Enteric-Coated TTM Formulation for Cancer Treatment
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Solution Overview
Problem
Current cancer treatments face challenges in effectively targeting angiogenesis and inflammation, with existing therapies often having limited efficacy and side effects, particularly in regulating copper levels and managing inflammation in cancer patients.
Innovation Solution
The use of a copper chelator, tetrathiomolybdate (TTM), in combination with diethylcarbamazine (DEC) and astaxanthin (ATX), administered in an enteric-coated, extended-release formulation to control copper levels and reduce inflammation, thereby inhibiting angiogenesis and inflammation pathways.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If copper chelators are administered to reduce copper levels in cancer treatment, then angiogenesis is inhibited, but side effects increase and bioavailability is reduced
Solution Approach 1:
The enteric coating is applied to TTM tablets in advance to protect them from gastric acid degradation before administration. This preliminary protective action ensures that the active ingredient remains intact until it reaches the intestine, where it can be properly absorbed and exert its anti-angiogenic effect without being neutralized by stomach acid, thereby reducing side effects while maintaining efficacy
Solution Approach 2:
The enteric coating acts as an intermediary barrier between the gastric acid environment and the TTM active ingredient. This intermediary layer protects the copper chelator from direct contact with harmful gastric acid, allowing it to pass through the stomach intact and release its active form in the intestine, thus reducing side effects while preserving anti-angiogenic efficacy
2Reliability
If TTM is administered to inhibit angiogenesis, then copper levels are reduced, but treatment compliance decreases due to multiple daily dosing requirements
Solution Approach 1:
The invention transitions from static immediate-release tablets requiring multiple daily administrations to dynamic extended-release tablets that continuously release TTM over 24 hours. This dynamic release mechanism maintains therapeutic copper depletion levels throughout the day, preserving anti-angiogenic efficacy while reducing dosing frequency to once daily, thereby significantly improving patient compliance
Solution Approach 2:
The extended-release formulation ensures continuous therapeutic action of TTM throughout the 24-hour dosing interval. By maintaining sustained copper depletion levels in the body, the formulation preserves continuous anti-angiogenic efficacy while requiring only once-daily administration, thus improving patient compliance without sacrificing treatment effectiveness
3Speed
If TTM is released in the stomach, then rapid copper chelation occurs, but the drug is destroyed by gastric acid
Solution Approach 1:
The enteric coating serves as a protective intermediary that shields TTM from gastric acid during stomach passage. This intermediary layer prevents acid-mediated degradation of the drug, ensuring it reaches the intestine in its active form where rapid copper chelation can occur without prior destruction, thus maintaining both drug stability in the stomach and rapid chelation speed in the intestine
Solution Approach 2:
The enteric coating creates a protective copy or replica layer over the TTM tablet, mimicking a barrier that prevents gastric acid from directly contacting and destroying the active ingredient. This protective copy allows the drug to survive the stomach environment intact and exert its rapid copper chelation effect in the intestine, preserving both stability and speed
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
This combination provides a more effective and controlled release of TTM, reducing side effects and enhancing bioavailability, leading to improved treatment outcomes for cancer and pulmonary arterial hypertension by inhibiting angiogenesis and inflammation, and improving patient compliance with once-a-day dosing.
Implementation Method 1
The copper chelator includes TTM
Implementation Method 2
administered in an enteric-coated, extended-release formulation
Implementation Method 3
The aim of copper depletion therapy is to decrease copper to a level where the signaling pathways of cytokines can be reduced
Implementation Method 4
due to its high redox activity (a process in which one substance or molecule is reduced and another oxidized; oxidation and reduction being considered together as complementary, processes) and its ability to catalyze the production of free radicals
Data Source
AI summary
Pharmaceutical compositions containing tetrathiomolybdate (TTM) are disclosed. Pharmaceutical compositions and formulations that contain TTM along with other co-drugs, such as diethylcarbamazine (DEC) and astaxanthin (ATX), are also disclosed. Formulations include a delayed release oral form that releases the TTM in the gastrointestinal tract after the oral form passes the stomach, and an enteric oral form that is not a delayed release form are disclosed. Methods of treating cancer, treating cancer patients as an adjuvant therapy, and treating pulmonary arterial hypertension by administering the pharmaceutical compositions are further disclosed.