68Ga-Trivehexin: Current Status of αvβ6-Integrin Imaging and Perspectives

Significant advancements have been made in molecular imaging, particularly positron emission tomography (PET), which has evolved from using metabolic radiotracers like 2-deoxy-2-[18F]fluoro-D-glucose [18F]FDG to more targeted probes. Among these, αvβ6-integrin has emerged as a promising target for both oncological and non-oncological diseases. This review explores the radiochemical properties and initial clinical applications of the PET probe [68Ga]Ga-Trivehexin. Preclinical and clinical studies are discussed, focusing on its radiochemical characteristics and preliminary clinical uses, highlighting advancements, challenges, and future potential. The results show that the optimized multimeric system significantly improved pharmacokinetic properties, binding affinity, and selectivity for αvβ6-integrin, achieving up to an 18-fold enhancement compared to previous monomeric tracers. Preliminary clinical applications, particularly in head and neck cancer and pancreatic adenocarcinoma, have demonstrated promising detection rates and improved differential diagnosis compared to [18F]FDG. Additionally, [68Ga]Ga-Trivehexin has shown potential in non-oncological conditions such as idiopathic pulmonary fibrosis and primary hyperthyroidism. This review emphasizes the progress made in the design and application of [68Ga]Ga-Trivehexin, a highly promising PET tracer for both oncological and non-oncological imaging.