BEBT-809 is a First-in-Class inhibitor of the GPR75 pathway. In 2021, a study published in "Science" reported that sequencing of nearly 650,000 individuals revealed that those with at least one copy of a G protein-coupled receptor 75 (GPR75) gene mutation had a lower body mass index (BMI), often weighing approximately 5.4 kilograms less than individuals without the mutation, and had a 54% reduced risk of obesity. The study also showed improvements in diabetes-related parameters, including reduced blood sugar levels. In a high-fat diet model, GPR75 gene knockout mice were resistant to weight gain induced by high-fat intake and exhibited improved blood sugar levels. Inhibiting the GPR75 signaling pathway holds promise as a therapeutic strategy for obesity. The company has innovatively developed a series of orally administered small molecule inhibitors targeting the GPR75 signaling pathway, from target screening and biological validation to drug design and compound optimization. The candidate compound, BEBT-809, has been selected and has the potential to become a First-in-Class GPR75 pathway inhibitor. Mechanism of action, pharmacokinetics, weight loss efficacy, early safety pharmacology studies, and patent applications for BEBT-809 have been preliminarily completed. The project is currently in the IND-enabling trial stage.

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