Billions of dollars are spent each year on approved injectable peptide and small molecule drugs, with numerous additional agents in clinical development. The parenteral route of administration has generally been chosen because these agents are degraded by digestive enzymes and are then blocked by the transcellular and paracellular routes within the epithelium, resulting in sub-therapeutic bioavailability and response.
Chiasma’s proprietary Transient Permeability Enhancer (TPE®) technology platform is designed to enable the development of oral forms of medications that are currently only available as injections. TPE aims to protect drug molecules from digestive enzymes and to trigger the temporary expansion of tight junctions between cells of the intestinal epithelium, a naturally occurring process. As a result, drug molecules may pass into the blood stream while larger structures such as toxins, bacteria and viruses are excluded.
TPE’s ability to enhance oral bioavailability is the result of a combination of excipients that create a lipophilic suspension of solid hydrophilic particles in a hydrophobic medium. In all chronic toxicology and clinical trials, there have been no TPE-related safety signals or formulation-related adverse events. The adverse events that have been detected were associated with side effects of the study drug itself and the underlying disease.