MetAP2 Inhibitor Combinations for Breast Cancer With Lower Hyperglycemia

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Solution Overview

Problem

Current treatments for triple-negative breast cancer (TNBC) and breast cancer with PIK3CA gene mutations are ineffective and induce dangerous side-effects, necessitating improved compositions and methods for treatment.

Innovation Solution

Combining MetAP2 inhibitors with eribulin, fulvestrant, alpelisib, or other therapeutic agents to treat cancer and mitigate treatment-induced hyperglycemia.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If cytotoxic chemotherapy is used to treat TNBC, then cancer cells are killed, but patient survival is limited and side effects occur

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the therapeutic parameter from cytotoxic chemotherapy to MetAP2 inhibition, targeting a different molecular pathway (methionine metabolism) to achieve cancer cell death while avoiding the side effects associated with traditional chemotherapy agents

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces MetAP2 inhibitors as an intermediary mechanism that blocks methionine metabolism in cancer cells, providing a novel pathway for treatment that does not rely on direct cytotoxic damage to cellular structures

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If PI3Kα inhibitors are used to treat PIK3CA mutated breast cancer, then tumor growth is inhibited, but dangerous side effects such as hyperglycemia andhyperinsulinemia occur

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidhyperglycemia

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the therapeutic parameter from PI3Kα inhibition to MetAP2 inhibition, targeting methionine metabolism instead of the PI3K pathway, thereby achieving anti-tumor effects while avoiding metabolic side effects like hyperglycemia andhyperinsulinemia

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent exploits the high methionine dependency of PIK3CA-mutated cancer cells as a vulnerability, using MetAP2 inhibitors to block their methionine metabolism and achieve selective toxicity against tumor cells while sparing normal cells from metabolic disruption

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If hormonal therapy is used for ER-positive breast cancer, then tumor growth is controlled, but treatment resistance develops in certain subtypes

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidtreatment resistance

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the therapeutic parameter from hormonal pathway modulation to methionine metabolism inhibition, providing a mechanism that is effective across different breast cancer subtypes including those resistant to hormonal therapy

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent develops MetAP2 inhibitors with universal applicability across multiple breast cancer subtypes (TNBC, ER-positive, PIK3CA-mutated), overcoming the subtype-specific limitations of hormonal therapy and other targeted approaches

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS20260014194A1Combinations comprising metap2 inhibitors for the treatment of cancer

Publication Date: 2026.01.15 SYNDEVRX INC

AI summary

The present disclosure provides pharmaceutical combinations comprising MetAP2 inhibitors for the treatment of cancer.