Ascletis selects ASC37, first oral GLP-1R/GIPR/GCGR triple peptide agonist for clinical development

Ascletis has selected ASC37 oral tablets, its first oral GLP-1R/GIPR/GCGR[1] triple peptide agonist, as a clinical development candidate. Ascletis expects to submit an Investigational New Drug Application (IND) to the FDA for ASC37 oral tablets for the treatment of obesity in the second quarter of 2026.

ASC37 oral tablets is the company's first incretin drug candidate developed with its proprietary Peptide Oral Transport ENhancement Technology (POTENT). ASC37, a GLP-1R, GIPR, and GCGR triple peptide agonist, was discovered and optimized in-house utilizing Ascletis' Artificial Intelligence-Assisted Structure-Based Drug Discovery (AISBDD). ASC37 in vitro activity was approximately 5-, 4-, and 4-fold more potent than retatrutide for GLP-1R, GIPR and GCGR, respectively.

Utilising Ascletis' POTENT technology, ASC37 oral tablets achieved average absolute oral bioavailability of 4.2%, which was approximately 9-, 30-, and 60-fold higher than semaglutide, tirzepatide, and retatrutide in the oral SNAC [3] formulation, respectively, in head-to-head non-human primate (NHP) studies. Furthermore, after oral administration, ASC37 oral tablets' drug exposure, as measured by the area under curve (AUC), with the POTENT formulation was approximately 57-fold of retatrutide's drug exposure with the oral SNAC formulation, in head-to-head NHP studies.

Average observed half-life of ASC37 oral tablets was approximately 56 hours in NHP studies, supporting once daily and less frequent oral dosing.

 "Selection of ASC37, a promising oral GLP-1R/GIPR/GCGR triple peptide agonist, for clinical development once again demonstrates our strong R&D capabilities and our commitment to address the unmet needs for the treatment of obesity," said Dr Jinzi Jason Wu, Founder, Chairman and CEO of Ascletis, "Leveraging our proprietary technology platforms, including AISBDD and POTENT, Ascletis has successfully established a highly competitive, differentiated and diverse pipeline portfolio which can potentially effectively address the various treatment needs of patients with obesity and other metabolic diseases."