Entera Bio Announces Robust Pharmacokinetic Data for First-in-Class Oral GLP-2 Peptide Tablet Treatment for Patients with Short Bowel Syndrome

JERUSALEM, March 20, 2024 (GLOBE NEWSWIRE) -- Entera Bio Ltd. (NASDAQ: ENTX), (“Entera” or the “Company”) a leader in the development of orally delivered peptides, announced today positive pharmacokinetic results from its collaborative research combining a proprietary long acting GLP-2 agonist developed by OPKO Health, Inc. (Nasdaq: “OPK”, or “OPKO”) with Entera’s proprietary N-Tab technology.

The program is focused on developing the first and only GLP-2 peptide tablet alternative for patients suffering from short bowel syndrome and additional disorders involving mucosal inflammation and nutrient malabsorption. Currently, the only approved GLP-2 agonist, which is marketed under the name Gattex (teduglutide), requires daily sub-cutaneous injections. Zealand Pharma and Ironwood are developing long acting GLP-2 therapies requiring once and twice weekly injections.

Entera and OPKO completed a proof of concept (PoC) single dose pharmacokinetic study in rodents as the first validation for oral administration of the GLP-2 treatment. Oral tablets (1.8 mg; n=15) and IV injections (2 mg/kg; n=6) were administered to rats. Pharmacokinetic blood samples were taken for 24 hours post-dose and drug concentrations were analyzed by a validated LC-MS/MS method.

The study’s objectives were met with oral GLP-2 tablets exhibiting significant systemic exposure. Furthermore, plasma levels achieved with the oral tablet form of the GLP-2 analogue were about 10-fold higher than therapeutic plasma concentrations reported for subcutaneously administered teduglutide (Gattex label). The pharmacokinetic analysis of the data obtained following the IV injections of the GLP-2 peptide showed the plasma half-life in rats to be about 6 times longer than the half-life reported for teduglutide in the same animal model. This data is consistent with previously reported PK data relating to OPKO’s GLP-2 peptide’s long acting profile, which had initially been developed as a weekly subcutaneous injection.

Dose (mg)	Cmax (ng/ml)	Tmax (hr)	AUC1-24 (ng*hr/ml)
1.8	312	0.5	678

“Given the challenging compliance rates attributed to injectable GLP-2 therapy, we believe a daily tablet format may address a significant unmet need in treating SBS patients more effectively. We are pleased with this first validation for the oral GLP-2 peptide program that we initiated in late 2023 in our collaboration with OPKO. The current PK data reinforces the data we previously published combining our N-Tab technology with teduglutide in tablet form¹. Based on the promising results from the current PK study, we are planning to advance the program to assess pharmacologic effects in vivo. We look forward to updating on these data later in 2024,” said Miranda Toledano, Entera Chief Executive Officer.