LB-100 PP2A Inhibitor Formulation with Glutamate for Storage Stability

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Solution Overview

Problem

Current PP2A inhibitors have not been explored in human clinical trials, and there is a need for stable pharmaceutical compositions suitable for clinical use.

Innovation Solution

A pharmaceutical composition comprising a protein phosphatase 2A inhibitor, specifically LB-100, combined with monosodium glutamate, which is stable under long-term storage conditions and suitable for clinical use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If PP2A inhibitors are formulated for long-term storage, then stability is improved, but suitability for clinical use may be compromised without proper formulation

Engineering Contradiction:
ImprovestabilityVSAvoidsuitability for clinical use
Core Design Contradiction:
Stability of the object's compositionVSReliability

Solution Approach 1:

Monosodium glutamate serves as a formulation intermediary that mediates between the PP2A inhibitor and the storage environment, enabling long-term stability while maintaining clinical suitability. The glutamate buffer system acts as a protective intermediary that prevents degradation without interfering with the drug's therapeutic action.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation utilizes specific parameter changes including pH adjustment to alkaline conditions (using monosodium glutamate buffer) and concentration optimization to achieve a stable state that maintains both long-term storage stability and clinical applicability. The pH parameter is critically adjusted to prevent degradation while ensuring safety for human administration.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If LB-100 is used as a single agent or in combination, then antiproliferative activity is improved, but formulation stability for clinical trials is compromised

Engineering Contradiction:
Improveantiproliferative activityVSAvoidformulation stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention creates a composite pharmaceutical formulation by combining LB-100 (the active PP2A inhibitor) with monosodium glutamate (the stabilizing buffer). This composite material integrates the therapeutic properties of LB-100 with the stabilizing properties of glutamate, achieving both antiproliferative activity and formulation stability simultaneously.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS12343342B2Methods for treating soft tissue sarcoma
Publication Date: 2025.07.01 LIXTE BIOTECHNOLOGY INC
  • US12343342B2 patent drawing
  • US12343342B2 patent drawing
  • US12343342B2 patent drawing

AI summary

The invention relates to a pharmaceutical composition comprising a protein phosphatase 2A (PP2A) inhibitor and monosodium glutamate.