Gan & Lee Pharmaceuticals has announced positive topline results from a Phase 1 clinical trial of its oral glucagon-like peptide-1 receptor agonist (GLP-1 RA), GZR18 tablets. The study, conducted in healthy participants in China, assessed the bioavailability, pharmacokinetics (PK), pharmacodynamics (PD), safety, and tolerability of the drug.
The randomized, open-label, first-in-human study involved 92 participants. Key findings include that GZR18 tablets were safe and well-tolerated, with gastrointestinal reactions being the most common adverse events, consistent with the established safety profile of GLP-1 based therapies. PK data indicated favorable absorption, supporting a once-daily oral regimen. Both single and multiple doses showed a dose-response relationship in terms of PK and PD parameters.
Weight Reduction Observed
Participants treated with the target dose of 60 mg daily for two weeks exhibited an average weight reduction of 4.16% from baseline. Notably, a week after stopping treatment, subjects continued to lose weight by 0.51%, reaching an average total reduction of 4.67% compared to baseline. At 21 days after discontinuation, neither the participants' body weight nor BMI had returned to baseline values.
About GZR18
GZR18 is an investigational, once-daily oral GLP-1 receptor agonist developed by Gan & Lee Pharmaceuticals. It utilizes a small molecule absorption enhancer, SNAC (N-[8-(2-hydroxybenzoyl)amino] caprylate), to facilitate drug absorption in the stomach by resisting pepsin degradation, thus prolonging the drug's half-life and enhancing its bioavailability. GZR18 tablets are currently in global Phase 1 clinical development.
Gan & Lee Pharmaceuticals developed the first Chinese domestic insulin analog. In China’s 2024 National Insulin-Specific Centralized Procurement, Gan & Lee Pharmaceuticals ranked first among all selected companies in terms of procurement demand for insulin analogs. The company is also making strides in international markets, with the disposable pen needle (GanleeFine®) approved by the US Food and Drug Administration (FDA) in 2020 and received GMP inspection approval from the European Medicines Agency (EMA) in 2024.
