Methods of making exenatide variants and pegylated conjugates thereof
The purification of exenatide variants and their polyethylene glycol conjugates using a three-step reversed-phase column chromatography and ion exchange chromatography solved the problem of large-scale production, achieving high-purity and high-yield preparation and improving the treatment efficacy for type II diabetes.
CN115703825BActive Publication Date: 2026-01-02PEGBIO CO LTD
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Patent Information
- Application Number
- CN202110943914.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2021-08-17
- Publication Date
- 2026-01-02
- Estimated Expiration
- 2041-08-17
AI Technical Summary
Technical Problem
Currently, there is no suitable synthesis and purification process for polyethylene glycolated exenatide or its variants for large-scale production, which affects its application in the treatment of type II diabetes.
Method used
A three-step reversed-phase column chromatography and ion exchange chromatography method was used to purify Cys39-Exendin-4 and mPEG-ppMAL-Cys39-Exendin-4, respectively. The mobile phase system and elution process were optimized, which improved the purity and yield of the target products.
Benefits of technology
This study achieved high-purity and high-yield preparation of polyethylene glycol-modified exenatide variants, meeting the needs of industrial production, prolonging the duration of drug action in vivo, and improving therapeutic efficacy.
✦ Generated by Eureka AI based on patent content.
Abstract
The present application belongs to the technical field of protein drugs, and relates to a preparation method of an exenatide variant and a polyethylene glycol conjugate thereof. Specifically, Cys 39 The preparation method of Exendin-4 adopts three-step reversed-phase column chromatography for purification, while the preparation method of mPEG-ppMAL-Cys 39 The preparation method of Exendin-4 adopts three-step reversed-phase column chromatography for purification, while the preparation method of mPEG-ppMAL-Cys 39 The preparation method of Exendin-4 adopts three-step reversed-phase column chromatography for purification, while the preparation method of mPEG-ppMAL-Cys When the polypeptide is purified, three-step reversed-phase column chromatography is used, and the acidic substance used in the second step is optimized, so that the purity and yield of the product are obviously improved. When the conjugate is purified, ion exchange chromatography and three-step reversed-phase column chromatography are used in sequence, so that the purity of the product can reach more than 99.5%, and the yield is high. The combined use of the two preparation methods can meet the needs of industrial production.
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