Anti-CEA Immunoconjugates Targeting Inaccessible Tumors

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Solution Overview

Problem

Current compositions and methods for delivering antibodies and immune adjuvants are inadequate for accessing inaccessible tumors, limiting treatment options for cancer patients.

Innovation Solution

Development of immunoconjugates comprising an anti-Carcinoembryonic Antigen (CEA) antibody conjugated to 8-phenyl-2-aminobenzazepine derivatives, which allows for the covalent binding of the antibody to a linker and subsequent attachment of 8-Phe-2-aminobenzazepine moieties, facilitating targeted cancer treatment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If conventional antibody delivery compositions are used, then the treatment approach is simple, but the ability to access inaccessible tumors is limited

Engineering Contradiction:
Improveaccess to inaccessible tumorsVSAvoidcomposition complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent combines an anti-CEA antibody with a cytotoxic payload (8-phenyl-2-aminobenzazepine derivative) into a single immunoconjugate molecule. This merging allows the antibody to deliver the toxic payload directly to CEA-expressing tumor cells, enabling access to inaccessible tumors while maintaining a manageable composition structure through covalent bonding via a linker.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If immunoconjugates with covalent binding are used, then targeted cancer treatment is enhanced, but the manufacturing process becomes more complex

Engineering Contradiction:
Improvetargeted treatment effectivenessVSAvoidconjugation process complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs a linker molecule as an intermediary to facilitate the covalent bonding between the anti-CEA antibody and the 8-phenyl-2-aminobenzazepine derivative. This intermediary approach enables stable conjugation while providing a controlled manufacturing process, balancing targeted treatment effectiveness with manufacturability through standardized conjugation chemistry.

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

The immunoconjugates enable effective targeting and treatment of cancer by enhancing the delivery of antibodies to tumors, expanding treatment options and improving therapeutic outcomes.

Implementation Method 1

an anti-CEA antibody covalently attached to a linker which is covalently attached to one or more 8-Phe-2-aminobenzazepine moieties

Methodology Applied
Scientific EffectCovalent bonding: Chemical Bonding

Data Source

PatentUS20240238430A1Anti-CEA immunoconjugates, and uses thereof
Publication Date: 2024.07.18 BOLT BIOTHERAPEUTICS INC
  • US20240238430A1 patent drawing
  • US20240238430A1 patent drawing
  • US20240238430A1 patent drawing

AI summary

The invention provides immunoconjugates of Formula I comprising an anti-CEA antibody linked by conjugation to one or more 8-phenyl-2-aminobenzazepine derivatives. The invention also provides 8-phenyl-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.