Development of Rybelsus<sup>Ⓡ</sup>, the world’s first oral GLP-1 receptor agonist

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  • Moriwaki Norichika
    Novo Nordisk Pharma Ltd., Clinical, Medical, Regulatory （CMR） Development Division, Project Planning & Management Dept
  • Akahori Mitsuru
    Novo Nordisk Pharma Ltd., Clinical, Medical, Regulatory （CMR） Development Division, Project Planning & Management Dept
  • Sugii Hiroshi
    Novo Nordisk Pharma Ltd., CMR Development Division

Bibliographic Information

Other Title
  • 世界初の経口GLP-1受容体作動薬リベルサス<sup>Ⓡ</sup>の開発

Description

Oral semaglutide tablets（RybelsusⓇ） is the world’s first once-daily oral formulation for glucagon like peptide-1（GLP-1） receptor agonist approved with the indication of type 2 diabetes mellitus in June 2020 in Japan. Oral semaglutide is co-formulated with the absorption enhancer salcaprozate sodium （SNAC） which enable to the oral absorption of semaglutide with high molecular weight peptide. This drug can be expected to improve adherence in the treatment by anti-diabetic drugs, as it is considered lower risk of hypoglycemia due to the glucose-dependent blood sugar lowering effect. This article describes the oral absorption enhancement mechanism of semaglutide by SNAC, pharmacokinetics and clinical trial results of oral semaglutide.

Journal

  • Drug Delivery System

    Drug Delivery System 37 (2), 169-173, 2022-03-25

    THE JAPAN SOCIETY OF DRUG DELIVERY SYSTEM

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