ASCLETIS-B(01672): Clinical development of a fixed-dose combination formulation of ASC30, a once-daily oral small molecule GLP-1R agonist, and ASC39, a once-daily oral small molecule selective insulin receptor agonist.

ASCLETIS-B (01672) announced that the board of directors has selected ASC30_39 FDC, a fixed-dose combination formulation of ASC30, a once-daily oral small molecule GLP-1R agonist, and ASC39, a once-daily oral small molecule selective amylin receptor agonist, for clinical development. Geli is expected to submit an Investigational New Drug Application (IND) for ASC30_39 FDC oral tablets for the treatment of obesity to the U.S. Food and Drug Administration (FDA) in the third quarter of 2026. After oral administration in dogs, ASC30_39 FDC tablets showed superior oral bioavailability, drug exposure, and a half-life of up to 12 hours. In a head-to-head dog study, the key parameters of ASC30_39 FDC tablets were consistent with those observed for ASC30 and ASC39 in their respective monotherapy. Additionally, ASC30_39 FDC tablets developed using Geli's proprietary formulation technology demonstrated good compatibility between ASC30 and ASC39, as well as room temperature stability and the characteristic of small tablet size. ASC30_39 FDC has superior pharmacokinetic characteristics, with ASC30 expected to have best-in-class efficacy and gastrointestinal tolerability, and ASC39 being the first small molecule amylin similar to eloralintide, these advantages support the potential for ASC30_39 FDC tablets to become a once-daily new therapy for obesity. ASC30 is a small molecule oral GLP-1R agonist that is ready to enter Phase III clinical trials, with good gastrointestinal tolerability. In non-head-to-head studies, the vomiting rate of weekly titrated ASC30 is only half of orforglipron's weekly titrated vomiting rate (as announced on December 8, 2025). ASC39 is a potent oral small molecule selective amylin receptor agonist, showing amylin selectivity and efficacy similar to eloralintide in preclinical models, and has been selected as a clinical development candidate. "To our knowledge, this is the first publicly announced oral GLP-1 combined with oral amylin fixed-dose combination formulation. Choosing this fixed-dose combination formulation is an important step in developing a novel potential oral combination therapy for obesity with ASC30 and ASC39," said Dr. Jinzi Wu, founder, chairman of the board, and CEO of Geli. "We believe that this fixed-dose combination formulation combines key features such as high bioavailability, high drug exposure, long half-life, and the convenience of small tablets, which may improve the treatment outcomes for patients with obesity."