing tumor aggressiveness
Data Source
AI summary
The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, and medical uses thereof.