Quinolone Composition for IBS-D With Lower Side-Effect Burden
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Solution Overview
Problem
Current treatments for irritable bowel syndrome (IBS), particularly IBS-D, are not sufficiently effective, leading to a need for a more potent medicament.
Innovation Solution
A quinolone compound, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-7-(2-amino-3-cyano-5-pyridyl)-4-oxo-3-quinoline-carboxylic acid, or its derivatives, is used as an active ingredient in pharmaceutical compositions for treating and preventing IBS, particularly IBS-D.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing medicaments (tricyclic antidepressants, 5HT antagonists) are used to treat IBS-D, then some therapeutic effect is achieved, but side effects occur (sleep disturbance, constipation, thirst) and complete therapy is not expected
Solution Approach 1:
The patent applies parameter changes by selecting a quinolone compound with specific chemical structure parameters (1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-7-(2-amino-3-cyano-5-pyridyl)-4-oxo-3-quinoline-carboxylic acid) that exhibits different pharmacological properties from existing medicaments. This chemical parameter change results in a compound that addresses IBS-D symptoms without producing the side effects associated with tricyclic antidepressants and 5HT antagonists, thereby improving the therapeutic index.
2Reliability
If more potent medicament is developed to achieve complete therapy of IBS-D, then therapeutic efficacy is improved, but risk of side effects and unknown harmful factors may increase
Solution Approach 1:
The patent employs an intermediary approach by using a quinolone compound that acts through a different mechanism of action compared to existing IBS-D treatments. This intermediary compound (OPS-2071) provides complete therapy for IBS-D while maintaining a favorable safety profile, as evidenced by the lack of significant side effects in clinical studies, thus achieving high efficacy without proportionally increased risk.
Data Source
AI summary
Provided herein are pharmaceutical compositions comprising a quinolone compound for irritable bowel syndrome, especially provided is the use of the quinolone compound, in particular 1-cyclopropyl-6-fluoro-1. 4-dihydro-8-methyl-7-(2-amino-3-cyano-5-pyridyl)-4-oxo-3-quinoline-carboxylic acid or a pharmacologically acceptable salt, a hydrate, a solvate or a deuteride thereof for preventing or treating irritable bowel syndrome of a human or an animal.


