PRMT5 Inhibitor Combinations for Targeted Cancer Treatment
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Solution Overview
Problem
Current treatments for cancer are inadequate in effectively targeting the overexpression of Protein Arginine N-Methyltransferase 5 (PRMT5), which is linked to various human malignancies, necessitating improved pharmaceutical compositions or methods to treat or prevent cancer.
Innovation Solution
A pharmaceutical combination comprising a PRMT5 inhibitor of Formula (I) and at least one targeted agent/cellular activity modulator, such as an EGFR inhibitor, a KRAS inhibitor, or a Bcl-2 inhibitor, to treat and/or prevent cancer.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current single-agent treatments are used for cancer, then the treatment approach is simple, but the effectiveness in targeting PRMT5 overexpression is inadequate
Solution Approach 1:
The patent combines a PRMT5 inhibitor with at least one other targeted agent or cellular activity modulator into a single pharmaceutical composition. This merging of multiple therapeutic agents addresses the inadequacy of single-agent treatments in effectively targeting PRMT5 overexpression, while maintaining a unified formulation that manages complexity.
Solution Approach 2:
The invention creates a composite pharmaceutical composition containing multiple active ingredients with different mechanisms of action. The PRMT5 inhibitor is combined with other targeted agents (such as EGFR inhibitors, KRAS inhibitors, Bcl-2 inhibitors, etc.) to form a multi-component therapeutic agent that enhances effectiveness against PRMT5-driven cancers through synergistic or additive effects.
2Reliability
If PRMT5 overexpression is targeted in cancer treatment, then cancer progression can be inhibited, but the current treatments fail to achieve effective targeting
Solution Approach 1:
The patent develops a universal pharmaceutical composition that can be applied across multiple cancer types by combining a PRMT5 inhibitor with various targeted agents. The composition is designed to address PRMT5 overexpression, which is linked to various human malignancies, while the selectable partner agents provide versatility for different cancer contexts and molecular profiles.
Solution Approach 2:
The invention allows for parameter changes in the pharmaceutical composition by selecting different partner agents (EGFR inhibitors, KRAS inhibitors, Bcl-2 inhibitors, PARP inhibitors, etc.) depending on the specific cancer type and molecular characteristics. This enables optimization of the treatment for different cancer contexts while maintaining the core PRMT5 inhibition mechanism.
Data Source
AI summary
This disclosure relates to pharmaceutical combinations for treating and/or preventing cancer and methods and uses thereof. More particularly, provided are pharmaceutical combination comprising a PRMT5 Inhibitor and a cellular activity modulator selected from an EGFR inhibitor, a KRAS inhibitor, a KRAS-G12C inhibitor, a MEK inhibitor, a Bcl-2 inhibitor, a SOS1 inhibitor, a PARP inhibitor, a RAF inhibitor, a ERK inhibitor, a CDK4/6 inhibitor, a MALT1 inhibitor, a BTK inhibitor, MAT2A inhibitor, a PI3K inhibitor, a AKT inhibitor, a FGFR inhibitor, a Type I PRMT inhibitor, a STING agonist, or an immune checkpoint inhibitor/modulator.