Recombinant VWF Formulation Stability

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Solution Overview

Problem

Current plasma-derived VWF formulations face challenges with quantity and purity issues, as well as risks of blood-borne pathogens such as viruses and Variant Creutzfeldt-Jakob disease, necessitating the development of a stable recombinant VWF pharmaceutical composition.

Innovation Solution

A stable liquid pharmaceutical formulation of recombinant von Willebrand Factor (rVWF) is developed, comprising rVWF, a buffering agent, salts, optionally a stabilizing agent, and a surfactant, with specific concentrations and pH ranges to ensure stability and safety, using the amino acid sequence set out in SEQ ID NO: 3 and buffering agents like citrate and histidine, with salts such as calcium chloride and sodium chloride, and stabilizing agents like trehalose and mannitol.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If plasma-derived VWF formulations are used, then VWF can be obtained for therapeutic use, but there are risks of blood-borne pathogens and issues with quantity and purity

Engineering Contradiction:
Improvesafety of VWF formulationVSAvoidblood-borne pathogens
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts only the necessary VWF protein from plasma through purification processes, separating it from harmful blood-borne pathogens. This extraction principle allows obtaining therapeutic VWF while eliminating contaminants, resolving the contradiction between obtaining VWF and avoiding pathogens.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent creates a recombinant copy of VWF produced in cell cultures rather than using plasma-derived VWF. This copying approach generates identical therapeutic protein without the risks associated with human plasma, eliminating pathogen transmission while maintaining therapeutic efficacy.

Inventive Principle:
Principle #26Copying

2Quantity of substance

If plasma-derived VWF is used, then VWF therapy can be provided, but quantity and purity issues arise

Engineering Contradiction:
Improveavailability of VWFVSAvoidpurity of VWF
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The recombinant VWF production system creates unlimited copies of the VWF protein in cell cultures, overcoming the limited quantity available from plasma sources. This copying mechanism enables scalable production with consistent purity levels.

Inventive Principle:
Principle #26Copying

Solution Approach 2:

The patent employs multiple purification steps to extract and isolate VWF from complex cell culture media, achieving high purity levels. This extraction process removes contaminants while concentrating the therapeutic protein, resolving the purity challenge.

Inventive Principle:
Principle #2Taking out (Extraction)

3Stability of the object's composition

If recombinant VWF formulation is developed, then stability and safety are improved, but formulation complexity increases

Engineering Contradiction:
Improvestability of rVWF compositionVSAvoidformulation complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent optimizes formulation parameters such as pH, ionic strength, and excipient concentrations to achieve optimal stability of rVWF. By carefully adjusting these parameters, the formulation maintains protein stability without requiring overly complex composition.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces excipients as intermediary substances that mediate between the rVWF protein and the formulation environment. These excipients protect the protein from degradation while maintaining solubility and stability, simplifying the overall formulation approach.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3936116A1Rrecombinant VWF containing formulations
Publication Date: 2022.01.12 TAKEDA PHARMA CO LTD
  • EP3936116A1 patent drawingFigure 1
  • EP3936116A1 patent drawingFigure 2
  • EP3936116A1 patent drawingFigure 3

AI summary

The present invention provides long-term stable pharmaceutical formulations of recombinant von-Willebrand Factor (rVWF) and methods for making and administering said formulations.