DPI-4452

DPI-4452 is a CAIX-targeting cyclic peptidomimetic with a DOTA cage, enabling chelation with radionuclides such as gallium-68 or lutetium-177 for theranostic applications. It is designed to selectively bind carbonic anhydrase IX (CAIX), a transmembrane enzyme overexpressed in many hypoxic solid tumors, including clear cell renal cell carcinoma (ccRCC), colorectal cancer (CRC), and pancreatic ductal adenocarcinoma (PDAC). The drug is developed in two forms: [68Ga]Ga-DPI-4452 for PET imaging and [177Lu]Lu-DPI-4452 for targeted radiotherapy. DPI-4452 demonstrates high specificity and affinity for CAIX, minimal off-target binding, rapid elimination from the body, and has shown strong tumor growth inhibition in preclinical models. Its mechanism leverages the restricted expression of CAIX in healthy tissues versus its high prevalence on certain tumor cells to enable precise diagnosis and therapy within the field of theranostics[1][3][4][5][7][8].