S1PR Modulator Composition for Skeletal Muscle Atrophy Prevention
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Solution Overview
Problem
Current treatments for skeletal muscle degeneration, such as sarcopenia and atrophy, are inadequate, and there is a need for specific molecules that can effectively modulate sphingosine-1-phosphate receptors (S1PR) to prevent or treat these conditions.
Innovation Solution
A pharmaceutical composition comprising specific modulators of S1PR receptors, including CYM5520, EN300, CYM5478, VPC23019, TY52156, and siRNA targeting S1PR3, is developed to inhibit the expression of Atrogin-1/MAFbx and prevent muscle atrophy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Strength
If exercise and nutritional intake are increased to slow muscle loss, then muscle mass is partially maintained, but the results are not replicable and do not provide sufficient protection against severe atrophy
Solution Approach 1:
The patent changes the biological parameter by targeting specific S1PR receptors with selective modulators. Instead of relying on general nutritional support, the invention uses receptor-specific pharmacological agents (S1PR1 agonists, S1PR2 agonists, S1PR3 antagonists) to directly influence muscle atrophy pathways, achieving more reliable and reproducible protection against muscle loss.
2Object-affected harmful factors
If no specific drug treatment is used, then side effects are minimized, but muscle degeneration progresses without effective intervention
Solution Approach 1:
The patent applies local quality by targeting specific S1PR receptor subtypes with selective modulators. Different S1PR subtypes are activated or inhibited selectively based on their specific roles in muscle atrophy pathways, allowing precise control over muscle protection mechanisms while minimizing off-target effects compared to non-specific approaches.
3Adaptability or versatility
If multiple S1PR modulators are combined in a single composition, then comprehensive receptor modulation is achieved, but formulation complexity increases
Solution Approach 1:
The patent merges multiple S1PR modulators (S1PR1 agonists, S1PR2 agonists, S1PR3 antagonists) into a single pharmaceutical composition. This combination allows simultaneous modulation of multiple receptor subtypes that play different roles in muscle atrophy, achieving comprehensive protection while managing formulation complexity through integrated delivery.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition effectively prevents muscle atrophy by reducing the expression of Atrogin-1/MAFbx and maintaining muscle integrity, as demonstrated in C2C12 myotubes models, showing significant improvements in muscle morphology and gene expression profiles.
Implementation Method 1
The present invention refers to a pharmaceutical composition of modulators of sphingosine-1-phosphate receptors (S1PR), useful in the treatment and in the prevention of sarcopenia, and of atrophy or degeneration of skeletal muscle
Implementation Method 2
S1P exerts a trophic action in isolated fibres in the excitation/contraction coupling, mainly mediated by S1P receptors
Data Source
AI summary
The present invention relates to a pharmaceutical composition useful in the prevention and treatment of atrophy or of degeneration of skeletal muscle caused by pathologies or of sarcopenia. The composition includes a combination of molecules that are modulators of the sphingosine-1-phosphate receptors S1PR and one or more pharmaceutically acceptable excipients and/or carriers.