Chymotrypsinogen–Trypsinogen Composition for Tumor-Surface Activation
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Solution Overview
Problem
There is a need for new or improved cancer treatments, particularly those that effectively utilize chymotrypsinogen and trypsinogen to target and treat various types of cancer, including pancreatic and ovarian cancer, while minimizing adverse effects.
Innovation Solution
A composition comprising chymotrypsinogen and trypsinogen, administered at significantly higher doses than previously used, is used to treat cancer, with the amounts ranging from 0.1 mg/kg to 500 mg/kg for chymotrypsinogen and 0.02 mg/kg to 80 mg/kg for trypsinogen, without causing significant adverse clinical events.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If higher doses of chymotrypsinogen and trypsinogen are administered, then therapeutic efficacy is improved, but risk of adverse effects increases
Solution Approach 1:
The patent applies parameter changes by administering chymotrypsinogen and trypsinogen at significantly higher doses than previously used (chymotrypsinogen: 0.1-500 mg/kg, trypsinogen: 0.02-80 mg/kg). This dosage optimization resolves the contradiction by identifying a therapeutic window where high doses achieve superior tumor regression while maintaining safety through selective activation at tumor cell surfaces rather than systemic distribution
Solution Approach 2:
The patent uses the tumor cell surface as an intermediary that selectively activates the proenzymes. The proenzymes chymotrypsinogen and trypsinogen remain inactive during circulation and are selectively converted to active enzymes at the tumor cell surface, enabling high dosing without systemic adverse effects. This intermediary mechanism allows the proenzymes to reach tumor sites in high concentrations while avoiding harmful effects in healthy tissues
2Adaptability or versatility
If proenzymes are used instead of active enzymes, then selectivity at tumor surface is improved, but activation efficiency may be reduced
Solution Approach 1:
The patent applies preliminary action by administering the proenzymes in inactive form that will be activated at the target site. The proenzymes chymotrypsinogen and trypsinogen are circulated to tumor sites in inactive form, ensuring selective accumulation, and then activated locally at the tumor cell surface. This preliminary delivery of inactive precursors resolves the contradiction by achieving both selectivity (through targeted accumulation) and efficiency (through local activation at high concentrations)
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 higher doses of chymotrypsinogen and trypsinogen effectively reduce tumor weight and provide a broader therapeutic window for cancer treatment, including pancreatic and ovarian cancer, with minimal adverse effects.
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 relates to compositions, methods, uses and kits for treating cancer. In particular, the invention relates to compositions and methods of treating cancer in a subject comprising administering chymotrypsinogen in certain amounts, for example greater than about 0.1 mg/kg, and trypsinogen in an amount, for example, greater than about 0.02 mg/kg, thereby treating cancer. The invention also relate to compositions and methods for treating cancer in a subject comprising chymotrypsinogen and trypsinogen wherein the weight ratio of chymotrypsinogen:trypsinogen is greater than 8:1.