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Abstract
A 14 amino acid cystin bridge containing neuropeptide was discovered in 1973 and designated as growth hormone-inhibiting hormone, in other words, somatostatin. Its discovery led to the synthesis of three analogs which were licensed for the treatment of acromegaly: octreotide, lanreotide and pasireotide. Somatostatin analogs are currently approved only as either subcutaneous or intramuscular long-acting injections. We examine the challenges that must be overcome to create oral formulations of somatostatin analogs and examine selected clinical trial data. While octreotide has low intestinal permeability, similar to almost all other peptides, it has an advantage of being more stable against intestinal peptidases. The development of new oral formulation strategies may eventually allow for the successful oral administration of potent somatostatin analogs with high therapeutic indices.
Financial & competing interests disclosure
D Brayden consulted for Chiasma Pharmaceuticals in 2014 and 2015. This project has received funding from the European Union's Horizon 2020 research and innovation programme under the Marie Skłodowska-Curie Grant agreement No 666010 and Science Foundation Ireland (SFI) Grant 13/RC/2073, the CÚRAM Centre for Medical Devices. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.