ASCLETIS-B (01672) has announced the selection of ASC30_39 FDC, a fixed-dose combination of once-daily oral small molecule GLP-1 receptor agonist ASC30 and once-daily oral small molecule amylin-selective amylin receptor agonist ASC39, for clinical development. The company expects to submit an Investigational New Drug application to the U.S. Food and Drug Administration in the third quarter of 2026 for ASC30_39 FDC oral tablets targeting obesity.
In canine studies, ASC30_39 FDC tablets demonstrated superior oral bioavailability, drug exposure, and a half-life of up to 12 hours. A head-to-head study in dogs showed that key pharmacokinetic parameters of ASC30_39 FDC aligned with those observed for ASC30 and ASC39 in their respective monotherapies.
Additionally, ASC30_39 FDC tablets developed using ASCLETIS’ proprietary formulation technology exhibited excellent compatibility between ASC30 and ASC39, along with room-temperature stability and a compact tablet size. The combination’s favorable pharmacokinetic profile, combined with ASC30’s potential for best-in-class efficacy and gastrointestinal tolerability and ASC39’s status as the first eloralintide-like small molecule amylin agonist, supports ASC30_39 FDC as a promising once-daily oral therapy for obesity.
ASC30 is an oral small molecule GLP-1R agonist ready to enter Phase III clinical trials. In non-head-to-head studies, weekly titration of ASC30 resulted in half the incidence of vomiting compared to weekly-titrated orforglipron. ASC39 is a potent, selective oral small molecule amylin receptor agonist that has shown eloralintide-like selectivity and efficacy in preclinical models and is now a clinical development candidate.
According to Dr. Wu Jinzi, founder, board chairman, and CEO of ASCLETIS, this represents the first publicly announced oral GLP-1 and oral amylin fixed-dose combination. He emphasized that the selection of this FDC marks a key step in developing a novel, potentially synergistic oral therapy for obesity, highlighting its high bioavailability, extended half-life, and patient-friendly tablet design as factors that may improve treatment outcomes.
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