Innovent Biologics (HKEX: 01801) has registered a Phase I study of IBI3042, an oral small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist designed for once-weekly dosing. The trial, which will be held in China, represents one of the latest entrants to the oral GLP-1 space, with multiple small-molecule programs now advancing through late-stage development.
The study (NCT07802899) is a two-part, randomized, triple-masked, placebo-controlled Phase I trial enrolling up to 94 healthy, overweight, and obese adults at the First Affiliated Hospital of Henan University of Science and Technology in Luoyang, China. Part A evaluates single ascending doses in healthy or overweight participants (BMI 20–28 kg/m²); Part B evaluates multiple ascending doses over 29 days in overweight or obese participants (BMI 24–40 kg/m²). Secondary endpoints in Part B include changes in body weight, body mass index, and waist circumference. The trial is listed as not yet recruiting, with an estimated start date of September 2026 and primary completion expected in March 2027.
IBI3042 activates the GLP-1R through a non-peptide small-molecule mechanism, producing glucose-lowering and weight-reducing effects without β-arrestin recruitment in preclinical assays — a signaling profile that Innovent said at the 2026 American Diabetes Association (ADA) Scientific Sessions may be relevant to tolerability. According to Innovent, in mice and monkey models IBI3042 produced efficacy that was comparable to or exceeded orforglipron. Innovent said in its June 2026 ADA press release that IBI3042 is "potentially the world's first once-weekly oral small-molecule GLP-1 receptor agonist candidate entering clinical studies by the end of 2026".