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口服司美格鲁肽综述:以丸剂形式用肽类药物治疗糖尿病的新时代的现有证据

A Review of Oral Semaglutide Available Evidence: A New Era of Management of Diabetes with Peptide in a Pill Form.

作者信息

Kalra Sanjay, Das Sambit, Zargar Abdul H

机构信息

Department of Endocrinology, Bharti Hospital, Karnal, Haryana, India.

Senior Consultant Endocrinologist Apollo Hospitals, Bhubaneshwar, Odisha, India.

出版信息

Indian J Endocrinol Metab. 2022 Mar-Apr;26(2):98-105. doi: 10.4103/ijem.ijem_522_21. Epub 2022 Jun 6.

DOI:10.4103/ijem.ijem_522_21
PMID:35873937
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9302409/
Abstract

Glucagon-like peptide 1 receptor agonists (GLP-1RAs) have gained an important place in the management of diabetes management because of their exceptional glucose-lowering, weight lowering and cardiovascular (CV) benefits. Despite recommendations by various clinical practice guidelines and benefits, their usage in clinical practice was limited because of being injectable in nature. Oral semaglutide is a novel GLP-1RA with 94% homology to human GLP-1 which is co-formulated with absorption enhancer sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC), that overcomes the challenges of peptide absorption in the acidic conditions of the stomach. Oral semaglutide has been evaluated in an extensive phase 3 clinical trial programme named Peptide Innovation for Early Diabetes Treatment (PIONEER) which demonstrated its robust glucose and weight lowering effects against other comparators. The evolution of the GLP-1RA class to include an oral pill will facilitate the use of this class of agents much earlier in the diabetes treatment cascade owing to wider acceptance from patients and clinicians alike. The current review discusses the various aspects of oral semaglutide and its place in clinical practice.

摘要

胰高血糖素样肽-1受体激动剂(GLP-1RAs)因其卓越的降糖、减重及心血管(CV)益处,在糖尿病管理中占据了重要地位。尽管各类临床实践指南给出了推荐且具有诸多益处,但因其为注射制剂,在临床实践中的使用受到限制。口服司美格鲁肽是一种新型GLP-1RA,与人类GLP-1具有94%的同源性,它与吸收增强剂N-(8-[2-羟基苯甲酰基]氨基)辛酸钠(SNAC)共同配制,克服了在胃酸性环境中肽吸收的难题。口服司美格鲁肽已在一项名为“早期糖尿病治疗肽创新(PIONEER)”的广泛3期临床试验项目中进行了评估,该试验证明其相对于其他对照药物具有强大的降糖和减重效果。GLP-1RA类别发展到包含口服片剂,将因患者和临床医生更广泛的接受度,在糖尿病治疗流程中更早地促进这类药物的使用。本综述讨论了口服司美格鲁肽的各个方面及其在临床实践中的地位。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/f4a2bc8a577d/IJEM-26-98-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/e3e916c27156/IJEM-26-98-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/546b702fd0a0/IJEM-26-98-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/5d9de3d90c93/IJEM-26-98-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/afc494c83f21/IJEM-26-98-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/f4a2bc8a577d/IJEM-26-98-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/e3e916c27156/IJEM-26-98-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/546b702fd0a0/IJEM-26-98-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/5d9de3d90c93/IJEM-26-98-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/afc494c83f21/IJEM-26-98-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/73b7/9302409/f4a2bc8a577d/IJEM-26-98-g005.jpg

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Diabetes Ther. 2021 Aug;12(8):2133-2147. doi: 10.1007/s13300-021-01113-y. Epub 2021 Jul 15.
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