Oral Semaglutide: Realising the Potential of Oral Peptide Delivery

3/12/2019 14:00 - 14:35

  • Peptides such as insulin and glucagon-like peptide-1 (GLP-1) receptor agonists are used in the treatment of type 2 diabetes.
  • The inherent physicochemical properties of these peptides (high molecular weight, enzymatically labile, hydrophilicity, and low permeability) have hampered attempts to deliver peptides via the oral route and necessitated that they be administered by injection.
  • Recently, oral semaglutide, a GLP-1 analog, coformulated with the absorption enhancer sodium N-[8-(2-hydroxybenzoyl) aminocaprylate] (SNAC) in a tablet has been developed.
  • This coformulation provides unique, site-directed release and absorption in the stomach and effectively surmounts inherent challenges relating to solubility, molecular size, and proteolytic lability to achieve therapeutically relevant plasma exposure of semaglutide.