Ascletis Pharma Inc. (HKEX: 1672), a China-based pharmaceutical company, announced on Wednesday that the first participants with obesity or overweight with at least one weight-related comorbidity have been dosed in a U.S. 13-week Phase IIa study of small molecule oral GLP-1 receptor (GLP-1R) agonist ASC30 for the treatment of obesity.

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) greater than 30 kg/m2) or overweight (BMI greater than 27 kg/m2 but less than 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 company says that 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.

ASC30 was discovered and developed in-house at Ascletis as a first and only investigational small molecule GLP-1R biased agonist designed to be dosed once daily orally and once monthly subcutaneously for the treatment of obesity.