Bispecific Anti-CD3/CD20 Formulation for Aggregation Stability

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Solution Overview

Problem

Bispecific antibodies targeting CD3 and CD20 are susceptible to degradation, aggregation, and instability under high-temperature conditions or shear stress, posing challenges for production, storage, and administration.

Innovation Solution

A liquid or lyophilized powder formulation of the bispecific anti-CD3/CD20 polypeptide complex using buffers like histidine salt, succinate, and citrate buffers, along with saccharides such as trehalose, and surfactants like polysorbate 80, to maintain stability and biological activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If bisspecific anti-CD3/CD20 polypeptide complex is used for therapy, then therapeutic effect is improved, but stability under high-temperature conditions or shear stress deteriorates

Engineering Contradiction:
Improvetherapeutic effectVSAvoidstability under high-temperature conditions or shear stress
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by optimizing formulation conditions including pH (5.0-7.5), temperature (2-8°C storage), concentration (0.1-50 mg/mL), and composition (buffers, excipients, surfactants) to achieve stable bispecific antibody formulations that maintain therapeutic efficacy while resisting degradation under various storage and transport conditions

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating complex formulations that combine bisspecific antibodies with multiple excipients including buffers (histidine, succinate, citrate), saccharides (trehalose, sucrose), amino acids (arginine, glycine, proline), and surfactants (polysorbate 80, poloxamer 188) to enhance stability while maintaining therapeutic function

Inventive Principle:
Principle #40Composite materials

2Reliability

If bisspecific antibody drugs are used, then therapeutic capability is improved, but susceptibility to degradation, aggregation or unwanted chemical modifications increases

Engineering Contradiction:
Improvetherapeutic capabilityVSAvoiddegradation, aggregation or unwanted chemical modifications
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary anti-action by incorporating stabilizing excipients and protective agents in the formulation that prevent degradation, aggregation, and chemical modifications before they can occur during storage and transport, thereby preserving therapeutic capability

Inventive Principle:
Principle #9Preliminary anti-action

Solution Approach 2:

The patent creates an inert environment through the use of stabilizing buffers and excipients that provide a protective chemical environment, preventing unwanted interactions between the bisspecific antibody and external factors that could cause degradation or aggregation

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

3Stability of the object's composition

If bisspecific polypeptide complex formulation is developed, then stability during storage is improved, but formulation complexity increases

Engineering Contradiction:
Improvestability during storageVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent applies universality by selecting excipients that perform multiple functions simultaneously - for example, buffers that maintain pH stability while also acting as stabilizers, and saccharides that provide both structural support and protection against aggregation, thereby managing formulation complexity

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP4190352B1Formulation of novel bispecific Anti-CD3/CD20 polypeptide complex
Publication Date: 2026.03.25 CHIA TAI TIANQING PHARMA GRP CO LTD
  • EP4190352B1 patent drawingFigure 1
  • EP4190352B1 patent drawingFigure 2A~2B
  • EP4190352B1 patent drawingFigure 3A~3B

AI summary

The present invention provides a novel bispecific anti-CD3/CD20 polypeptide complex formulation containing a first antigen-binding portion and a second antigen-binding portion. Specifically, the formulation comprises a liquid formulation and a lyophilized formulation.