Multispecific Binding Protein Purification via Affinity Tag

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Solution Overview

Problem

The development of multispecific binding proteins, such as bispecific antibodies, is hindered by the complexity of assembly, manufacturing, and purification, leading to reduced yields and increased costs due to the formation of undesired molecules and impaired effector functions, immunogenicity concerns, and altered pharmacokinetic properties.

Innovation Solution

The development of multispecific binding proteins with specific amino acid residues in their antigen binding domains, such as kappa light chain Fab regions with lysine and aspartic acid modifications, which enhance purification efficiency, stability, and reduce immunogenicity risk, while maintaining affinity and assembly, using affinity chromatography for purification.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If traditional recombinant expression methods are used to produce multispecific binding proteins, then the proteins can be manufactured, but a mixture including undesired molecules (monospecific proteins, single chain pairs) is expressed requiring additional purification steps

Engineering Contradiction:
Improveyield of desired multisspecific binding proteinVSAvoidcomplexity of assembly, manufacturing and purification
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent introduces a purification tag sequence at the N-terminus of the light chain constant region before recombinant expression. This preliminary action enables selective purification of the desired multisspecific binding protein from the expression mixture, preventing the yield reduction that would otherwise result from complex purification requirements.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The purification tag acts as an intermediary element that facilitates the separation of desired multisspecific binding proteins from undesired molecules. The tag provides a specific binding site that allows purification reagents to selectively capture the target protein, simplifying the purification process and increasing yield.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Manufacturing precision

If additional purification steps are implemented to remove undesired molecules, then purification efficiency improves, but the overall manufacturing cost increases

Engineering Contradiction:
Improvepurification efficiencyVSAvoidmanufacturing cost
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

By incorporating the purification tag during the recombinant expression step, the patent prepares the protein for efficient purification in advance. This preliminary action reduces the need for multiple complex purification steps, thereby lowering manufacturing costs while maintaining high purification efficiency.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The introduction of the purification tag changes the physical-chemical parameters of the protein molecule, adding a specific sequence that provides selective binding properties. This parameter change enables a single effective purification step using affinity chromatography, reducing both time and cost compared to traditional multi-step purification protocols.

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If purification tags or other modifications are added to enhance purification, then purification efficiency improves, but the time and cost of the purification process increase

Engineering Contradiction:
Improvepurification efficiencyVSAvoidpurification process time
Core Design Contradiction:
Manufacturing precisionVSLoss of time

Solution Approach 1:

The purification tag is incorporated during the protein expression step, preparing the molecule for rapid purification before the purification process begins. This preliminary preparation enables a single-step affinity purification, saving time compared to traditional multi-step methods that would require sequential processing.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent replaces complex mechanical purification procedures with a biochemical affinity-based system. The purification tag provides specific molecular recognition that allows rapid separation using affinity chromatography, reducing the time required compared to traditional mechanical separation methods.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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 approach results in improved purification yields, reduced protein aggregation, and preserved affinity and stability of multispecific binding proteins, without increasing the time or cost of the purification process, and minimizes the risk of immunogenicity and altered pharmacokinetic properties.

Implementation Method 1

using affinity chromatography for purification

Methodology Applied
Scientific EffectAffinity chromatography: Chromatography

Data Source

PatentUS20230242671A1Multispecific binding proteins and methods of developing the same
Publication Date: 2023.08.03 ELI LILLY & CO

AI summary

Multispecific binding proteins that bind a first antigen and a second antigen and methods of purifying multispecific binding proteins.