Oral Protein Delivery Breakthrough?

Receptor targeted endocytosis in GI tract PREMIUM CONTENT subscriber access

Back in 2007, I was CMO and VP Clinical Development at Emisphere Technologies, a small startup company developing carrier molecules for oral peptide/protein delivery in the GI tract. In particular, we collaborated with Novo Nordisk to successfully create a formulation for their GLP-1 agonist molecule, semaglutide, with our carrier salcaprozate sodium (SNAC). The proposed mechanism of action was by opening the paracellular water channels inserted between mucosal barrier cells and flowing through them via mass action.

https://www.mdpi.com/1999-4923/11/2/78

“Novo Nordisk and Emisphere have collaborated since 2007, on Emisphere’s proprietary drug delivery technology Eligen^®, which facilitates the enhanced oral absorption of molecules without altering their chemical form, biological integrity or pharmacological properties. Novo Nordisk is currently utilizing Emisphere’s carrier technology under an existing license agreement in its oral formulation of a GLP-1 receptor agonist semaglutide, which is marketed and sold under the brand name Rybelsus^®.” - www.globenewswire.com

RYBELSUS® (formulation R1) contains 3 mg, 7 mg or 14 mg of semaglutide and the following inactive ingredients: magnesium stearate, microcrystalline cellulose, povidone and salcaprozate sodium (SNAC)

A recent research paper reports a new method for oral delivery to the GI for large peptide/protein products, utililizing receptor-dependent uptake into intestinal mucosal cells.