GIP receptor antagonism
GIP receptor (GIPR) antagonism represents a novel therapeutic approach that not only holds the potential to deliver significant weight loss but also improves long-term cardiometabolic outcomes in patients.
Our preclinical studies have demonstrated substantial weight loss when combined with GLP-1 receptor agonists (GLP-1RAs) and dual amylin and calcitonin receptor agonists (DACRA), involving mechanisms independent of appetite suppression. In addition, we observed synergistic improvements in glycemic control and lipid profiles, alongside favorable changes in body composition, all without added tolerability issues.
By antagonizing the GIPR in people with overweight and obesity and associated cardiometabolic disease, our approach addresses a dysregulated biological pathway that otherwise contributes to excessive fat storage, insulin resistance, and metabolic dysfunction.