Humanized PD-L1 Rodent Models for Accurate Cancer Drug Screening

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Solution Overview

Problem

Current cancer drug development methods, particularly those involving antibody drugs targeting immunological checkpoints, face challenges due to the inability of traditional in vitro and in vivo screening approaches to accurately replicate human tumor microenvironments, leading to high failure rates and discrepancies between animal and clinical trial results.

Innovation Solution

The development of genetically modified rodents expressing human or chimeric PD-L1 proteins, allowing for the creation of humanized animal models that can accurately mimic human PD-L1 target sites, facilitating drug screening and evaluation, and enabling the study of PD-L1 function and cancer therapy efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If traditional in vitro screening approaches are used, then drug development can proceed with simpler methods, but the results cannot accurately reflect human tumor microenvironment and lead to high failure rates

Engineering Contradiction:
Improvesimplicity of screening methodVSAvoidaccuracy of drug screening results
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the biological parameters of the animal model by introducing humanized immune system components (human T cells, human PD-L1 expression) into immunodeficient mice. This parameter change enables the model to better replicate human tumor microenvironment while maintaining the ease of in vivo experimentation, thus resolving the contradiction between screening simplicity and result accuracy.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses humanized animal models as an intermediary system between in vitro screening and clinical trials. These models serve as a bridge that incorporates human biological elements (human immune cells, human PD-L1 targets) within an animal physiology framework, allowing drug screening to occur in a living system that more accurately predicts human response while avoiding the complexity and ethical constraints of human clinical trials.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If conventional experimental animals are used for in vivo pharmacological tests, then animal experimentation can be conducted with existing models, but the test results cannot reflect real human disease state and targeting site interactions

Engineering Contradiction:
Improveavailability of existing animal modelsVSAvoidaccuracy of disease state representation
Core Design Contradiction:
Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent applies local quality by selectively humanizing specific components of the animal model rather than attempting to create a fully human system. Specifically, the mice are engineered to express human PD-L1 on tumor cells and/or human immune cells while maintaining mouse physiology for other functions. This localized humanization provides accurate representation of the PD-L1 target site and immune interactions without requiring complete humanization of the organism.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent creates a composite biological system combining mouse physiology with human cellular and molecular components. The humanized animal model consists of mouse tissue structures populated with human immune cells and human PD-L1 expression, forming a hybrid system that leverages the advantages of both species - the controllable physiology of mice combined with the human-specific target molecules and immune responses.

Inventive Principle:
Principle #40Composite materials

3Reliability

If humanized animal models are developed to accurately mimic human PD-L1 target sites, then drug screening accuracy improves, but model complexity and development costs increase

Engineering Contradiction:
Improveaccuracy of drug screening resultsVSAvoidcomplexity of animal model
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent implements partial humanization by introducing only the specific human elements necessary for PD-L1 target validation - namely human PD-L1 expression in tumor cells and/or human immune cell components - rather than attempting full humanization of the animal model. This partial approach provides sufficient accuracy for antibody screening against human PD-L1 while avoiding the excessive complexity and costs associated with complete humanization.

Inventive Principle:
Principle #16Partial or excessive action

Data Source

PatentEP3507373B1Genetically modified non-human animal with human or chimeric PD-l1
Publication Date: 2023.09.13 BIOCYTOGEN PHARMACEUTICALS (BEIJING) CO LTD
  • EP3507373B1 patent drawingFigure 1
  • EP3507373B1 patent drawingFigure 2
  • EP3507373B1 patent drawingFigure 3

AI summary

Disclosed is a genetically modified expressing human or chemeric (e. g., humanized) programmed death-ligand 1 (PD-L1, PDL1, or B7-H1), and methods of use thereof.