Regulatable CAR With Dimerization Switch For Immune Control

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Solution Overview

Problem

Current adoptive cell transfer therapies with Chimeric Antigen Receptors (CARs) lack optimal control over immune responses, leading to potential safety and efficacy issues in targeting and inactivating cancer cells.

Innovation Solution

Development of regulatable chimeric antigen receptors (RNKR-CARs and RCAR/NKR-CARs) with a dimerization switch mechanism that separates binding and signaling domains, allowing external control over immune effector responses through the use of dimerization molecules, enabling temporal regulation of immune activation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If CAR molecules are used to target and inactivate cancer cells, then cancer cell targeting efficacy is improved, but safety control and specificity are worsened due to lack of temporal regulation

Engineering Contradiction:
Improvecancer cell targeting efficacyVSAvoidsafety control
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The CAR molecule is designed with a dimerization switch that allows dynamic control between active and inactive states. The switch domain can be regulated by external stimuli such as small molecules or antibodies, enabling temporal control over the immune effector response. This dynamic regulation mechanism allows the CAR to be activated only when needed, improving safety control while maintaining cancer cell targeting efficacy.

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The CAR molecule is divided into separate functional domains: an antigen binding domain, a transmembrane domain, a switch domain, and a signaling domain. The switch domain is further segmented into two separate domains that must dimerize to activate signaling. This segmentation allows independent control of different functional aspects, enabling temporal regulation of CAR activation while preserving targeting capability.

Inventive Principle:
Principle #1Segmentation

2Productivity

If CAR activation is continuously active, then cancer cell inactivation is improved, but off-target effects and toxicity are worsened

Engineering Contradiction:
Improvecancer cell inactivation rateVSAvoidoff-target effects
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The CAR activation is designed to be periodic rather than continuous. The dimerization switch can be activated and deactivated in response to external stimuli, creating pulsed activation cycles. This periodic action allows the CAR to eliminate cancer cells during active phases while remaining inactive during other phases, thereby reducing off-target effects and toxicity associated with continuous activation.

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

A dimerization molecule or antibody serves as an intermediary to control CAR activation. This intermediary binds to the switch domain and facilitates dimerization only when present, acting as a temporal gatekeeper. The intermediary mechanism ensures that CAR activation occurs only under specific conditions, preventing unwanted off-target effects while maintaining the ability to inactivate cancer cells when needed.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of manufacture

If the CAR structure is simplified for ease of manufacture, then manufacturing complexity is reduced, but control over immune response timing is worsened

Engineering Contradiction:
ImproveCAR construction simplicityVSAvoidtemporal control capability
Core Design Contradiction:
Ease of manufactureVSEase of operation

Solution Approach 1:

The dimerization switch incorporates an intermediary binding interface that can be targeted by small molecules or antibodies. This intermediary mechanism adds temporal control capability without significantly complicating the overall CAR structure. The switch domain can be designed using standard protein engineering techniques, maintaining ease of manufacture while enabling precise control over immune response timing through external modulation of the dimerization interface.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 approach enhances the safety and efficacy of immune responses by providing temporal control over CAR activation, reducing off-target effects and improving the specificity and effectiveness of cancer cell targeting.

Implementation Method 1

activation of signaling through the CAR only occurs when the switch domains, and hence the binding domain and the signaling domain, are brought together by a dimerization molecule

Methodology Applied
Scientific EffectDimerization:

Data Source

PatentEP3811970A1Regulatable chimeric antigen receptor
Publication Date: 2021.04.28 NOVARTIS AG
  • EP3811970A1 patent drawingFigure 1
  • EP3811970A1 patent drawingFigure 2
  • EP3811970A1 patent drawingFigure 3

AI summary

Provided are compositions and methods relating to regulatable chimeric antigen receptors (RCARs), natural killer cell receptor CARs (NKR-CARs), and regulatable NKR-CARs (RNKR-CARs), where the intracellular signaling or proliferation of the RCAR or RNKR-CAR can be controlled to optimize the use of an RCAR/NKR-CAR- or RNKR-CAR-expressing cell to provide an immune response. Cells can be engineered to express a RNKR-CAR or to express a RCAR and a NKR-CAR (e.g., inhibitory NKR-CAR). For example, a RCAR or RNKR-CAR can comprise a dimerization switch that, upon the presence of a dimerization molecule, can couple an intracellular signaling domain to an extracellular recognition element, e.g., an antigen binding domain, an inhibitory counter ligand binding domain, or costimulatory ECD domain. An RCAR or RNKR-CAR can be engineered to include an appropriate antigen binding domain that is specific to a desired antigen target and used in the treatment of a disease.