Entera Bio's oral GLP-2 analog shows longer half-life, comparable peak levels to Gattex.

Entera Bio has presented preclinical data for OPK-8801003, an oral GLP-2 analog, demonstrating a substantially longer biological half-life and peak plasma levels comparable to Gattex, the only approved GLP-2 therapy. This oral tablet has the potential to transform the treatment paradigm for the 30,000 patients with short bowel syndrome currently dependent on daily injections of the peptide. The data was presented at the ESPEN Congress in Prague.

Entera Bio (NASDAQ: ENTX) has made significant strides in the development of oral peptide therapies, presenting compelling preclinical data for OPK-8801003, an oral GLP-2 analogue, at the 2025 ESPEN Congress in Prague. The data showcases a substantially longer biological half-life and peak plasma levels comparable to Gattex, the current standard of care for Short Bowel Syndrome (SBS) patients.

The oral GLP-2 tablet, OPK-8801003, demonstrated a 15-hour plasma half-life, nearly 18 times longer than the injectable Gattex, which has a half-life of approximately 0.85 hours. This extended half-life could significantly improve patient compliance and reduce the frequency of injections, a critical aspect for patients with chronic conditions like SBS. The tablet also achieved peak plasma concentrations of ~200 ng/ml, which is comparable to the 36.8 ng/ml reported for subcutaneous injections of Gattex in humans. This suggests that the oral formulation may offer superior bioavailability through Entera's N-Tab™ delivery platform.

The sustained exposure profile of OPK-8801003, with an AUC of ~2 h*μg/ml maintained for over 24 hours, supports once-daily oral dosing, a significant advancement over the current daily injection regimen. The absence of toxicity signals in preclinical studies further strengthens the developmental potential of this oral GLP-2 therapy.

If these preclinical results translate to humans, OPK-8801003 could fundamentally transform care for the 30,000 SBS patients currently dependent on daily injections. The ability to titrate dosing through a tablet formulation opens possibilities for personalized treatment approaches, potentially improving both efficacy and compliance compared to fixed-dose injections.

Entera Bio's collaboration with OPKO Health has been instrumental in developing this oral peptide candidate. The partnership combines OPKO's proprietary long-acting GLP-2 analogue with Entera's N-Tab™ oral peptide platform, aiming to revolutionize the treatment of SBS.

The success of OPK-8801003 could have a profound impact on the $800 million annual market for SBS treatments, which is currently dominated by Gattex. The potential to offer a less-invasive administration method with comparable efficacy could significantly improve patient quality of life and reduce healthcare costs.

Entera Bio's Chief Executive Officer, Miranda Toledano, stated, "The pharmacokinetic data presented at ESPEN represent a significant milestone in our journey to develop the first oral GLP-2 therapy and an incremental milestone in validating our N-Tab™ oral peptide platform. Given the robust oral bioavailability demonstrated in our preclinical studies, we believe this daily GLP-2 tablet candidate could fundamentally change how SBS patients are treated."

This development marks a meaningful step toward addressing significant unmet needs in the rare disease population of SBS patients.