OPK-8801003

Preclinical Data for OPK-8801003 Demonstrate Substantially Longer Biological Half-Life with Peak Plasma Levels Comparable to Gattex®, the Only Approved GLP-2 Therapy Oral GLP-2 Tablet Could Transform Treatment Paradigm for 30,000 Short Bowel Syndrome (SBS) Patients Currently Dependent on Daily Injections of the Peptide Sept. 15, 2025 -- Entera Bio Ltd. (NASDAQ: ENTX), a leader in the development of oral peptides and protein replacement therapies, today announced the presentation of a poster titled "A First-in-Class Oral GLP-2 Analog for Treatment of Short Bowel Syndrome” at the 47th European Society for Clinical Nutrition & Metabolism (ESPEN) Congress in Prague, Czech Republic, highlighting pharmacokinetic (PK) data relating to its oral GLP-2 analog program. Entera and OPKO Health, Inc. entered into a research collaboration in 2023 to develop oral peptide candidates for intestinal malabsorption syndromes, combining OPKO's proprietary long-acting GLP-2 analog (OPK-8801003) with Entera's N-Tab™ oral peptide platform. Currently, the only approved GLP-2 therapy is Gattex® (teduglutide), which generates approximately $800 million in annual sales despite requiring daily subcutaneous injections with challenging compliance rates and limited patient access. "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," said Miranda Toledano, Chief Executive Officer of Entera. "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, offering a less-invasive administration that can be titrated to enable personalized dosing in this rare and heterogeneous condition." Extended Half-Life: OPK-8801003 GLP-2 tablet demonstrated a plasma half-life of approximately 15 hours in minipigs, representing an approximate 18-fold improvement over teduglutide, which has a half-life of only 0.85 hours in the same species. Robust Oral Bioavailability: Following oral administration of OPK-8801003 tablets in minipigs, peak plasma concentrations reached ~200 ng/ml (Cmax), substantially exceeding the reported Cmax of 36.8 ng/ml for daily 0.05 mg/kg teduglutide subcutaneous injection in humans. Sustained Exposure: Systemic exposure (AUC ~2 h*μg/ml) was maintained for more than 24 hours with relatively low variability, supporting once-daily oral dosing. Favorable Safety Profile: No signs of toxicity were observed in the preclinical studies. Short bowel syndrome is a rare and potentially life-threatening malabsorptive condition caused by a significant loss of functional bowel mass (secondary to congenital defects or disease-associated loss of absorption) or physical bowel mass (secondary to extensive intestinal resection). Approximately 30,000 patients across the U.S. and EU are living with SBS, and current annual sales of GATTEX® (teduglutide), the only approved therapy for SBS, total roughly $800 million. SBS patients have a reduced ability to absorb nutrients and fluids and are at risk of malnutrition, unintended weight loss and additional symptoms due to the loss of essential vitamins and minerals.1 SBS is the most common cause of chronic intestinal failure, accounting for approximately 75% of chronic intestinal failure cases in adults and 50% of such events in children.1 Entera is a clinical stage company focused on developing oral peptide and protein replacement therapies for significant unmet medical needs where an oral tablet form holds the potential to transform the standard of care. The Company leverages on a disruptive and proprietary technology platform (N-Tab™) and its pipeline of first-in-class oral peptide programs targeting PTH(1-34), GLP-1 and GLP-2. The Company’s most advanced product candidate, EB613 (oral PTH(1-34), teriparatide), is being developed as the first oral, osteoanabolic (bone building) once-daily tablet treatment for post-menopausal women with low BMD and high-risk osteoporosis. A placebo-controlled, dose-ranging Phase 2 study of EB613 tablets (n= 161) met primary (PD/bone turnover biomarker) and secondary endpoints (BMD). The EB612 program is being developed as the first oral PTH(1-34) tablet peptide replacement therapy for hypoparathyroidism. Entera is also developing the first oral oxyntomodulin, a dual targeted GLP1/glucagon peptide, in tablet form for the treatment of obesity and metabolic syndromes; and first oral GLP-2 peptide as an injection-free alternative for patients suffering from rare malabsorption conditions such as short bowel syndrome in collaboration with OPKO Health. 1 Zhu C, Li Y. An updated overview of glucagon-like peptide-2 analog trophic therapy for short bowel syndrome in adults. J Int Med Res. 2022 Mar;50(3):3000605221086145. doi: 10.1177/03000605221086145. PMID: 35343263; PMCID: PMC8966062. The content above comes from the network. if any infringement, please contact us to modify.