Amiselimod Two-Phase Dosing for Ulcerative Colitis

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Solution Overview

Problem

There is an unmet need for safe and effective treatments for ulcerative colitis (UC) and other gastrointestinal tract disorders, as existing treatments often have limitations in efficacy and safety.

Innovation Solution

Administering amiselimod in a two-dose regimen where the first dose is larger than the second dose, with amiselimod being a selective S1P receptor modulator that reduces lymphocyte counts and inflammation in the gastrointestinal tract, thereby treating or ameliorating UC without inducing negative chronotropic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments are used for ulcerative colitis, then some therapeutic effect may be achieved, but safety and efficacy limitations occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidsafety limitations
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by implementing a two-phase dosing regimen where the dose amount varies over time. The loading phase uses higher doses (0.3-1.0 mg/day) to rapidly achieve therapeutic effect, then transitions to a maintenance phase with lower doses (0.1-0.3 mg/day) to sustain efficacy while minimizing side effects. This dynamic parameter adjustment resolves the contradiction between achieving reliable treatment efficacy and avoiding safety limitations.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If a single dose regimen is used, then treatment simplicity is maintained, but therapeutic steady-state concentration is not achieved

Engineering Contradiction:
Improvetherapeutic steady-state concentrationVSAvoiddosing regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the treatment into two distinct phases: a loading phase (first administration period) and a maintenance phase (second administration period). This segmentation allows the dosing regimen to achieve therapeutic steady-state concentration through the initial loading phase while simplifying long-term management through the reduced-dose maintenance phase. The segmentation resolves the contradiction by dividing the complex dosing requirement into manageable temporal stages.

Inventive Principle:
Principle #1Segmentation

3Reliability

If higher doses are administered continuously, then therapeutic effect is maximized, but negative chronotropic effects occur

Engineering Contradiction:
Improvetherapeutic effectVSAvoidnegative chronotropic effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent implements periodic action through its two-phase dosing structure. The loading phase provides periodic high-dose administrations to maximize therapeutic effect and rapidly reduce inflammation. The transition to the maintenance phase with lower periodic doses sustains therapeutic effect while reducing the frequency and intensity of negative chronotropic effects. This periodic variation in dosing resolves the contradiction between maximizing therapeutic effect and minimizing harmful cardiac side effects.

Inventive Principle:
Principle #19Periodic action

Data Source

PatentUS20240299318A1Amiselimod for preventing, treating or ameliorating ulcerative colitis
Publication Date: 2024.09.12 BAUSCH HEALTH IRELAND LTD
  • US20240299318A1 patent drawing
  • US20240299318A1 patent drawing
  • US20240299318A1 patent drawing

AI summary

Described herein are methods for treating, ameliorating, and/or preventing ulcerative colitis (UC) as well as other inflammatory gastrointestinal disorders using amiselimod. The method of treatment includes dosing amiselimod at a larger initial dose as compared to the eventual maintenance dose.