IL-23R Peptide Inhibitors With Enteric Coating for Oral IBD Therapy
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Solution Overview
Problem
There is a need for new therapeutics that specifically target the IL-23 pathway to treat and prevent IL-23-associated diseases, particularly those affecting the intestinal tract, such as inflammatory bowel diseases, and existing treatments face challenges in selectively targeting IL-23R in the intestine for effective intestinal inflammation treatment.
Innovation Solution
Development of novel peptide inhibitors of the interleukin-23 receptor (IL-23R) that inhibit IL-23 binding and signaling, suitable for oral administration, and can be formulated with an enteric coating to protect and release the composition in the lower gastrointestinal system.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If peptide inhibitors are administered orally, then patient compliance and ease of administration are improved, but the peptides may be degraded by gastrointestinal enzymes and acidic environments
Solution Approach 1:
The patent applies enteric coating to peptide inhibitors before administration, creating a protective barrier that prevents degradation by gastric acid and enzymes in the upper gastrointestinal tract. This preliminary protective action allows the peptide to reach the lower GI tract intact, where it can exert its therapeutic effect on IL-23R expressing cells
Solution Approach 2:
The enteric coating acts as an intermediary substance between the peptide inhibitor and the harsh gastrointestinal environment. This coating layer protects the peptide from direct contact with degrading enzymes and acidic conditions, enabling oral administration while maintaining peptide integrity until it reaches the target site
2Reliability
If antibodies targeting IL-23 or IL-23R are used, then therapeutic efficacy is improved, but the molecular weight and complexity increase, potentially limiting tissue penetration and requiring injection administration
Solution Approach 1:
The patent extracts the essential functional domain of full-length antibodies by developing peptide inhibitors that specifically target the IL-23R binding interface. These peptides contain only the minimal sequence necessary to bind IL-23R with high affinity, eliminating the need for large antibody structures while retaining therapeutic efficacy
Solution Approach 2:
The patent creates simplified peptide copies that replicate the key binding function of full-length antibodies. These peptide inhibitors mimic the critical interaction between antibodies and IL-23R, providing comparable therapeutic effects with reduced molecular complexity and the potential for oral administration
3Measurement precision
If existing peptide inhibitors are designed, then selectivity for IL-23R is improved, but stability in gastrointestinal conditions and suitability for oral administration remain challenging
Solution Approach 1:
The patent applies enteric coating to peptide inhibitors before administration, creating a protective barrier that prevents degradation by gastric acid and enzymes in the upper gastrointestinal tract. This preliminary protective action allows the peptide to reach the lower GI tract intact, where it can exert its therapeutic effect on IL-23R expressing cells
Solution Approach 2:
The patent modifies peptide sequences through systematic variation of amino acid residues to optimize both IL-23R binding affinity and stability in gastrointestinal conditions. By changing specific parameters of the peptide structure while maintaining key binding interactions, the invention achieves enhanced selectivity and stability simultaneously
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 peptide inhibitors effectively target IL-23R, reducing intestinal inflammation by inhibiting IL-23 signaling, providing therapeutic benefits for conditions like Crohn's disease and psoriasis, with potential for oral and various administration routes.
Implementation Method 1
can be formulated with an enteric coating to protect and release the composition in the lower gastrointestinal system
Implementation Method 2
peptide inhibitors that bind IL-23R to inhibit IL-23 binding and signaling
Data Source
AI summary
The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel diseases.