GC-C Receptor Peptides for Gastrointestinal Motility

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Solution Overview

Problem

Current treatments for irritable bowel syndrome (IBS) and other gastrointestinal disorders are limited, with few effective prescription options available, leading to significant economic impact and reduced quality of life for patients, and there is a need for therapies that can address abdominal pain, bowel motility issues, and inflammation.

Innovation Solution

Development of pharmaceutical compositions featuring peptides that activate the guanylate cyclase C (GC-C) receptor to increase gastrointestinal motility, decrease inflammation, and alleviate pain, which can be administered alone or in combination with other therapeutic agents, and are designed to be stable and effective in treating various gastrointestinal disorders, obesity, congestive heart failure, and benign prostatic hyperplasia.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for IBS, then current therapy options are available, but the number of effective prescription options is limited and quality of life is reduced

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidnumber of treatment options
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by modifying the peptide structure (amino acid sequence, disulfide bonds, terminal modifications) to optimize GC-C receptor activation while improving therapeutic properties such as stability, solubility, and bioavailability, thereby enhancing treatment effectiveness and creating multiple effective options for IBS therapy

Inventive Principle:
Principle #35Parameter changes

2Reliability

If new peptide-based therapies are developed, then treatment effectiveness is improved, but development complexity and manufacturing challenges increase

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtherapy development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the peptide molecule into functional domains (N-terminal region, core GC-C binding region, C-terminal region) that can be independently optimized and modified. This modular approach allows systematic development of multiple peptide variants with different properties, managing complexity through structured design while maintaining effectiveness

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent uses parameter changes to systematically modify peptide properties (amino acid composition, disulfide bond configuration, terminal modifications) to optimize therapeutic effectiveness while establishing standardized development protocols that manage complexity through controlled variation of key parameters

Inventive Principle:
Principle #35Parameter changes

3Reliability

If peptides are designed for enhanced stability and efficacy, then treatment performance is improved, but manufacturing and formulation challenges increase

Engineering Contradiction:
Improvetherapeutic performanceVSAvoidformulation ease
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies the extraction principle by isolating and optimizing the critical functional elements of the peptide (GC-C binding region, disulfide bond structure) while removing or modifying non-essential portions. This allows focused manufacturing on the core active structure and simplifies formulation by concentrating on stabilizing the essential functional domains

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs composite materials by combining the peptide with excipients, carriers, or delivery systems that enhance stability and facilitate manufacturing. The peptide itself represents a composite structure with multiple disulfide bonds and modified amino acids working together to achieve both stability and efficacy while enabling practical formulation

Inventive Principle:
Principle #40Composite materials

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 peptides effectively treat IBS and other gastrointestinal disorders by enhancing motility, reducing pain and inflammation, and offer potential benefits for obesity and congestive heart failure, providing a more effective alternative to existing treatments.

Implementation Method 1

peptides that activate the guanylate cyclase C (GC-C) receptor to increase gastrointestinal motility

Methodology Applied
Scientific EffectReceptor activation:

Implementation Method 2

decrease inflammation

Methodology Applied
Scientific EffectAnti-inflammatory effect:

Implementation Method 3

alleviate pain

Methodology Applied
Scientific EffectAnalgesic effect:

Data Source

PatentUS7772188B2Methods and compositions for the treatment of gastrointestinal disorders
Publication Date: 2010.08.10 IRONWOOD PHARMACEUTICALS INC
  • US7772188B2 patent drawing
  • US7772188B2 patent drawing
  • US7772188B2 patent drawing

AI summary

The present invention features compositions and related methods for treating IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, Inflammatory bowel disease, functional heartburn, dyspepsia (including functional dyspepsia or nonulcer dyspepsia), gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), and disorders and conditions associated with constipation, e.g., constipation associated with use of opiate pain killers, post-surgical constipation (post-operative ileus), and constipation associated with neuropathic disorders as well as other conditions and disorders using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.