Our proprietary Transient Permeability Enhancer (TPE®) technology is designed to convert select peptide based injectables into oral formulations. By leveraging this technology, patients may be alleviated of the burdens associated with chronic injectable therapies.

How TPE® Works

Certain drugs can excessively degrade in the stomach, often preventing them from reaching the small intestine for absorption. Capsules containing TPE® have an enteric coating that protects peptides from degradation in the stomach. Even if able to reach the small intestine, tight junctions in the lining of the intestinal wall routinely prevent the absorption of orally delivered peptide drugs, leading to sub-therapeutic bioavailability and responses.

TPE® technology induces the expansion of seals or tight junctions made up of proteins within the lining of the small intestine. TPE® allows therapies to enter the bloodstream while maintaining the natural defense mechanism that excludes toxins, bacteria and viruses. Once in the small intestine, the coated capsule dissolves and releases the TPE® formulation.

In all chronic toxicology and clinical trials of encapsulated TPE®, there have been no TPE®-related safety signals or formulation-related adverse events 1,2. The only adverse events identified in clinical trials to date were associated with the side-effects of the study drug itself and the underlying disease.

In addition to employing TPE® to develop its first FDA-approved drug, Chiasma looks forward to identifying additional indications and potentially applying its TPE® technology to benefit patients in need of oral therapeutic options.

References

  • Melmed S, al. “Safety and Efficacy of Oral Octreotide in Acromegaly: Results of a Multicenter Phase III Trial.” The Journal of Clinical Endocrinology & Metabolism, Volume 100, Issue 4, 1 April 2015, Pages 1699–1708, https://doi.org/10.1210/jc.2014-4113
  • Tuvia S, et. Al. “A Novel Suspension Formulation Enhances Intestinal Absorption of Macromolecules Via Transient and Reversible Transport Mechanisms.” Pharmaceutical Research, Volume 31, issue 8, 21 February 2014, Pages 2010–2021, https://doi.org/10.1007/s11095-014-1303-9