ASCLETIS-B (01672) announced that it has selected its first oral GLP-1R/GIPR/GCGR triple-target agonist peptide, ASC37 oral tablets, as a clinical development candidate. The company plans to submit an Investigational New Drug (IND) application to the U.S. Food and Drug Administration (FDA) in the second quarter of 2026 for ASC37 oral tablets as a potential treatment for obesity.
ASC37 oral tablets represent the company's first incretin candidate drug developed using its proprietary Peptide Oral Transport Enhancement Technology (POTENT). ASC37 is a triple-target agonist peptide targeting GLP-1R, GIPR, and GCGR, discovered and optimized through ASCLETIS's AI-assisted structure-based drug discovery (AISBDD) technology.
In vitro studies demonstrated that ASC37 exhibits approximately 5-fold, 4-fold, and 4-fold stronger agonistic activity on GLP-1R, GIPR, and GCGR, respectively, compared to retatrutide. In non-human primate head-to-head studies, ASC37 oral tablets achieved an average absolute oral bioavailability of 4.2% using POTENT technology—approximately 9 times, 30 times, and 60 times higher than semaglutide, tirzepatide, and retatrutide, respectively, which utilize oral SNAC formulation technology.
Additionally, in non-human primate head-to-head studies, the drug exposure (measured by area under the curve, AUC) of ASC37 oral tablets (POTENT formulation) was about 57 times higher than that of retatrutide (oral SNAC formulation) after oral administration. ASC37 oral tablets showed an average apparent half-life of approximately 56 hours in non-human primate studies, supporting once-daily or less frequent oral dosing.
"Selecting ASC37, a promising oral GLP-1R/GIPR/GCGR triple-target agonist peptide, for clinical development reaffirms our strong R&D capabilities and underscores our commitment to addressing unmet needs in obesity treatment," said Dr. Jinzi Wu, Founder, Chairman, and CEO of ASCLETIS. "Leveraging our proprietary platforms, such as AISBDD and POTENT, ASCLETIS has successfully built a highly competitive, differentiated, and diversified pipeline to effectively meet the diverse therapeutic needs of patients with obesity and other metabolic diseases."