FTD-TPI and Platinum Complex Combination for Tumor Regression

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Solution Overview

Problem

Current cancer treatments using the FTD⋅TPI combination drug and anti-tumor platinum complexes often result in significant side effects, and there is a need for a regimen that enhances anti-tumor effects while minimizing these side effects.

Innovation Solution

Administering the FTD⋅TPI combination drug at a molar ratio of 1:0.5 in combination with anti-tumor platinum complexes like cisplatin, carboplatin, or oxaliplatin, within specific dose ranges (50-100% of recommended monotherapy doses) to achieve enhanced anti-tumor effects with reduced side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the FTD⋅TPI combination drug and anti-tumor platinum complex are used in combination, then anti-tumor effects are enhanced, but side effects increase

Engineering Contradiction:
Improveanti-tumor effectVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by optimizing the dose ranges of both FTD⋅TPI combination drug and anti-tumor platinum complex to specific percentages (50-100% of recommended monotherapy doses), thereby achieving enhanced anti-tumor effects while controlling side effects through precise dosage parameter adjustment

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials by combining FTD⋅TPI combination drug with anti-tumor platinum complexes (cisplatin, carboplatin, or oxaliplatin) to create a synergistic treatment regimen that produces superior anti-tumor effects compared to either agent alone, while managing toxicity through composite formulation

Inventive Principle:
Principle #40Composite materials

2Productivity

If the FTD⋅TPI combination drug is used at higher doses to enhance anti-tumor effect, then tumor regression improves, but side effects become more severe

Engineering Contradiction:
Improvetumor regressionVSAvoidside effects
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes dosage parameters by administering FTD⋅TPI combination drug at 50-100% of the recommended monotherapy dose and anti-tumor platinum complex at 50-100% of the recommended monotherapy dose, achieving effective tumor regression while avoiding excessive side effects through precise parameter control

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

This approach results in significant tumor regression and prolonged life span with minimal side effects, making it an effective cancer treatment method for digestive, lung, and breast cancers.

Implementation Method 1

Trifluridine (another name: α,α,α-trifluorothymidine; hereinafter also called 'FTD') interferes with DNA synthesis by inhibition of thymidylate synthesis and interferes with DNA function by incorporation into DNA

Methodology Applied
Scientific EffectThymidylate synthesis inhibition:

Implementation Method 2

Trifluridine (another name: α,α,α-trifluorothymidine; hereinafter also called 'FTD') interferes with DNA synthesis by inhibition of thymidylate synthesis and interferes with DNA function by incorporation into DNA

Methodology Applied
Scientific EffectDNA incorporation:

Implementation Method 3

tipiracil hydrochloride (chemical name: 5-chloro-6-[(2-iminopyrrolidin-1-yl) methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride; hereinafter also called 'TPI') has a thymidine phosphorylase inhibitory effect. It is known that TPI suppresses in vivo degradation of FTD by thymidine phosphorylase

Methodology Applied
Scientific EffectThymidine phosphorylase inhibition:

Implementation Method 4

Anti-tumor platinum complexes are metal complex compounds containing platinum as the central metal, and inhibit DNA replication by binding to DNA

Methodology Applied
Scientific EffectDNA binding:

Data Source

PatentUS10092589B2Anti-tumor agent containing anti-tumor platinum complex, and anti-tumor effect enhancer
Publication Date: 2018.10.09 TAIHO PHARMA CO LTD
  • US10092589B2 patent drawing
  • US10092589B2 patent drawing
  • US10092589B2 patent drawing

AI summary

In order to provide a novel cancer treatment method using a FTD⋅TPI combination drug that exhibits markedly excellent anti-tumor effects with fewer side effects, the present invention provides an anti-tumor agent characterized in that the FTD⋅TPI combination drug and an anti-tumor platinum complex are administered in combination.