Protease Proenzyme Cancer Therapy Composition
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Solution Overview
Problem
Current cancer treatments using protease enzymes face challenges with enzyme inactivation and loss during oral administration, and there is a need for enhanced compositions that effectively target cancer cells with a multi-functional approach.
Innovation Solution
A pharmaceutical composition combining a protease proenzyme, such as trypsinogen or chymotrypsinogen, with active agents like selenium compounds, vanilloid compounds, or cytoplasmic glycolysis reduction agents to enhance cell-to-cell adhesion, induce apoptosis, or promote differentiation of tumour cells, potentially reducing metastasis and improving treatment efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high dosages of protease enzymes are administered orally, then cancer treatment efficacy may be improved, but enzyme inactivation and loss through digestion and plasma serpins increases
Solution Approach 1:
The patent converts protease enzymes into their proenzyme forms (inactive precursors) before administration. These proenzymes are activated in situ at the tumor site, preventing premature inactivation during digestion and by plasma serpins. This preliminary conversion to inactive form allows the enzyme to survive administration and reach the target before becoming active.
Solution Approach 2:
The patent uses proenzymes as intermediary forms that bridge the gap between administration and activation. The proenzyme acts as a protected carrier that delivers the enzymatic potential to the tumor site without being inactivated by digestive enzymes or plasma inhibitors, then converts to the active protease form at the target.
2Reliability
If crude enzyme extracts are used to treat human cancer patients, then tumor progression reduction and survival time prolongation is achieved, but enzyme inactivation through digestion and plasma serpins occurs
Solution Approach 1:
The patent converts protease enzymes into their proenzyme forms (inactive precursors) before administration. These proenzymes are activated in situ at the tumor site, preventing premature inactivation during digestion and by plasma serpins. This preliminary conversion to inactive form allows the enzyme to survive administration and reach the target before becoming active.
Solution Approach 2:
The patent uses proenzymes as intermediary forms that bridge the gap between administration and activation. The proenzyme acts as a protected carrier that delivers the enzymatic potential to the tumor site without being inactivated by digestive enzymes or plasma inhibitors, then converts to the active protease form at the target.
3Stability of the object's composition
If protease proenzymes are used to overcome oral administration problems, then enzyme stability is improved, but treatment efficacy may be reduced without enhanced compositions
Solution Approach 1:
The patent creates composite pharmaceutical compositions that combine multiple proenzymes (such as trypsinogen and chymotrypsinogen) with complementary proteolytic activities. This composite approach ensures that even if one proenzyme is partially inactivated, others provide sufficient therapeutic effect, thereby maintaining treatment efficacy while preserving the stability benefits of proenzyme formulation.
Solution Approach 2:
The patent employs multiple proenzymes with different specificities and activation characteristics in combination. This multi-functional approach ensures broader coverage of tumor protease needs and provides redundancy, maintaining treatment efficacy while leveraging the stability of proenzyme forms.
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 composition effectively activates protease proenzymes at tumour cell surfaces, enhancing cell adhesion and inducing apoptosis or differentiation, thereby reducing tumour metastasis and improving cancer treatment outcomes.
Implementation Method 1
The mechanism of action of trypsin is believed to occur by way of proteolysis of the tumour cells
Data Source
AI summary
The present invention generally relates to pharmaceutical compositions containing a protease proenzyme and use thereof for treating cancer. The pharmaceutical compositions are directed to compositions comprising a protease proenzyme and an active agent, the composition being capable of providing a multi-functional approach for treating cancer. The pharmaceutical compositions are also directed to compositions comprising a first and a second protease proenzyme capable of activation at or near a surface of a tumor cell to enhance cell-to-cell adhesion of tumor cells, effect proteolysis of tumor cells, or induce tumor cell apoptosis, differentiation or immunorecognition, wherein the first protease proenzyme is chymotrypsinogen and the second protease proenzyme is trypsinogen. The pharmaceutical compositions are also directed to compositions comprising a first and second active agent each capable of inducing intracellular activity in tumor cells.