LSD1 Inhibitor Formulation Stability via Organic Acid Mediation
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Solution Overview
Problem
Current LSD1 inhibitors face challenges in stability and efficacy, particularly in maintaining their potency over time due to degradation issues, which affects their effectiveness in treating LSD1-mediated cancers.
Innovation Solution
The development of a pharmaceutical formulation comprising Compound 1 di-tosylate salt, an organic acid like fumaric acid, and a diluent such as lactose, which enhances stability and reduces degradation, forming a solid oral dosage form that inhibits LSD1 activity effectively.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If LSD1 inhibitors are formulated without organic acid and diluent, then the formulation is simple, but the stability and bioavailability of the compound deteriorates
Solution Approach 1:
The patent introduces organic acid (such as fumaric acid) and diluent (such as lactose) as intermediary substances that mediate between the active ingredient and the environment. These intermediaries protect the compound from degradation while maintaining formulation simplicity through well-established pharmaceutical excipients.
Solution Approach 2:
The formulation combines multiple materials (Compound 1 di-tosylate salt, organic acid, and diluent) into a composite pharmaceutical composition. This composite structure enhances the stability and bioavailability of the active ingredient while managing its degradation issues through synergistic interactions between components.
2Duration of action of stationary object
If LSD1 inhibitors are stored without protective formulation, then storage is simple, but degradation increases over time
Solution Approach 1:
The patent applies preliminary protective action by incorporating organic acid and diluent into the formulation before storage. This pre-protection prevents degradation during storage, extending the duration of efficacy without requiring complex manufacturing processes, as these are standard pharmaceutical excipients.
3Reliability
If the compound is administered without formulation optimization, then administration is simple, but bioavailability and therapeutic efficacy are reduced
Solution Approach 1:
The patent changes the physical and chemical parameters of the compound by forming it into a formulated composition with organic acid and diluent. This parameter change improves bioavailability and therapeutic efficacy by protecting the compound from degradation and enhancing its delivery, while the formulation structure remains relatively simple using standard excipients.
Data Source
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AI summary
The present application relates to pharmaceutical formulations and dosage forms of a lysine specific demethylase-1 (LSD1) inhibitor, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, including methods of preparation thereof, which are useful in the treatment of LSD1 mediated diseases such as cancer.