Protein Engineering and Biopharmaceuticals Science, Hubei University of Technology, Wuhan 430068, China; Hubei Key Laboratory of Diabetes and Angiopathy, National Demonstration Center for Experimental General Medicine Education, Xianning Medical College, Hubei University of Science and Technology, Xianning, Hubei 437100, China.
Protein Engineering and Biopharmaceuticals Science, Hubei University of Technology, Wuhan 430068, China; School of Pharmaceutical Sciences and Institute of Materia Medica, Xinjiang University, Urumqi 830017, China.
Biochem Pharmacol. 2024 Nov;229:116471. doi: 10.1016/j.bcp.2024.116471. Epub 2024 Aug 8.
Peptide glucagon-like peptide-1 receptor agonists (GLP-1RAs) are effective drugs for treating type 2 diabetes (T2DM) and have been proven to benefit the heart and kidney. Apart from oral semaglutide, which does not require injection, other peptide GLP-1RAs need to be subcutaneously administered. However, oral semaglutide also faces significant challenges, such as low bioavailability and frequent gastrointestinal discomfort. Thus, it is imperative that advanced oral strategies for peptide GLP-1RAs need to be explored. This review mainly compares the current advantages and disadvantages of various oral delivery strategies for peptide GLP-1RAs in the developmental stage and discusses the latest research progress of peptide GLP-1RAs, providing a useful guide for the development of new oral peptide GLP-1RA drugs.
肽类胰高血糖素样肽-1 受体激动剂（GLP-1RAs）是治疗 2 型糖尿病（T2DM）的有效药物，已被证明对心脏和肾脏有益。除了不需要注射的口服司美格鲁肽外，其他肽类 GLP-1RAs 需要皮下给药。然而，口服司美格鲁肽也面临着生物利用度低和经常出现胃肠道不适等重大挑战。因此，必须探索肽类 GLP-1RAs 的先进口服策略。本综述主要比较了处于研发阶段的各种肽类 GLP-1RA 口服递送策略的当前优缺点，并讨论了肽类 GLP-1RA 的最新研究进展，为新型口服肽类 GLP-1RA 药物的开发提供了有益的指导。
