Heterobifunctional AR-BRD4 Compounds for Resistant Cancer Treatment
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current cancer treatments are not effective for all patients and often have substantial adverse side effects, necessitating new therapies that achieve an anti-cancer effect through a different mechanism.
Innovation Solution
Development of heterobifunctional compounds, represented by Formulas I and II, which can be administered to patients to treat cancer by causing death of cancer cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current cancer therapies (alkylation, topoisomerase inhibition, mitotic inhibition) are used, then cancer treatment is provided, but the therapies are not effective for all patients and have substantial adverse side effects
Solution Approach 1:
The patent changes the fundamental mechanism parameter of cancer therapy from conventional approaches (alkylation, topoisomerase inhibition, mitotic inhibition) to a novel mechanism involving heterobifunctional compounds that simultaneously bind to androgen receptor and BRD4, thereby achieving effective cancer treatment with reduced adverse side effects by altering the therapeutic mechanism rather than adjusting dosage or formulation of existing mechanisms
Solution Approach 2:
The patent employs heterobifunctional compounds that function as composite therapeutic agents, simultaneously engaging multiple targets (androgen receptor and BRD4) within a single molecular structure, enabling dual mechanism of action that improves treatment effectiveness while reducing the need for multiple separate therapies that would accumulate adverse effects
2Reliability
If conventional cancer therapies are used, then treatment is provided, but resistance develops in cancer cells
Solution Approach 1:
The heterobifunctional compounds are designed with universal binding capability to multiple cancer-related targets (androgen receptor and BRD4), allowing a single compound class to address diverse cancer types and mechanisms of resistance, thereby maintaining treatment effectiveness against cancer cells that have developed resistance to conventional single-mechanism therapies
Data Source
AI summary
The invention provides heterobifunctional compounds which may bind to both an androgen receptor and BRD4 (bromodomain-containing protein 4). Also provided are pharmaceutical compositions comprising the same and their use in treating disease, CN such as cancer.