Sustained-Release Befiradol Dosing to Limit Peak Side Effects

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Solution Overview

Problem

Befiradol, a selective serotonin 5-HT1A receptor agonist, is effective for treating movement disorders but its use is limited by significant side effects such as dizziness and nausea, which are particularly problematic for patients already experiencing balance and nausea issues due to their condition or treatment.

Innovation Solution

Administering befiradol in a sustained release formulation that maintains an average patient's maximum plasma concentration below 15 ng/mL, occurring more than 4 hours post-administration, to minimize side effects like dizziness and nausea.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If befiradol is administered at effective doses to treat movement disorders, then therapeutic efficacy is improved, but side effects such as dizziness and nausea increase

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidside effects (dizziness and nausea)

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the pharmacokinetic parameters of befiradol through sustained release formulation. This changes the concentration-time profile by reducing peak plasma concentrations and extending the duration of action, thereby maintaining therapeutic efficacy while reducing side effects like dizziness and nausea that are concentration-dependent

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The sustained release formulation implements periodic action by providing controlled, extended-release dosing that maintains therapeutic levels over time. This periodic release pattern ensures continuous therapeutic effect while avoiding the sharp peaks that cause adverse effects

Inventive Principle:

Principle #19Periodic action

2Speed

If conventional immediate release formulation is used, then rapid onset of action is achieved, but peak plasma concentrations cause increased side effects

Engineering Contradiction:

Improveonset of actionVSAvoidside effects at peak concentration

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent applies dynamics by transitioning from static immediate release to dynamic controlled release. The sustained release formulation dynamically adjusts the release rate of befiradol over time, providing rapid initial onset followed by a gradual, controlled decline in plasma concentration, thereby avoiding harmful peak levels while maintaining therapeutic effect

Inventive Principle:

Principle #15Dynamics

Data Source

PatentUS12472169B2Method for treating movement disorders with befiradol

Publication Date: 2025.11.18 PIERRE FABRE MEDICAMENT SAS

AI summary

The present invention relates to a method of treatment of movement disorders, comprising administering to a patient in need thereof an effective amount of befiradol, wherein the administering step provides an average patient's maximum plasma concentration of befiradol below 15 ng/mL which occurs more than 4 hours post administration, said method minimizing side effects of dizziness and nausea. Sustained release pharmaceutical compositions that can be used according to this method are also described.