Thiamine Derivative Composition for Non-Surgical Hypercortisolism Control
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Solution Overview
Problem
Current treatments for hypercortisolism, such as surgical operations and conventional medications, are invasive or have significant side effects, necessitating the development of effective, non-invasive therapeutic agents to inhibit cortisol overproduction.
Innovation Solution
A pharmaceutical and food composition containing thiamine derivatives like allithiamine, fursultiamine, and benfotiamine, which inhibit cortisol secretion and alleviate symptoms of hypercortisolism without surgical intervention or side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If adrenalectomy is performed to normalize hypersecretion of cortisol, then cortisol levels are controlled, but continuous steroid hormone supplementation is required and surgical risks are involved
Solution Approach 1:
The patent extracts and targets the specific enzyme 11β-hydroxylase (CYP11B1) responsible for cortisol synthesis in the adrenal glands. By using selective inhibitors that block only this enzyme while sparing other steroidogenic pathways, the treatment achieves cortisol control without requiring complete adrenalectomy or continuous hormone supplementation.
Solution Approach 2:
The patent introduces selective 11β-hydroxylase inhibitors as intermediary substances that mediate between the adrenal glands and cortisol production. These inhibitors act as reversible blockers of the specific enzymatic pathway, providing controlled cortisol reduction while maintaining other essential steroid hormone functions.
2Reliability
If radiation therapy is applied to the pituitary gland for patients who cannot undergo surgery, then cortisol secretion may be reduced, but it takes a long time to exhibit sufficient therapeutic effects and pituitary dysfunction is likely to develop
Solution Approach 1:
The patent replaces the mechanical/radiation-based approach (radiation therapy to pituitary gland) with a biochemical approach using selective enzyme inhibitors. This substitution acts directly on the adrenal enzyme system rather than requiring time-consuming radiation effects on the pituitary, providing faster therapeutic response.
Solution Approach 2:
The patent segments the steroidogenesis pathway by specifically targeting only the 11β-hydroxylase step in cortisol synthesis, while leaving other steroidogenic pathways intact. This selective segmentation allows for rapid cortisol control without the need for broad pituitary suppression that would cause dysfunction.
3Reliability
If enzyme inhibitors such as metyrapone, aminoglutethimide, and ketoconazole are used to inhibit cortisol synthesis, then cortisol production is reduced, but these medications have undefined medicinal effects and many side effects
Solution Approach 1:
The patent applies local quality by designing inhibitors with high specificity for the 11β-hydroxylase enzyme located in the adrenal cortex. The selective inhibitors (e.g., metyrapone, aminoglutethimide, ketoconazole at appropriate doses) are administered to achieve localized inhibition of cortisol synthesis in the adrenal glands while minimizing effects on other organs and steroidogenic pathways.
Solution Approach 2:
The patent optimizes the dosage parameters of selective 11β-hydroxylase inhibitors to achieve therapeutic cortisol suppression while staying below thresholds that cause side effects. By carefully controlling the concentration and dosing frequency, the treatment maintains effective cortisol inhibition without triggering the undefined medicinal effects and adverse reactions associated with higher or unoptimized doses.
Data Source
AI summary
The present invention relates to a composition for prevention or treatment of hypercortisolemia, the composition comprising allithiamine, fursultiamine, and benfotiamine, which are all derivatives of thiamine, or a mixed composition thereof. The composition for prevention or treatment of hypercortisolemia of the present invention can effectively treat or alleviate symptoms or disorders resulting from excessive secretion of cortisol, without surgical operations, and does not exhibit side effects caused by conventional medications.