Niraparib Dosing for Primary and Metastatic Brain Cancer

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Solution Overview

Problem

There is a need for effective therapies to treat primary and metastatic brain cancer, which has a low 5-year survival rate and high mortality rates, with existing treatments being inadequate.

Innovation Solution

Administering an effective dose of niraparib or its pharmaceutically acceptable salt to treat primary or metastatic brain cancer, potentially combined with radiation therapy and maintenance treatment, to achieve sufficient tumor concentrations of niraparib beyond a 5-fold of its biochemical IC50 value.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments are used for brain cancer, then treatment is provided, but treatment efficacy is insufficient and survival rate remains low

Engineering Contradiction:
Improvetreatment efficacyVSAvoidsurvival rate
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent achieves effective brain cancer treatment by changing the concentration parameter of niraparib through multiple dosing regimens (e.g., 300 mg daily for 14 days followed by 200 mg daily for 14 days) to achieve tumor concentrations exceeding 5-fold of the biochemical IC50 value, thereby resolving the contradiction between treatment efficacy and survival rate improvement

Inventive Principle:
Principle #35Parameter changes

2Reliability

If niraparib is administered to achieve therapeutic concentrations, then treatment efficacy is enhanced, but treatment complexity increases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtreatment regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies preliminary action by administering niraparib in a specific dosing schedule (300 mg daily for 14 days followed by 200 mg daily for 14 days) before evaluating response, ensuring therapeutic concentrations are achieved and maintained. This predetermined regimen simplifies the overall treatment complexity while ensuring efficacy

Inventive Principle:
Principle #10Preliminary action

3Productivity

If combination therapy with radiation is used, then survival is extended, but treatment side effects increase

Engineering Contradiction:
Improvesurvival extensionVSAvoidtreatment side effects
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses niraparib as an intermediary agent that enhances the effectiveness of radiation therapy while potentially reducing the required radiation dose. By administering niraparib in a specific dosing regimen that achieves therapeutic concentrations, the treatment extends survival while the intermediary作用 helps mitigate the harmful effects of intensive combination therapy

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS20250352534A1Use of Niraparib for the Treatment of Brain Cancer
Publication Date: 2025.11.20 TESARO INC
  • US20250352534A1 patent drawing
  • US20250352534A1 patent drawing
  • US20250352534A1 patent drawing

AI summary

The present invention provides methods of administering niraparib for the treatment of primary and metastatic brain cancer.