Chinese biotechnology company Ascletis Pharma Inc (HKEX:1672) announced on Sunday that it has selected ASC37 oral tablets, its first oral GLP-1R/GIPR/GCGR triple peptide agonist, as a clinical development candidate.
The company expects to submit an Investigational New Drug Application (IND) to the US Food and Drug Administration (FDA) for ASC37 oral tablets for the treatment of obesity in the second quarter of 2026.
The product is the company's first incretin drug candidate developed with its proprietary Peptide Oral Transport ENhancement Technology (POTENT). It is a GLP-1R, GIPR, and GCGR triple peptide agonist that was discovered and optimised in-house using Ascletis' Artificial Intelligence-Assisted Structure-Based Drug Discovery (AISBDD).
According to Ascletis, ASC37 in vitro activity was approximately 5-, 4-, and 4-fold more potent than retatrutide for GLP-1R, GIPR and GCGR, respectively. Using 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 formulation, respectively, in head-to-head non-human primate (NHP) studies. 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.
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