Anti-TIGIT Antibody Formulation for Non-Refrigerated Stability

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Solution Overview

Problem

Conventional pharmaceutical formulations for anti-TIGIT antibodies face challenges in maintaining physical and chemical stability, particularly under non-refrigerated conditions, leading to aggregation and degradation, necessitating stringent storage requirements.

Innovation Solution

A pharmaceutical formulation comprising an anti-TIGIT antibody, acetate or histidine buffer, sucrose or sorbitol as a stabilizer, and polysorbate 20 or polysorbate 80 as a surfactant, with specific pH and concentration ranges, ensuring stability under various environmental conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If protein liquid formulations are used for parenteral administration, then convenience of use is improved, but stability of the protein is worsened due to aggregation and degradation

Engineering Contradiction:
Improveconvenience of useVSAvoidprotein stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by optimizing the formulation's pH to a specific range (5.0-6.5) and incorporating stabilizing agents at controlled concentrations. These parameter adjustments create a formulation environment that prevents protein aggregation and degradation while maintaining liquid formulation convenience for parenteral administration.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces protective agents as intermediaries between the protein and the formulation environment. These stabilizing agents act as mediators that prevent direct harmful interactions between the protein and formulation components, thereby maintaining protein stability while preserving the liquid formulation's ease of administration.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Stability of the object's composition

If protective agents are added to enhance protein stability, then stability is improved, but formulation complexity increases

Engineering Contradiction:
Improveprotein stabilityVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent resolves formulation complexity by defining specific parameter ranges for stabilizing agents rather than requiring complex multi-component systems. By optimizing pH to 5.0-6.5 and using controlled concentrations of protective agents, the formulation achieves stability without excessive complexity in composition or preparation.

Inventive Principle:
Principle #35Parameter changes

3Stability of the object's composition

If stringent storage conditions are imposed to maintain stability, then stability is improved, but ease of operation and storage flexibility is worsened

Engineering Contradiction:
Improveprotein stabilityVSAvoidstorage flexibility
Core Design Contradiction:
Stability of the object's compositionVSEase of operation

Solution Approach 1:

The patent enables storage flexibility by adjusting the formulation's pH to a relatively broad range (5.0-6.5) and incorporating stabilizing agents that maintain protein stability under varied storage conditions. This allows the formulation to remain stable without requiring stringent temperature control, thereby improving ease of storage while maintaining stability.

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 formulation maintains high stability with minimal aggregation, turbidity, and pH drift, exhibiting superior thermostability and freeze-thaw stability, making it suitable for diverse storage conditions.

Implementation Method 1

the buffer is an acetate buffer or a histidine buffer

Methodology Applied
Scientific EffectBuffering:

Implementation Method 2

the stabilizer is sucrose, sorbitol, or proline

Methodology Applied
Scientific EffectStabilization:

Implementation Method 3

the surfactant is polysorbate 20 or polysorbate 80

Methodology Applied
Scientific EffectSurfactant action: Surfactant

Data Source

PatentEP4643876A1Pharmaceutical preparation comprising Anti-tigit antibody
Publication Date: 2025.11.05 SHANGHAI HENLIUS BIOTECH INC
  • EP4643876A1 patent drawingFigure 1a~2b
  • EP4643876A1 patent drawingFigure 3a~4b
  • EP4643876A1 patent drawingFigure 5a~5b

AI summary

A pharmaceutical preparation comprising an anti-TIGIT antibody, comprising an anti-TIGIT antibody, a stabilizer, a buffer solution, and a surfactant.