Enteris BioPharma, a 24-person biotech based in Boonton, N.J., last month launched a trial of its oral leuprolide endometriosis therapy, Ovarest.
Ovarest is the company’s most advanced internal candidate and represents Enteris’ attempt to overcome the challenges presented by the oral delivery of peptides, according to CEO Joel Tune.
The Phase IIa trial, which is slated to enroll 32 healthy female volunteers, will compare Enteris’ oral formulation of leuprolide to a monthly intramuscular injection.
Tune told Drug Delivery Business News that Enteris is hoping the trial will reaffirm pharmacokinetic data that it collected in a Phase I trial. But the company is also hoping that over a 30-day period, the treatment can effectively suppress estradiol – one way to provide relief to patients with endometriosis.
Although the intramuscular depot injection is the approved method of treatment for endometriosis, Tune believes an orally-delivered therapy could prove beneficial to patients.
“[The standard therapy] is a long-term injection. And once it’s in the patient’s body, they can’t get it back out if they start having side-effects,” he said. “By switching to the oral route, market research suggests patients will be more willing to take it. And physicians will be much more confident and comfortable prescribing it.”
The company’s ‘Peptellingence’ platform is designed to overcome the challenges of oral peptide delivery. A person’s gastrointestinal tract degrades and digests peptides, Tune said, and a normal peptide can’t break through the intestinal cell layer to be absorbed.
Enteris tackled this problem by developing a coating that stops the peptide from opening in the stomach and instead triggers the therapy to dissolve once it reaches the person’s small intestine.
The company also uses a compound to boost the intestinal cell layer’s permeability, temporarily widening the gaps between cells to facilitate drug transfer, Tune said.
Enteris’ platform focuses on the oral delivery of peptides, but the company is also working on a way to deliver small molecules orally.
“I think there’s real value for the patient in oral formulations,” Tune said. “They’re the ultimate beneficiary here.”
Tune, who previously spent 28 years at Baxter Healthcare, pointed towards research showing that patients are generally more compliant if their prescribed treatment involves an oral medication compared to an injection.
“We also found that we are able to expand indications,” Tune added. The company’s Tobrate product is an oral formulation of tobramycin designed to treat uncomplicated urinary tract infections – a new potential application for the antibiotic.
The company, which has an array of programs in preclinical development, also partners with bigger players in the pharmaceutical industry. This year, Enteris announced that it inked a number of deals, including a partnership with Sanofi to develop an oral peptide for Type II diabetes.
“There’s a lot of value to be created there both for our partners and for us,” Tune said. “But also, that’s really the way we fund our continued development.”
In the year ahead, Tune said the company hopes to move two or three partnered compounds into the clinic. Enteris is also expecting results from its Phase IIa endometriosis trial by the end of 2017.
The company’s oral formulation of leuprolide could also be used to treat uterine fibroids, Tune said, so Enteris is considering whether the company should pursue that indication simultaneously or pour all of their focus into endometriosis.
“Six million women in the U.S. have been diagnosed with endometriosis, so it would help them immensely,” he said. “We’re just very excited about being able to potentially help that many patients.”