Entera Bio Ltd. announced positive pharmacokinetic results from its collaborative research combining a proprietary long acting GLP-2 agonist developed by OPKO Health, Inc. 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.