New drug for type 2 diabetes: introduction of oral Semaglutide (Rybelsus<sup>®</sup> tablets), an oral GLP-1 receptor agonist
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- Miyasaka Kota
- CMR Development Division, Medical Affairs Department, Novo Nordisk Pharma Ltd.
Bibliographic Information
- Other Title
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- 2型糖尿病治療剤 経口GLP-1受容体作動薬：経口セマグルチド（リベルサス<sup>®</sup>錠）の薬理学的特性と臨床試験成績
Abstract
<p>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 (Ozempic® Subcutaneous 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. Rybelsus® have 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.</p>
Journal
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- Folia Pharmacologica Japonica
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Folia Pharmacologica Japonica 157 (2), 146-154, 2022
The Japanese Pharmacological Society
