According to the Zhitong Finance App, Goli Pharmaceutical-B (01672) announced that it has selected ASC48, the GIPR agonist, which is expected to be the first of its kind (first-in-class) oral small molecule, and a fixed-dose compound formulation of the oral small molecule GLP-1R agonist ASC30 for clinical development. The ASC30 and ASC48 fixed-dose compound formulation (ASC30_48 FDC) targets both GLP-1R and GIPR, and is expected to be the first “one-pill, once-daily)” oral obesity treatment of its kind.
ASC48 was independently developed using Golie's structure-based AISBDD (AISBDD) technology. In head-to-head human GIPR (hGIPR) cAMP activation experiments, the EC50 of ASC48 was 1 pM, showing stronger excitatory activity than telpotide (EC50 = 3 pM), and is a selective agonist of GIPR, with no agonist activity against GLP-1R and GCGR. In gnats and non-human primates, ASC48 showed excellent oral bioavailability, drug exposure, and long half-life, supporting oral administration once a day in humans.
In head-to-head non-human primate studies, the weight loss effect of ASC30_48 FDC was about 52% higher than that of ASC30 alone.
When ASC30_48 FDC is taken orally once a day for eight consecutive days, the weight loss effect was 52% and 518% higher than that of ASC30 and ASC48 alone, respectively.
A new drug clinical trial application (IND) for ASC30_48 FDC oral tablets is expected to be submitted to the US Food and Drug Administration (FDA) in the fourth quarter of 2026.
“We look forward to conducting this clinical trial to evaluate the fixed-dose combination of ASC48 and ASC30, with the aim of developing first-in-class (first-in-class) oral therapy, which is expected to improve treatment outcomes for patients with obesity.” Dr. Wu Jinzi, founder, chairman of the board of directors and CEO of Goli, said, “We believe that there is still an unmet medical need, that is, an oral medication that, when combined with GLP-1R therapy, can achieve the same weight loss effect and tolerability as a weekly dose of tirpotide.”