Paclitaxel and Compound A Combination for Pancreatic Cancer

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Solution Overview

Problem

Current anti-tumor therapies using gemcitabine and paclitaxel or their combinations exhibit limited efficacy in treating pancreatic cancer, with response rates and survival periods being insufficient.

Innovation Solution

Combining paclitaxel or its nanoparticle form with 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine (Compound A) or its salt/prodrug, administered in various dosages and forms, to enhance anti-tumor effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If paclitaxel or gemcitabine is used alone or in combination for pancreatic cancer treatment, then anti-tumor therapy is provided, but the response rate is low (10-25%) and survival period is short (12-15 months)

Engineering Contradiction:
Improveanti-tumor effectVSAvoidresponse rate and survival period
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines paclitaxel (a taxane-based anti-tumor agent) with Compound A (1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine, a pyrimidine anti-tumor agent) to create a multidrug combination therapy. This merging of different drug classes with distinct mechanisms of action aims to achieve synergistic anti-tumor effects, overcoming the limitations of single-agent or conventional combination therapies in pancreatic cancer treatment

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent creates a composite therapeutic regimen by formulating paclitaxel and Compound A together in specific dosage ratios. This composite approach integrates two chemically and mechanistically distinct anti-tumor agents into a unified treatment protocol, leveraging their complementary anti-tumor properties to achieve superior clinical outcomes compared to individual agents

Inventive Principle:
Principle #40Composite materials

2Reliability

If multidrug combination therapy is carried out to compensate for differences in susceptibility and enhance drug efficacy, then drug efficacy is enhanced, but the therapeutic effect is still insufficient (response rate 23%, median survival 8.5 months with gemcitabine and nab-paclitaxel)

Engineering Contradiction:
Improvedrug efficacyVSAvoidtherapeutic effect
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent optimizes the dosage parameters of the combination therapy by specifying that Compound A is administered at 0.01 to 100-fold molar amount relative to paclitaxel. This parameter optimization ensures that each drug is administered at effective concentrations that maximize synergistic interaction while minimizing individual drug toxicities, thereby enhancing overall therapeutic effect

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs dynamic administration strategies where paclitaxel and Compound A can be administered simultaneously, sequentially, or at different intervals. This dynamic approach allows flexibility in timing and dosing schedules to optimize the therapeutic window and enhance anti-tumor efficacy while managing side effects, achieving superior outcomes compared to fixed combination protocols

Inventive Principle:
Principle #15Dynamics

Data Source

PatentUS11369625B2Anti-tumor agent, anti-tumor effect enhancer, and anti-tumor kit
Publication Date: 2022.06.28 FUJIFILM CORP
  • US11369625B2 patent drawing
  • US11369625B2 patent drawing

AI summary

An object of the present invention is to provide an anti-tumor agent and an anti-tumor kit which have superior anti-tumor effect as compared with a therapy with gemcitabine, paclitaxel or a combination thereof; as well as an anti-tumor effect enhancer. According to the present invention, provided is an anti-tumor agent including paclitaxel or a salt thereof and 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine or a salt or prodrug thereof.