Bcl-2 and BTK Inhibitor Combination for Resistant Cancer

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Solution Overview

Problem

Current treatments for cancers, autoimmune diseases, and inflammatory diseases often face challenges due to drug resistance and the need for multi-targeted therapies to effectively manage these conditions, particularly in cases resistant to BTK inhibitors like ibrutinib.

Innovation Solution

A combination product comprising a Bcl-2 inhibitor or a Bcl-2/Bcl-xL dual inhibitor and a BTK inhibitor is developed, where the Bcl-2 inhibitors are specific compounds or their pharmaceutically acceptable salts, administered alone or in combination with BTK inhibitors such as ibrutinib, to treat refractory or resistant diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If single drug therapy is used, then treatment simplicity is maintained, but drug resistance develops and treatment effectiveness decreases

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidtherapy complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines Bcl-2 inhibitor and BTK inhibitor into a fixed-dose combination product, merging two separate therapeutic mechanisms into a single administered regimen. This resolves the contradiction by maintaining treatment simplicity (single pill administration) while improving reliability through synergistic anti-cancer effects that overcome drug resistance

Inventive Principle:

Principle #5Merging (Combining)

2Productivity

If high dose single drug is used, then immediate therapeutic effect is achieved, but side effects increase and drug resistance develops

Engineering Contradiction:

Improvetherapeutic effect efficiencyVSAvoidside effects

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the dosing parameters by administering two drugs at lower individual doses in combination, rather than high doses of a single drug. The fixed-dose combination allows each component to be given at optimized lower doses that achieve synergistic therapeutic effect while reducing individual drug toxicity and side effects

Inventive Principle:

Principle #35Parameter changes

3Reliability

If combination therapy is used, then drug resistance is overcome and treatment effectiveness improves, but treatment complexity increases

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidtreatment administration

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent merges Bcl-2 inhibitor and BTK inhibitor into a single fixed-dose combination tablet, allowing patients to receive complex combination therapy through a simple single-pill regimen. This resolves the contradiction by maintaining ease of operation (single administration) while improving reliability through multi-targeted anti-cancer mechanisms that overcome resistance

Inventive Principle:

Principle #5Merging (Combining)

4Duration of action of stationary object

If prolonged treatment is used, then sustained therapeutic effect is achieved, but cumulative toxicity increases

Engineering Contradiction:

Improvetreatment durationVSAvoidcumulative toxicity

Core Design Contradiction:

Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent changes the dosing parameters by using lower individual doses of each inhibitor in combination, which reduces cumulative toxicity while maintaining sustained therapeutic effect through the synergistic interaction between Bcl-2 and BTK inhibition pathways

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS11478470B2Combination product of Bcl-2 inhibitor or Bcl-2/Bcl-xL dual inhibitor and BTK inhibitor and use thereof in the prevention and/or treatment of diseases

Publication Date: 2022.10.25 ASCENTAGE PHARMA SUZHOU CO LTD

AI summary

Provided herein is a combination product comprising a Bcl-2 inhibitor (or a Bc1-2/Bc1-xl dual inhibitor) and a BTK inhibitor, the combination product providing a use in the prevention and/or treatment of a disease (e.g., cancer, autoimmune disease and inflammatory disease.).