First participants dosed in Ascletis’ 13-week Phase IIa study of oral GLP-1r agonist ASC30

The first participants with obesity or overweight with at least one weight-related comorbidity have been dosed in Ascletis Pharma’s US 13-week Phase IIa study of small molecule oral GLP-1 receptor (GLP-1R) agonist ASC30 for the treatment of obesity. 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.

The Phase IIa study is a 13-week, randomised, double-blind, placebo-controlled and multi-centre study to evaluate the efficacy, safety, and tolerability in participants with obesity (body mass index (BMI) ≥ 30 kg/m2) or overweight (BMI ≥ 27 kg/m2 but < 30 kg/m2) with at least one weight-related comorbidity.

Two oral formulations of ASC30, once-daily are being evaluated: formulation 1 (ASC30 tablets) and formulation 2 (ASC30 tablets A1). The primary endpoint of this Phase IIa study is the mean percentage body weight change from baseline at Week 13. The tolerability and efficacy data from the ASC30 oral Phase Ia and Ib studies support a lower starting dose and slower titration strategy for the 13-week Phase IIa study design of ASC30 oral once-daily.

The 13-week Phase IIa study protocol has a lower starting dose of 1 mg of both formulation 1 and formulation 2, with weekly titrations to the desired maintenance doses of 20 mg and 40 mg of formulation 1 or 20 mg, 40 mg and 60 mg of formulation 2. Both formulations 1 and 2 have been evaluated in the oral ASC30 Phase Ia single ascending dose (SAD) study. Formulation 2 demonstrated a flatter pharmacokinetic profile than formulation 1.

"We are happy that we are ahead of the schedule of our U.S. 13-week Phase IIa study since we have initiated screening of participants in June and recently completed dosing of the first participants," said Dr Jinzi Jason Wu, Founder, Chairman and CEO of Ascletis, "We are looking forward to the topline data from this Phase IIa study in the fourth quarter 2025. As a small molecule, ASC30 has the potential to offer both once-daily oral and once-monthly subcutaneous injection dosing options for obesity treatment, if approved."

ASC30 is a new chemical entity, with US and global compound patent protection until 2044 without patent extensions.