– ASC30 once-daily oral tablet demonstrated up to 6.5% placebo-adjusted mean body weight reduction from baseline after 28-day treatment.
– ASC30 tablet’s higher efficacy is supported by its higher oral drug exposures.
– ASC30 is safe and well tolerated with only mild-to-moderate gastrointestinal (GI) adverse events (AEs). There was no vomiting incidence in multiple ascending dose (MAD) cohort 1 due to 2 mg to 5 mg weekly titration strategy.
HONG KONG, Sept. 17, 2025 /PRNewswire/ — Ascletis Pharma Inc. (HKEX: 1672, “Ascletis”) announces that results from cohorts 1 and 2 of 28-day multiple ascending dose (MAD) study of its oral small molecule GLP-1 receptor (GLP-1R) agonist ASC30 (NCT06680440) were presented in the short oral discussion session event A at the 61st European Association for the Study of Diabetes (EASD) Annual Meeting in Vienna, Austria on September 16, 2025.
The Phase Ib MAD study is a randomized, double-blind, placebo-controlled study, conducted in the U.S., to evaluate safety and tolerability, various titration schemes, pharmacokinetics (PK) and preliminary efficacy of ASC30 once-daily oral tablet in participants with obesity (body mass index (BMI): 30-40 kg/m2).
ASC30 once-daily oral tablet demonstrated a 6.5% placebo-adjusted mean body weight reduction from baseline after 28-day treatment in MAD cohort 2 (weekly titrations of 2 mg, 10 mg, 20 mg, and 40 mg). ASC30 once-daily oral tablet also demonstrated a 4.5% placebo-adjusted mean body weight reduction from baseline after 28-day treatment in MAD cohort 1 (weekly titrations of 2 mg, 5 mg, 10 mg, and 20 mg). No sign of plateau was observed at Day 29.
20 mg and 40 mg ASC30 demonstrated superior oral PK profile at steady state. Higher area under the curve (AUC) positively correlated with greater body weight reduction. Table 1 summarizes the PK profile of ASC30.
Table 1. PK profile of ASC30
|
MAD cohort 1 |
MAD cohort 2 |
||
|
Dose level (mg) |
2, 5, 10, 20 |
2, 10, 20, 40 |
|
|
Day 28 |
Tmax (h) |
8.000 (2.00-8.00) |
8.000 (3.00-24.00) |
|
Cmax (ng/mL) |
272±101 |
397±274 |
|
|
AUC0-24h (h*ng/mL) |
3,560±1,440 |
5,060±2,080 |
|
|
T1/2 (h) |
41.9±12.9 |
35.7±13.7 |
|
Notes: PK: pharmacokinetics; MAD: multiple ascending dose; Tmax: time to maximum concentration, shown as median (range); Cmax: maximum concentration, shown as mean±standard deviation; AUC0-24h: area under the curve over 0-24 hours, shown as mean±standard deviation; T1/2: half-life, shown as mean±standard deviation.
ASC30 is safe and well tolerated with only mild to moderate gastrointestinal (GI) adverse events (AEs). During 28-day treatment and 7-day follow up, MAD cohort 1 (2 mg, 5 mg, 10 mg, and 20 mg) had zero incidence of vomiting. Although vomiting events occurred in MAD cohort 2 (2 mg, 10 mg, 20 mg, and 40 mg), most of these vomiting events occurred during 10 mg titration week and no vomiting event was reported during 2 mg titration week. Taken together, the data suggest that weekly titration from 2 mg to 5 mg represents an appropriate escalation pace and provided key evidence to inform the titration schemes for the Phase IIa study design.
No serious adverse events (SAEs) were reported. There were no Grade 3 or higher AEs observed. There were no elevations of liver enzymes including alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin (TBL) during the treatment. There were no abnormal findings in laboratory tests, vital signs, ECGs (electrocardiograms, including QTc intervals), and physical exams.
Detailed data presented at the 61st EASD Annual Meeting can be found at Ascletis’ website (link).
“We’re very excited that we presented in an oral session the clinical data of ASC30 oral tablet at this year’s EASD Annual Meeting,” said Jinzi Jason Wu, Ph.D., Founder, Chairman and CEO of Ascletis. “ASC30 oral tablet has shown promising efficacy and safety data, which once again demonstrated our strong R&D capabilities to develop more differentiated options for the treatment of obesity. We’re looking forward to reporting topline results from ASC30 oral tablet 13-week Phase IIa study in the fourth quarter this year.”
About ASC30
ASC30 is an investigational GLP-1R biased small molecule agonist and has unique and differentiated properties that enable the same small molecule for both oral tablet and subcutaneous injection administrations. ASC30 is a new chemical entity (NCE), with U.S. and global compound patent protection until 2044 without patent extensions.
About Ascletis Pharma Inc.
Ascletis Pharma Inc. is a fully integrated biotechnology company focused on the development and commercialization of potential best-in-class and first-in-class therapeutics to treat metabolic diseases. Utilizing its proprietary Artificial Intelligence-Assisted Structure-Based Drug Discovery (AISBDD) Platform and Ultra-Long-Acting Platform (ULAP), Ascletis has developed multiple drug candidates in-house, including its lead program, ASC30, a small molecule GLP-1R agonist designed to be administered once daily orally and once monthly to once quarterly subcutaneously as a treatment therapy and a maintenance therapy for chronic weight management. Ascletis is listed on the Hong Kong Stock Exchange (1672.HK).
To learn more about Ascletis, please visit www.ascletis.com.
Contact：
Peter Vozzo
ICR Healthcare
443-231-0505 (U.S.)
Peter.vozzo@icrhealthcare.com
Ascletis Pharma Inc. PR and IR teams
+86-181-0650-9129 (China)
pr@ascletis.com
ir@ascletis.com
