ASCLETIS-B(01672): Selected oral insulin receptor agonist peptide ASC36 for clinical development.

ASCLETIS-B (01672) announced that the company's board of directors has selected its first oral peptide glucagon-like peptide-1 receptor agonist, ASC36 oral tablets, for clinical development. Goliath expects to submit an Investigational New Drug (IND) application for ASC36 oral tablets for the treatment of obesity to the United States Food and Drug Administration (FDA) in the second quarter of 2026. ASC36 oral tablets were developed by Goliath using its proprietary Oral Peptide Transport Enhancer Technology (POTENT). In non-human primates, the absolute oral bioavailability of ASC36 oral tablets was 8% after a dose of 10 mg per animal once daily for 7 days, with an elimination half-life of 116 hours; and 6% after a dose of 25 mg per animal once daily for 7 days, with an elimination half-life of 167 hours. The longer elimination half-life of ASC36 oral tablets (116 to 167 hours) supports once-daily and less frequent dosing regimens. ASC36 oral tablets showed significant weight loss effects in both non-human primates and diet-induced obese (DIO) rats. In non-human primates, after 7 days of once-daily dosing with ASC36 oral tablets, the average weight decreased by up to 13.2% relative to baseline. ASC36 tablets also significantly reduced food intake. In a head-to-head DIO rat model, after 7 days of treatment, the weight loss effect achieved by ASC36 was approximately 32% and 91% higher compared to eloralintide and petrelintide, respectively. Compared to a recently FDA-approved GLP-1R agonist peptide, ASC36 oral tablets are expected to have a lower dosing requirement due to their potential superior oral bioavailability and efficacy. The more superior weight loss effect of each milligram of ASC36 peptide may also result in lower costs in manufacturing during scale-up production. ASC36 is a glucagon-like peptide-1 receptor agonist peptide developed independently by Goliath using their Artificial Intelligence-assisted Structure-Based Drug Discovery (AISBDD) technology. The ASC36 oral tablet formulation was developed and optimized by Goliath using their proprietary POTENT technology, which is used for oral peptide delivery. "We have three key glucagon-like peptide candidates: oral small molecule glucagon, oral glucagon-like peptide peptides, and monthly subcutaneous injection glucagon-like peptides. ASC36 oral tablets are an important glucagon-like peptide agonist among them," said Dr. Wu Jingzi, founder, chairman, and CEO of Goliath. "With our three proprietary technology platforms, including AISBDD, Ultra-Long-Acting Platform (ULAP), and POTENT, Goliath has successfully built a highly competitive, differentiated, and diversified product pipeline that is poised to address the diverse treatment needs of patients with obesity and other metabolic diseases."