ASCLETIS-B (01672) announced that it has recently received approval from the U.S. Food and Drug Administration (FDA) for the Investigational New Drug (IND) application for its oral small molecule GLP-1 drug, ASC30, for a Phase II study in subjects with diabetes.

This Phase II study is a 13-week, randomized, double-blind, placebo-controlled, and multicenter trial designed to evaluate the efficacy, safety, and tolerability of ASC30 in subjects with type 2 diabetes.

The primary endpoint of this Phase II study is the mean change from baseline in glycated hemoglobin (HbA1c) at week 13, comparing the treatment group to the placebo group.

Secondary endpoints include: the mean change from baseline in fasting plasma glucose at week 13, comparing the treatment group to the placebo group; the mean change from baseline in body weight at week 13, comparing the treatment group to the placebo group; as well as safety and tolerability.

The Phase II study will enroll approximately 100 subjects with type 2 diabetes across multiple centers in the United States.

Subjects will be randomly assigned in a ratio of approximately 2:3:3:2 to the 40 mg, 60 mg, and 80 mg ASC30 tablet treatment groups and a matching placebo group, respectively.

ASC30 will be initiated at a dose of 1 mg and titrated weekly up to the target doses of 40 mg, 60 mg, and 80 mg.

Subject enrollment is expected to commence in the first quarter of 2026.

ASCLETIS has recently completed its 13-week Phase II study (NCT07002905) evaluating the oral small molecule GLP-1 receptor (GLP-1R) agonist ASC30 for the treatment of obesity.

This study was conducted at multiple centers in the U.S. and enrolled a total of 125 obese subjects or overweight subjects with at least one weight-related comorbidity.

At the primary endpoint of week 13, once-daily 20 mg, 40 mg, and 60 mg ASC30 tablets achieved placebo-adjusted mean body weight reductions of 5.4%, 7.0%, and 7.7%, respectively, demonstrating statistically significant, clinically meaningful, and dose-dependent weight loss.

No weight loss plateau was observed.

The incidence of vomiting with weekly-titrated ASC30 was approximately half of the published vomiting incidence observed with weekly-titrated orforglipron.

The gastrointestinal tolerability of weekly-titrated ASC30 was comparable to the published results of orforglipron titrated every four weeks in the Phase III ATTAIN-1 study.

In the Phase II study of ASC30 for the treatment of obesity or overweight, the overall discontinuation rate due to adverse events was 4.8%.

ASC30, independently developed by ASCLETIS, is the first and only small molecule GLP-1R full biased agonist currently in clinical studies that can be administered either once-daily orally or via subcutaneous injection from once-monthly to once-quarterly, for the treatment of obesity, diabetes, and other metabolic diseases.

"The IND approval for this Phase II study in diabetes treatment is a significant milestone for ASCLETIS as we continue to accumulate research data on ASC30," said Dr. Jinzi J. Wu, Founder, Chairman of the Board, and Chief Executive Officer of ASCLETIS.

"Furthermore, the FDA's approval of our IND application paves the way for the clinical development of ASC30 to enter the vast diabetes treatment market."