BEBT-809 is a first-in-class, oral 20-HETE/GPR75 pathway inhibitor that demonstrates favorable efficacy and safety compared to GLP-1 drugs in animal models. Unlike GLP-1 agonists, which are injectable and primarily reduce body weight through food intake reduction, BEBT-809 effectively decreases body weight by up to 45% in diet-induced-obesity (DIO) mice without significantly altering food consumption. Additionally, it minimizes body weight rebound, enhances insulin sensitivity, and preserves lean muscle mass while reducing white adipose tissue. BEBT-809 also offers a significant safety advantage with over 200-fold safety margins, showcasing its potential as a novel, more compliant, cost-effective, and efficacious therapy for obesity and diabetes compared to GLP-1 drugs.