Dimeric CCK2R radiotheranostic tracers synergize with mTOR inhibition for enhanced tumor therapy.

ABSTRACT: Purpose: The cholecystokinin-2 receptor (CCK2R) is highly expressed in several neuroendocrine cancers, particularly in medullary thyroid carcinoma (MTC) and small cell lung cancer (SCLC) and represents a promising target for radiotheranostic applications. Several minigastrin-derived analogs, such as DOTA-MGS5 and DOTA-CCK-66, have demonstrated favorable tumor targeting and imaging performance. Building on these advances, we developed and evaluated a novel dimeric CCK₂R-targeted radiotracer, and further investigated its radiosensitization potential in combination with mTOR inhibition. Experimental Design: We designed a dimeric CCK₂R-targeted agent, DOTA-CCK₂R-dimer, labeled with ⁶⁸Ga for PET imaging and ¹⁷⁷Lu for radionucl

SUBMITTER: Bian L 

PROVIDER: S-EPMC12439480 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature