Long-acting glucagon-like peptide-2 analogs, methods of making and uses

By modifying the structure of GLP-2 analogs and preparing them using solid-phase synthesis, the problem of the short half-life of natural GLP-2 has been solved, resulting in a longer half-life and higher bioactivity, which is suitable for the treatment of gastrointestinal diseases and has good clinical application potential.

CN122404529APending Publication Date: 2026-07-17SUZHOU QINGRUI BIOTECHNOLOGY CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUZHOU QINGRUI BIOTECHNOLOGY CO LTD
Filing Date
2026-01-16
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

The short half-life of natural GLP-2 necessitates frequent injections, affecting patient compliance. Existing analogues such as Teduglutide and Apraglutide have short half-lives and low in vitro potency, requiring high doses.

Method used

A GLP-2 analogue was designed to increase stability and half-life through structural modification. It was prepared by solid-phase synthesis, and specific substituents were introduced to prolong the half-life and retain biological activity. The specific structure is HGDGSFSDE(NIe)(D-Phe)TILDLX17AARDFIX24WLIQTKITD-XX1-R1. The selection of XX1 and R1 was optimized to improve chemical stability.

Benefits of technology

GLP-2 analogues exhibit longer half-lives and higher biological activity in vivo, significantly superior to apraglutide, and have promising clinical application prospects for the prevention and treatment of gastrointestinal diseases.

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Abstract

本发明属于医药领域,具体涉及一种胰高血糖素样肽‑2(GLP‑2)类似物、制备方法和在预防和治疗例如胃肠相关病症以及减轻化学疗法和放射性疗法的副作用中的用途。本发明针对目前现有技术存在的天然的GLP‑2半衰期短、不具有临床药物价值这一技术问题,提供一类GLP‑2类似物,与野生GLP‑2相比,所述GLP‑2类似物具有更稳定的化学特性,更长的半衰期,同时仍然保留具有类似于GLP‑2的生物活性,且所述GLP‑2类似物的效果显著优于Apraglutide,具有良好的临床应用前景。
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