Benzinga | Oct 28, 2021 08:45AM EDT

Entera Bio Publishes Key Study Describing Its Oral Delivery Technology Platform For Biologic Drugs

Entera Bio Ltd. (NASDAQ:ENTX), today announced that researchers at the company and the University of East Anglia in the UK published preclinical in vivo studies which demonstrate the technologies efficiency in the oral delivery of large molecule biologic drugs. The approach described in the research underpins Entera's lead product, EB613, an oral parathyroid hormone (hPTH) entering Phase 3 clinical development for the treatment of osteoporosis. The pivotal Phase 3 study is planned for 2022.

The studies were published on line in the peer-reviewed International Journal of Pharmaceutics X.

"Entera's highly innovative technology has the potential to transform the way we treat many diseases," stated William Fraser, MD, Professor of Medicine at The Norfolk and Norwich University Hospitals and Norwich Medical School at the University of East Anglia. "Not only can replacing injections improve patient compliance and reduce patient discomfort, but the administration of oral PTH in both hypoparathyroidism and osteoporosis will allow for the customized titration of dose so critical to each individual patient. At present, most injections are administered via "pen" injectors, which are frequently not amenable to dose titration."

"Entera's innovation is to combine in a single formulation two approaches to enhancing the delivery of large molecule biologics," said Spiros Jamas, the company's CEO. "This research supports our strategy to address the two key challenges in delivering hPTH to the bloodstream at appropriate therapeutic levels consistently: protecting proteins from breaking down in the gastrointestinal tract; and 2) improving absorption of proteins through the gastro-intestinal tract."

"With a burgeoning number of injectable biologics on the market and in development, there is a growing need for effective oral formulations especially in chronic conditions where replacing injections with oral dosage may result in higher patient compliance, adherence, and quality of life," stated Entera CEO Spiros Jamas. "Beyond the near-term opportunity for our EB613 oral PTH in osteoporosis, Entera's platform technology has applications in many other indications currently treated through injectables."

In this paper researchers evaluated three different formulations of oral hPTH (1-34): 1. hPTH with a protease inhibitor which can protect the molecule in the gastrointestinal tract, and 2. hPTH with just a permeation enhancer (SNAC) which allows for the trans-cellular absorption of large molecules in the GI tract, and 3. hPTH combined with both protease inhibitor and permeation enhancer (the formulation technology currently utilized by Entera). In studies utilizing a porcine model, the Entera combined formulation achieved significantly higher PTH blood levels (Cmax and AUC, ~10- and ~20-fold respectively) as compared to each of these approaches on their own. The researchers concluded that an appropriate combination of these different technological approaches considerably contributes to the efficient oral delivery of a number of biological macromolecules.

The study is titled, "The combined effect of permeation enhancement and proteolysis inhibition on the systemic exposure of orally administrated peptides: Salcaprozate sodium, soybean trypsin inhibitor, and teriparatide study in pigs." The authors on the paper are, Gregory Burshtein, Constantin Itin, Hillel Galitzer and Phillip Schwartz, from Entera Bio, Jonathan C. W. Tang, of the University of East Anglia (Norwich, UK) William D. Fraser, of the University of East Anglia and Norfolk and Norwich University Hospital (Norwich, UK).