ASCLETIS-B (01672) announced that the company presented results from Cohorts 1 and 2 of its ASC30 oral small molecule GLP-1 receptor (GLP-1R) agonist 28-day multiple ascending dose (MAD) study (NCT06680440) during the brief oral discussion session A at the 61st European Association for the Study of Diabetes (EASD) annual meeting 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 designed 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 (2mg, 10mg, 20mg, and 40mg with weekly dose escalation), ASC30 once-daily oral tablets demonstrated a placebo-adjusted mean weight loss of 6.5% relative to baseline after 28 days of treatment. In MAD Cohort 1 (2mg, 5mg, 10mg, and 20mg with weekly dose escalation), ASC30 once-daily oral tablets showed a placebo-adjusted mean weight loss of 4.5% relative to baseline after 28 days of treatment. No signs of weight loss plateau were observed on Day 29.

The 20mg and 40mg ASC30 doses showed superior oral PK characteristics at steady state. Higher area under the curve (AUC) was positively correlated with more significant weight loss. Table 1 summarizes the PK characteristics of ASC30.

ASC30 demonstrated good safety and tolerability, with only mild to moderate gastrointestinal (GI) adverse events (AEs). During the 28-day treatment period and 7-day follow-up period, the incidence of vomiting was zero in MAD Cohort 1 (2mg, 5mg, 10mg, and 20mg). Although vomiting events occurred in MAD Cohort 2 (2mg, 10mg, 20mg, and 40mg), most occurred during the 10mg dose escalation week, with no vomiting events reported during the 2mg dose escalation week.

In summary, the data indicate that weekly escalation from 2mg to 5mg is an appropriate escalation rate and provides key evidence for dose escalation regimens in Phase IIa study design. No serious adverse events (SAEs) were reported, and no Grade 3 or higher AEs were observed. Liver enzymes, including alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bilirubin (TBL), showed no elevation during treatment. Laboratory tests, vital signs, ECGs (electrocardiograms, including heart rate-corrected QT interval (QTc)), and physical examinations revealed no abnormalities.