Evaluating the therapeutic efficacy of gastramide theranostics targeting cholecystokinin-2 receptors in a preclinical setting

Abstract

Cholecystokinin-2 receptors (CCK2R) are overexpressed in neuroendocrine tumors, making them attractive targets for radiopharmaceutical therapy. However, clinical CCK2R-targeting agents demonstrate limited therapeutic efficacy, with only a small fraction of patients achieving sufficient tumor uptake for effective treatment. This study presents the evaluation of novel gastramide theranostic compounds GA4 and GA13, designed with enhanced structural properties for superior CCK2R targeting. DOTA-GA4, DOTA-GA13, and the clinical standard CP04 were synthesized and radiolabeled with lutetium-177 (177Lu) for comprehensive evaluation. The gastramide analogues achieved superior radiochemical stability ..