Polymer Agonists for Mu Opioid Receptor Pain Relief
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Solution Overview
Problem
Current opioid medications are limited by negative side effects such as abuse liability, respiratory depression, and cognitive and motor impairment, and they often fail to provide adequate pain relief for the majority of patients experiencing acute or chronic pain.
Innovation Solution
Development of polymers and their modified forms that act as μ-opioid receptor agonists, specifically linear and cyclic polymers comprising 4 to 6 residues, which can be conjugated with various moieties to enhance solubility and efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional opioid medications are used to provide pain relief, then analgesic efficacy is achieved, but negative side effects such as abuse liability, respiratory depression, and cognitive impairment occur
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of opioid compounds through polymerization and conjugation with various moieties. This transforms traditional small-molecule opioids into polymer structures with altered pharmacological properties, maintaining analgesic efficacy while reducing abuse liability and respiratory depression through changed molecular characteristics
Solution Approach 2:
The patent employs composite materials by creating conjugated polymers that combine opioid pharmacophores with various functional moieties. These composite structures integrate the analgesic function with modified pharmacokinetic and pharmacodynamic properties, achieving pain relief with reduced side effects through the synergistic combination of multiple chemical components
2Reliability
If existing opioid drugs are administered to patients, then some pain relief is provided, but adequate relief is not achieved for the majority of patients due to limited efficacy and excessive side effects
Solution Approach 1:
The patent applies local quality by creating polymers with specific localized functional groups and moieties at different positions along the polymer chain. This allows different regions of the molecule to provide different functions - maintaining receptor binding affinity for analgesia while other regions provide solubility, stability, or reduced abuse potential, thereby improving overall therapeutic performance
Solution Approach 2:
The patent uses segmentation by dividing the opioid molecule into repeating polymer units with 4 to 6 residues. This segmentation allows for modular design where each residue can be optimized for specific functions, and the overall polymer structure can be tuned to achieve both adequate pain relief and reduced side effects across different patient populations
Data Source
AI summary
The subject invention provides compositions and methods for alleviating pain. Specifically, the subject invention provides pharmaceutical formulations of polymers, and/or their salts, having advantageous μ-opioid receptor binding activity.