Positive Results in Ovarest® Endometriosis Trial

Enteris BioPharma Announces Positive Results from Expanded Phase 2a Clinical Trial of Ovarest® (oral leuprolide tablet) for Endometriosis

Optimized tablet formulation achieved estradiol suppression in line with currently available treatments, further validating Proof-of-Concept

BOONTON, N.J., June 26, 2018 /PRNewswire/ – Enteris BioPharma, Inc., an oral dosage form biotechnology company developing innovative drug products built around its proprietary oral peptide delivery technologies, announced positive results today from the final treatment arm of the Phase 2a clinical trial of Ovarest®, an oral formulation of leuprolide, for the treatment of endometriosis.

Ovarest® leverages Enteris’ proprietary Peptelligence® technology, which the Company uses to develop innovative oral drug formulations for clients, in addition to advancing its own internal product pipeline of oral tablet reformulations of drug products that address significant treatment opportunities.

Data indicate that the optimized formulation and dose achieved estradiol suppression in line with Lupron Depot®, the current standard-of-care injectable formulation, as well as other pharmaceutical products with proven efficacy in the treatment of endometriosis. All subjects met the estradiol suppression target (estradiol ≤ 40 pg/mL) during the dosing period. Based on these positive results, Enteris plans to advance Ovarest® into the next stage of clinical development.

“The objective of the last Phase 2a treatment arm was to demonstrate that an optimized tablet formulation at a 10 mg twice daily dose would further improve estradiol suppression. We are very pleased to report that the data hit the mark, showing that Ovarest® tablets are now expected to demonstrate similar efficacy to Lupron Depot® and other products developed and being developed to treat endometriosis,” said Joel Tune, Chief Executive Officer and Executive Chairman of Enteris BioPharma. “We now intend to advance Ovarest® into a Phase 2b trial planned for later this year, which we believe is likely to establish Ovarest® as a Phase 3-ready asset. It is Enteris’ strategy to partner Ovarest® and all its internal pipeline products either at the proof of concept stage or before they enter Phase 3.”

“Women suffering from endometriosis remain underserved by the current array of treatment modalities,” said Dr. Gary Shangold, a Reproductive Endocrinologist who is a consultant to Enteris. “GnRH agonists are the most effective approved therapeutic category, and Leuprolide has been the most widely used agent in this class, yet its utility in treating this condition retains significant limitations in convenience and tolerability attributable to the depot injection delivery method. The data from this trial validate the feasibility of a leuprolide tablet to treat endometriosis. With the added flexibility of daily oral dosing and rapid reversibility, more patients will benefit from this drug.”

Interim Phase 2a data from the prior arms of the study announced earlier this year indicated that Ovarest® is able to suppress estradiol in a dose-proportional pattern. Results from the last Phase 2a cohort, comprised of 12 healthy volunteers, demonstrated that the optimized formulation of a 10 mg Ovarest® dose administered twice daily further improved estradiol suppression. Importantly, pharmacokinetic (PK) data for this Ovarest® dosing regimen indicate reliable drug delivery with leuprolide levels in the systemic circulation generally exceeding the Lupron Depot® metrics. Reliable drug delivery was demonstrated by maintaining blood level concentrations well above established threshold levels for efficacy throughout the 28-day treatment period.

About Enteris BioPharma

Enteris BioPharma, Inc. is a privately held, New Jersey-based biotechnology company offering innovative formulation solutions utilizing its proprietary oral peptide drug delivery technology, Peptelligence®. The technology has been the subject of numerous feasibility studies and active development programs, several of which are in late stage clinical development. Additionally, Enteris BioPharma is advancing an internal product pipeline of oral tablet reformulations of drug products that address significant treatment opportunities for which there is no oral delivery option.

Enteris BioPharma’s most advanced internal product candidate, Ovarest® (oral leuprolide tablet), is an oral peptide being developed initially for the treatment of endometriosis, with possible follow on indications, including uterine fibroid tumors, prostate cancer, in vitro fertilization, and central precocious puberty. Tobrate® (oral tobramycin tablet) is also being developed by Enteris BioPharma for the treatment of uncomplicated urinary tract infection (uUTI). A third internal compound, octreotide, is currently in preclinical development. For more information on Enteris BioPharma and its proprietary oral delivery technology, please visit https://www.enterisbiopharma.com.

About Endometriosis

Endometriosis is an estrogen-dependent, chronic, inflammatory disease characterized by the appearance and growth of endometrial cells or tissues in locations outside the uterus. Sources suggest endometriosis affects up to 9 million females in the United States, with the vast majority of patients remaining undertreated due to the limitations of current options. There is no cure for endometriosis, and the associated pain is currently managed with oral contraceptives, progestins, nonsteroidal anti-inflammatory drugs (NSAIDs), opioids, and GnRH agonists of which Lupron Depot® is the standard of care.