Periodic Dosing Regimen for Antineoplastic Efficacy and Toxicity Management

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Solution Overview

Problem

Current cancer treatments using Compound A often involve frequent doses at lower concentrations or larger doses at intermittent periods, leading to suboptimal efficacy and increased toxicity, necessitating a more effective and safer administration protocol.

Innovation Solution

Administering Compound A in specific dose ranges (400-3000 mg/day) for defined periods (up to 7 days) followed by rest periods within a 28-day treatment cycle, optimizing the dosing schedule to maximize antineoplastic effects while minimizing toxicity, such as the 5+/23− schedule where Compound A is given daily for 5 days followed by 23 days of rest.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If frequent doses at lower concentrations are administered, then continuous antineoplastic effect is maintained, but toxicity increases and efficacy becomes suboptimal

Engineering Contradiction:
Improveantineoplastic efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent implements periodic dosing schedules where Compound A is administered for a defined period (e.g., 5 days) followed by a rest period (e.g., 23 days) within a 28-day cycle. This periodic action allows the drug to exert its antineoplastic effect during the treatment phase while providing recovery time during the rest phase, thereby reducing cumulative toxicity while maintaining therapeutic efficacy.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The patent optimizes dosing parameters by administering specific dose ranges (e.g., 800-3000 mg/day) for defined periods rather than continuous low-dose administration. This parameter change in dosing intensity and duration achieves superior antitumor activity while managing toxicity through the structured treatment-rest cycle.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If larger doses at intermittent periods are administered, then antineoplastic efficacy is enhanced, but toxicity increases

Engineering Contradiction:
Improveantineoplastic efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs periodic action by administering larger doses (800-3000 mg/day) during specific treatment windows (e.g., 5 days) followed by rest periods (e.g., 23 days). This approach concentrates the antineoplastic effect during treatment phases while allowing physiological recovery during rest phases, thereby achieving enhanced efficacy with controlled toxicity.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The patent segments the dosing regimen into distinct treatment phases and rest phases within a 28-day cycle. This segmentation allows high-dose administration to be divided into manageable intervals, maximizing therapeutic benefit while distributing toxic effects across time to allow recovery.

Inventive Principle:
Principle #1Segmentation

3Reliability

If more frequent dosing is administered, then antineoplastic coverage is improved, but patient tolerability decreases

Engineering Contradiction:
Improveantineoplastic coverageVSAvoidpatient tolerability
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent implements periodic dosing schedules (e.g., 5 days on, 23 days off) that provide continuous antineoplastic coverage during treatment phases while ensuring patient tolerability through extended rest phases. This rhythm allows patients to recover from side effects while maintaining therapeutic pressure on tumors.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The patent optimizes dosing parameters including dose amount (800-3000 mg/day), treatment duration (up to 7 days preferably 5 days), and rest period length (21-23 days) to achieve the optimal balance between antineoplastic coverage and patient tolerability.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS11382892B2Method for administration
Publication Date: 2022.07.12 F HOFFMANN LA ROCHE INC
  • US11382892B2 patent drawing
  • US11382892B2 patent drawing
  • US11382892B2 patent drawing

AI summary

There is provided a new dosage regimen for Compound A which maximizes anti-tumor activity while maintaining acceptable toxicity levels.