Recombinant hCG Sialylation for Pharmacokinetic Profile

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Solution Overview

Problem

Current recombinant human chorionic gonadotropin (hCG) products, such as Ovitrelle, have a different pharmacokinetic profile compared to hCG produced from human urine, leading to reduced bioactivity and shorter plasma half-life due to lower sialic acid content and limited glycan heterogeneity.

Innovation Solution

Development of a recombinant hCG product that includes both α2,3 and α2,6 sialylation, resulting in mono-, di-, tri-, and tetra-sialylated structures, with a sialic acid content of 15 mol/mol or greater, more closely mimicking the natural hCG glycosylation profile.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If recombinant hCG is produced using CHO cells, then the production process is simplified and scalable, but the glycan heterogeneity is reduced and sialic acid content is lower compared to natural hCG

Engineering Contradiction:
Improveproduction process simplicityVSAvoidglycan heterogeneity
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent changes the host cell type from CHO cells to human-derived cells (such as human ovarian cells or human embryonic kidney cells), which fundamentally alters the glycosylation parameters. This cell line change enables the production of rhCG with glycan structures that more closely match natural hCG, including higher sialic acid content and greater glycan heterogeneity, while maintaining the benefits of recombinant production.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention aims to copy the natural hCG glycosylation pattern more accurately by using human-derived cell lines that possess the same glycosylation machinery as natural human cells. This allows the recombinant product to replicate the complex glycan structures, including α2,6-sialylated glycans and various antennary configurations, that are naturally present in urinary hCG.

Inventive Principle:
Principle #26Copying

2Quantity of substance

If recombinant hCG has lower sialic acid content, then the production cost is reduced, but the plasma half-life and bioactivity are shortened

Engineering Contradiction:
Improvesialic acid contentVSAvoidplasma half-life
Core Design Contradiction:
Quantity of substanceVSDuration of action of moving object

Solution Approach 1:

By changing the host cell line to human-derived cells, the patent achieves a fundamental parameter change in sialic acid content. Human cells naturally produce higher levels of sialic acid and can perform α2,6-sialylation, which is absent in CHO cells. This results in rhCG with sialic acid content and glycan composition that more closely matches natural hCG, thereby extending plasma half-life and maintaining bioactivity.

Inventive Principle:
Principle #35Parameter changes

3Manufacturing precision

If recombinant hCG is produced in CHO cells, then the product consistency is improved, but the pharmacokinetic profile differs from natural hCG

Engineering Contradiction:
Improveproduct consistencyVSAvoidpharmacokinetic profile accuracy
Core Design Contradiction:
Manufacturing precisionVSReliability

Solution Approach 1:

The patent changes the biological parameters of the production system by using human-derived cell lines instead of CHO cells. This enables the production of rhCG with pharmacokinetic properties that more accurately reflect natural hCG, including appropriate plasma half-life and bioactivity, while the controlled recombinant production process maintains product consistency and batch-to-batch uniformity.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3611185B1Pharmaceutical preparation
Publication Date: 2025.04.30 FERRING BV
  • EP3611185B1 patent drawingFigure 1
  • EP3611185B1 patent drawingFigure 2~3
  • EP3611185B1 patent drawingFigure 4

AI summary

Preparations including recombinant hCG (r hCG).