CDK4/6-Endocrine Combination Therapy for Breast Cancer Recurrence

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Solution Overview

Problem

Current adjuvant endocrine therapy regimens for HR+/HER2- early-stage breast cancer patients are not optimized to sufficiently reduce recurrence risk, necessitating more precise treatment strategies.

Innovation Solution

A combined pharmaceutical composition comprising a substituted 2-hydro-pyrazole derivative (compound of formula (I)) and an endocrine therapeutic agent, such as aromatase inhibitors, estrogen receptor antagonists, or pituitary gonadotropin-releasing hormone analogues, is used to treat or prevent breast cancer post-surgery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If standard adjuvant endocrine therapy regimens are used for HR+/HER2- early-stage breast cancer patients, then drug accessibility and clinical efficacy benefit are maintained, but recurrence risk reduction is insufficient for high-risk patients

Engineering Contradiction:

Improverecurrence risk reductionVSAvoidtreatment regimen precision

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the therapeutic parameter by combining CDK4/6 inhibition with endocrine therapy, creating a new treatment paradigm that enhances the efficacy of standard endocrine therapy regimens for high-risk HR+/HER2- early-stage breast cancer patients

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite therapeutic approach by combining two different mechanism of action: CDK4/6 inhibition (compound of formula I) and endocrine therapy (aromatase inhibitors, estrogen receptor antagonists, or gonadotropin-releasing hormone analogues), achieving synergistic effect that improves recurrence risk reduction

Inventive Principle:

Principle #40Composite materials

2Reliability

If CDK4/6 inhibition is added to endocrine therapy, then recurrence risk is reduced, but treatment complexity increases

Engineering Contradiction:

Improverecurrence risk reductionVSAvoidtreatment regimen complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges two therapeutic approaches (CDK4/6 inhibition and endocrine therapy) into a single combined regimen, where the compound of formula I is administered together with aromatase inhibitors, estrogen receptor antagonists, or gonadotropin-releasing hormone analogues, achieving enhanced efficacy while managing complexity through integrated treatment planning

Inventive Principle:

Principle #5Merging (Combining)

Data Source

PatentEP4663633A1Combined pharmaceutical composition of substituted 2-hydrogen-pyrazole derivative and use thereof

Publication Date: 2025.12.17 CHIA TAI TIANQING PHARMA GRP CO LTD

AI summary

The present disclosure relates to a combined pharmaceutical composition of a substituted 2-hydrogen-pyrazole derivative and the use thereof, and specifically relates to a combined pharmaceutical composition of a compound of formula (I) and the use thereof in the treatment of breast cancer. According to the combined pharmaceutical composition of the present disclosure, the distant relapse-free survival can be remarkably prolonged.