Nihon yakurigaku zasshi. Folia pharmacologica JaponicaMar 1, 2022

Introducing oral Semaglutide (Rybelsus®), a new pill for type 2 diabetes that works like natural blood sugar hormones

GLP-1 Therapies Weekly Brief ↗PubMed ↗DOI ↗

Updated Mar 31, 2026

Abstract

Semaglutide, a GLP-1 receptor agonist, is used globally as a once-weekly treatment for type 2 diabetes at a dose of 2 mg.

GLP-1 promotes insulin secretion in response to glucose levels and has a hypoglycemic effect.
Endogenous GLP-1 is quickly degraded by DPP-4, necessitating the use of a longer-lasting analog like semaglutide.
Semaglutide has 94% similarity to human GLP-1 and binds to GLP-1 receptors in pancreatic β-cells.
It has a prolonged half-life due to its high affinity for albumin and specific amino acid modifications.
Oral semaglutide (Rybelsus) is the first GLP-1 receptor agonist approved for oral use and has shown continuous benefits across various stages of type 2 diabetes.
Clinical trials indicate that oral semaglutide may help patients achieve earlier improvements in glycemic control.

Simplified

GLP-1 (glucagon-like peptide-1) is one of the incretin hormone secreted from L cells in the small intestine and it is known to promote insulin secretion in a glucose concentration-dependent manner and have a hypoglycemic effect. However, since endogenous GLP-1 is rapidly degraded by ubiquitously expressing DPP-4, a GLP-1 receptor agonist with a longer half-life has been required. Semaglutide is a GLP-1 analog that has 94% homology with human GLP-1 and it binds to the GLP-1 receptor in pancreatic β-cells to induce the insulin secretion in a glucose concentration-dependent manner. Semaglutide has a high affinity for the fatty acid binding site of albumin and has an extended half-life by being protected from degradation by DPP-4, due to specific modification of its amino acid sequence. A once weekly semaglutide (OzempicSubcutaneous Injection 2 mg) is used worldwide as a treatment for type 2 diabetes when diet and exercise therapy are inadequate. In Japan, it was approved for manufacturing and marketing in March 2018. Oral semaglutide (Rybelsus) has been co-formulated with the absorption enhancer sodium N-(8-[2-hydroxybenzoyl]amino) caprylate (SNAC), and is the first GLP-1 receptor agonist (GLP-1RA) to be approved for oral administration. Rybelsushave been shown to be of continuous benefit in patients with type 2 diabetes at various stages by monotherapy and combination therapy with 3, 7 and 14 mg Rybelsus in eight global clinical trials and two Japanese trials. It was suggested that oral semaglutide make patients with chronic and progressive type 2 diabetes may be able to achieve the earlier improvement in glycemic control as global diabetes association recommended. ® ® ®

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Introducing oral Semaglutide (Rybelsus®), a new pill for type 2 diabetes that works like natural blood sugar hormones

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