ASCLETIS-B (01672) reported the results of its ASC30 oral small molecule GLP-1R agonist multi-dose escalation studies in Cohorts 1 and 2 at the 61st Annual Meeting of the European Association for the Study of Diabetes.

ASCLETIS-B (01672) announced that the company reported the results of its ASC30 oral small molecule GLP-1 receptor (GLP-1R) agonist 28-day multiple dose escalation (MAD) study (NCT06680440) in Cohort A at the 61st Annual Meeting of the European Association for the Study of Diabetes (EASD) held in Vienna, Austria on September 16, 2025. The phase Ib MAD study is a randomized, double-blind, placebo-controlled study conducted in the United States to evaluate the safety and tolerability, different dose escalation regimens, pharmacokinetic (PK) characteristics, and preliminary efficacy of ASC30 once-daily oral tablets in obese subjects (body mass index (BMI): 30-40 kg/m2). In MAD Cohort 2 (2 mg, 10 mg, 20 mg, and 40 mg, weekly dose escalation), ASC30 once-daily oral tablets showed an average weight decrease of 6.5% compared to baseline after 28 days of treatment. In MAD Cohort 1 (2 mg, 5 mg, 10 mg, and 20 mg, weekly dose escalation), ASC30 once-daily oral tablets showed an average weight decrease of 4.5% compared to baseline after 28 days of treatment. There were no signs of a weight loss plateau on day 29. The 20 mg and 40 mg doses of ASC30 showed favorable oral PK characteristics at steady-state. Higher area under the curve (AUC) values were positively correlated with more significant weight loss. Table 1 summarizes the PK characteristics of ASC30. ASC30 showed good safety and tolerability, with only mild to moderate gastrointestinal (GI) adverse events (AEs) reported. In the 28-day treatment period and 7-day follow-up period, there were no reports of vomiting in MAD Cohort 1 (2 mg, 5 mg, 10 mg, and 20 mg). While vomiting events occurred in MAD Cohort 2 (2 mg, 10 mg, 20 mg, and 40 mg), most occurred during the 10 mg dose escalation cycle, and no vomiting events were reported during the 2 mg dose escalation week. Overall, the data suggest that escalating from 2 mg to 5 mg weekly is an appropriate escalation speed and provides key guidance for dose escalation regimens designed for phase IIa studies. There were no reports of serious adverse events (SAEs), and no grade 3 or higher AEs were observed. Liver enzymes including alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bilirubin (TBL) did not increase during treatment. Laboratory tests, vital signs, ECGs (electrocardiograms, including QTc interval corrected for heart rate), and physical examinations did not reveal any abnormalities.