Therapeutic Compound Inhibiting MPC and MCT1 for Metabolic Disease Treatment
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Solution Overview
Problem
Current treatments lack effective agents that can directly or indirectly inhibit mitochondrial pyruvate carrier (MPC) and monocarboxylate transporter (MCT) to target metabolic pathways in cancer cells, as well as other conditions like non-alcoholic steatohepatitis, diabetes, obesity, and chronic graft versus host disease.
Innovation Solution
A compound is identified that potently inhibits MPC and MCT1, offering potential therapeutic benefits through pharmaceutical compositions and methods for treating related diseases and conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used, then existing therapeutic options are available, but effective inhibition of MPC and MCT to target metabolic pathways in cancer cells and related conditions is not achieved
Solution Approach 1:
The compound of formula (I) is designed to inhibit multiple transporters (MPC and MCT1) that are involved in pyruvate metabolism across different disease contexts. This multi-target inhibition mechanism allows a single agent to address cancer, non-alcoholic steatohepatitis, diabetes, obesity, and chronic graft versus host disease, achieving broad therapeutic versatility while maintaining reliable efficacy in each indication
2Reliability
If direct inhibition of MPC is implemented, then pyruvate uptake into mitochondria is blocked, but feedback inhibition of MCTs requires additional therapeutic mechanisms
Solution Approach 1:
The compound of formula (I) merges dual inhibitory capabilities into a single molecular entity: it directly inhibits MPC to block pyruvate uptake into mitochondria, and simultaneously inhibits MCT1 to prevent lactate-pyruvate exchange. This combined action on multiple transporters simplifies the therapeutic mechanism while enhancing reliability through complementary inhibition pathways
Data Source
AI summary
The invention provides a compound of formula (I) or a salt thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof and methods of inhibiting an MPC and treating an MPC related disease or condition.