Stem Cell Metabolomic Ratio for Teratogenicity Prediction

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Solution Overview

Problem

Current methods for testing developmental toxicity rely on animal models, which are costly, time-consuming, and limited in predictive accuracy due to species differences, leading to missed signals and delayed safety assessments in drug development, necessitating a more efficient and human-specific in vitro testing method.

Innovation Solution

A method using undifferentiated human stem cell-like cells (hSLCs) to culture test compounds, measuring fold changes in ornithine and cystine levels, and calculating their ratio to predict teratogenicity, with ratios ≤0.88 indicating teratogenicity and >0.88 indicating non-teratogenicity, facilitating rapid and accurate classification.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If animal models are used for developmental toxicity testing, then safety assessment can be conducted, but the predictive accuracy is limited due to species differences and the process is costly and time-consuming

Engineering Contradiction:
Improvepredictive accuracyVSAvoidtesting duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent segments the complex in vivo animal testing process into simpler in vitro components by using human embryonic stem cells to model specific developmental processes. This allows toxicity assessment to be conducted on isolated cellular systems rather than whole animals, reducing complexity while maintaining human relevance.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates a simplified copy of the human developmental system using stem cell models that replicate key aspects of embryonic development. These cellular models serve as substitutes for animal models, providing human-specific predictive data without requiring actual human subjects or animal testing.

Inventive Principle:
Principle #26Copying

2Reliability

If animal models are used for developmental toxicity testing, then safety assessment can be conducted, but the cost and complexity are high

Engineering Contradiction:
Improvepredictive accuracyVSAvoidtesting complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent divides the integrated animal testing system into separate modular in vitro assays using stem cells. Each assay targets specific developmental endpoints or toxicological parameters, allowing for standardized, reproducible testing that is less complex than maintaining and managing animal studies.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent changes the fundamental parameters of the testing system by transitioning from in vivo to in vitro conditions, using human stem cells instead of animal subjects. This parameter change simplifies the system while improving human relevance, as stem cell responses more closely match human developmental responses.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If traditional animal models are used, then regulatory gold standard is met, but species differences lead to missed signals of developmental toxicity

Engineering Contradiction:
Improvehuman predictive valueVSAvoidsafety assessment timing
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent creates human-specific copies of developmental systems using stem cell models, eliminating species differences entirely. These human stem cell models provide direct human predictive value without requiring translation from animal data, capturing human-specific toxicological responses that animal models miss.

Inventive Principle:
Principle #26Copying

Solution Approach 2:

The patent enables preliminary toxicity screening using rapid in vitro stem cell assays before committing to lengthy animal studies. This preliminary action identifies potential teratogens early in the drug development process, allowing for faster decision-making and reducing the need for follow-up animal testing.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP2914748B1Predicting human developmental toxicity of pharmaceuticals using human stem-like cells and metabolomic ratios
Publication Date: 2019.03.13 STEMINA BIOMARKER DISCOVERY
  • EP2914748B1 patent drawingFigure 1A~1B
  • EP2914748B1 patent drawingFigure 2
  • EP2914748B1 patent drawingFigure 3A~3B

AI summary

This present invention provides rapid, reproducible, biomarker-based screening methods for the developmental toxicity testing of compounds. The methods are designed to identify the exposure level at which a test compound perturbs metabolism in a manner predictive of developmental toxicity. In particular, the perturbation of two metabolites, ornithine and cystine, is measured, wherein a ratio of the fold change in ornithine to the fold change in cystine of less than or equal to about 0.88 is indicative of the teratogenicity of a test compound.