Anti-CD79b Immunoconjugates with Cleavable Linkers

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Solution Overview

Problem

There is a need for agents that specifically target CD79b for the diagnosis and treatment of CD79b-associated conditions, such as cancer, as existing technologies lack effective solutions for targeting this antigen.

Innovation Solution

Development of anti-CD79b antibodies and immunoconjugates comprising these antibodies covalently attached to cytotoxic agents like pyrrolobenzodiazepines, with specific amino acid sequences for the antibody variable regions, and a cleavable linker for targeted therapy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing technologies are used for targeting CD79b, then general cancer treatment approaches can be applied, but specific and effective targeting of CD79b is not achieved

Engineering Contradiction:
Improvetargeting effectivenessVSAvoidspecificity to CD79b
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces anti-CD79b antibodies as intermediary molecules that specifically recognize and bind to the CD79b antigen on B-cell surfaces. These antibodies serve as mediators between the therapeutic agent and the target cells, enabling selective targeting of CD79b-positive cancers while sparing other cell types. The antibodies can be conjugated to cytotoxic agents, radioisotopes, or other therapeutic molecules to deliver targeted therapy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention applies local quality by designing therapeutic agents with specific binding properties for CD79b-expressing cells. The anti-CD79b antibodies exhibit high affinity and specificity for their target antigen, concentrating the therapeutic effect locally at the site of CD79b-positive tumor cells. This localized action maximizes therapeutic effectiveness while minimizing off-target effects on healthy tissues.

Inventive Principle:
Principle #3Local quality

2Object-affected harmful factors

If non-specific chemotherapy agents are used, then broad cancer cell killing is achieved, but damage to healthy cells and lack of targeted therapy occurs

Engineering Contradiction:
Improvecollateral damage to healthy cellsVSAvoidtherapeutic agent concentration at target site
Core Design Contradiction:
Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The anti-CD79b antibody serves as a selective intermediary that guides the therapeutic agent specifically to CD79b-positive cancer cells. By conjugating the antibody to cytotoxic agents, the system ensures that the harmful substance is delivered only to target cells expressing the CD79b antigen, thereby minimizing collateral damage to healthy cells while maintaining high therapeutic concentration at the tumor site.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The therapeutic system exhibits local quality by concentrating the cytotoxic agent specifically at CD79b-positive tumor cells through antibody-antigen binding. This localized delivery mechanism creates a high concentration of therapeutic agent at the target site while keeping the concentration in healthy tissues negligible, thus achieving selective cytotoxicity without widespread damage to normal cells.

Inventive Principle:
Principle #3Local quality

3Reliability

If antibody-drug conjugates are developed with specific sequences, then targeted therapy is achieved, but complexity of antibody design and manufacturing increases

Engineering Contradiction:
Improvetargeted therapy effectivenessVSAvoidantibody structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The antibody is designed with segmented functional regions including variable domains (VH and VL) with specific hypervariable regions (HVRs) for antigen binding, and constant regions for effector functions. This segmentation allows independent optimization of binding affinity, specificity, and therapeutic activity. The modular structure facilitates rational design and engineering of antibody-drug conjugates with tailored properties for targeted therapy.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention employs parameter changes by modifying specific amino acid sequences in the antibody's hypervariable regions to optimize binding affinity and specificity for CD79b. By adjusting sequence parameters such as complementarity determining region (CDR) compositions and lengths, the antibody can be fine-tuned for maximum effectiveness while maintaining structural integrity and manufacturability.

Inventive Principle:
Principle #35Parameter changes

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 effectively bind to CD79b-positive cancer cells, inhibiting cell proliferation and providing a targeted therapeutic approach for CD79b-associated cancers, including lymphomas and leukemias.

Implementation Method 1

an antibody that binds CD79b

Methodology Applied
Scientific EffectAntigen-antibody binding:

Implementation Method 2

the immunoconjugate comprises a cleavable linker degraded by a protease

Methodology Applied
Scientific EffectProtease cleavage: Enzyme

Data Source

PatentEP2869850B1Immunoconjugates comprising Anti-CD79b antibodies
Publication Date: 2017.08.23 GENENTECH INC
  • EP2869850B1 patent drawingFigure 1A
  • EP2869850B1 patent drawingFigure 1B
  • EP2869850B1 patent drawingFigure 2A

AI summary

The invention provides immunoconjugates comprising anti-CD79b antibodies covalently attached to a pyrrolobenzodiazepine and methods of using the same.