FkpA Purification via Multi-Step Chromatography

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Solution Overview

Problem

Current methods lack sufficient specificity and sensitivity for detecting and quantifying FkpA, a chaperone protein overexpressed in recombinant bacterial host cells, which is essential for biopharmaceutical protein folding, and existing assays fail to accurately remove product-specific impurities like non-paired antibody arms and misassembled antibodies from multispecific antibodies.

Innovation Solution

A multi-step chromatographic process involving cation exchange, hydrophobic interaction, and size exclusion chromatography is employed to purify FkpA, utilizing strong cation exchangers and specific buffers to achieve high purity, and the use of antibodies specific to FkpA for immunopurification and detection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If FkpA is overexpressed to facilitate protein folding, then protein folding and solubility improve, but host cell protein impurities increase

Engineering Contradiction:
Improveprotein foldingVSAvoidhost cell protein impurities
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies extraction by removing FkpA and other host cell protein impurities from the recombinant polypeptide product through a multi-step purification process involving affinity chromatography, ion exchange chromatography, and size exclusion chromatography, thereby resolving the contradiction between FkpA's beneficial folding function and its harmful presence as an impurity

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent discards FkpA from the final product by implementing purification steps that specifically remove this host cell protein, while recovering the recombinant polypeptide at high purity levels, thus eliminating the harmful impurity while maintaining the beneficial folding assistance during production

Inventive Principle:
Principle #34Discarding and recovering

2Productivity

If conventional chromatographic methods are used to remove impurities, then general purification is achieved, but product-specific impurities like non-paired antibody arms and misassembled antibodies remain

Engineering Contradiction:
Improvepurification efficiencyVSAvoidremoval of product-specific impurities
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

The patent segments the purification process into multiple specialized steps: affinity chromatography for initial capture, ion exchange chromatography for removing general host cell proteins, and size exclusion chromatography for separating product-specific impurities like misassembled antibodies, thereby achieving both high productivity and manufacturing precision

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs parameter changes by adjusting pH, ionic strength, and buffer conditions at different purification stages to optimize the removal of specific impurity types, enabling selective elimination of product-specific impurities while maintaining overall purification efficiency

Inventive Principle:
Principle #35Parameter changes

3Difficulty of detecting and measuring

If existing assays are used to detect FkpA, then general protein detection is possible, but specific and sensitive detection of FkpA is not achieved

Engineering Contradiction:
ImproveFkpA detectionVSAvoidFkpA quantitation
Core Design Contradiction:
Difficulty of detecting and measuringVSMeasurement precision

Solution Approach 1:

The patent introduces specific antibodies as intermediary detection reagents that selectively bind to FkpA, enabling sensitive and specific detection and quantitation of this host cell protein impurity, thereby resolving the difficulty of detecting FkpA with conventional non-specific assays

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 process achieves a high purity of FkpA with less than 2% impurities and stability through multiple freeze-thaw cycles, enabling effective detection and removal of FkpA and other impurities from recombinant polypeptides, meeting stringent pharmaceutical standards.

Implementation Method 1

applying the clarified cell lysate comprising the FkpA polypeptide to a cation exchange chromatography material

Methodology Applied
Scientific EffectCation exchange: Ion Exchange

Implementation Method 2

applying the cation exchange eluate comprising the FkpA polypeptide to a hydrophobic interaction chromatography (HIC) material

Methodology Applied
Scientific EffectHydrophobic interaction: Hydrophobe

Implementation Method 3

applying the HIC eluate comprising the FkpA polypeptide to a size exclusion chromatography material

Methodology Applied
Scientific EffectSize exclusion chromatography: Chromatography

Implementation Method 4

clarifying the cell lysate by centrifugation

Methodology Applied
Scientific EffectCentrifugation: Centrifugal Separation

Data Source

PatentEP3337819B1Method of purifying for producing recombinant polypeptides using fkpa
Publication Date: 2024.02.21 F HOFFMANN LA ROCHE & CO AG
  • EP3337819B1 patent drawingFigure 1
  • EP3337819B1 patent drawingFigure 2
  • EP3337819B1 patent drawingFigure 3A

AI summary

The present invention provides methods for producing FKBP-type peptidyl-prolyl cis-trans isomerase (FkpA) polypeptides at very high levels of purity. Also provided are ultrapure FkpA and methods of using same, e.g., for use in immunoassays to show removal of FkpA from biologies produced in bacteria. In addition, the present invention provides methods of purifying polypeptides (e.g., multispecific antibodies) produced in bacteria overexpressing one or more chaperones. The methods include affinity chromatography, mixed-mode chromatography and hydrophobic interaction chromatography. In some aspects, the invention provides compositions of polypeptides (e.g., multispecific antibodies) that are essentially free of product-specific impurities.