Research progress on the development and clinical translation of αvβ6-targeted radiopharmaceuticals

Integrin αvβ6 is minimally expressed in normal epithelial tissues but is upregulated in a wide range of malignancies and fibrotic diseases, where it is closely linked to epithelial remodeling, tumor invasion, and disease progression. Owing to its restricted expression pattern and biological significance, integrin αvβ6 has emerged as an attractive target for molecular imaging and targeted therapy. This review summarizes recent progress in the development of αvβ6-targeted radiopharmaceuticals, covering linear and cyclic peptide-based tracers as well as emerging theranostic agents. These advances have led to imaging agents with improved in vivo imaging performance and enhanced translational potential, while also highlighting the complementary biological information provided by imaging of integrin αvβ6 in oncology and fibrotic diseases. Several radiopharmaceuticals have entered early clinical evaluation, providing initial evidence for the clinical feasibility of αvβ6-specific imaging and supporting its further investigation in oncology and fibrosis. In parallel, the development of αvβ6-targeted radionuclide therapy has broadened the therapeutic landscape and strengthened interest in αvβ6-targeted theranostic strategies. Together, these developments support continued evaluation of αvβ6-targeted radiopharmaceuticals for precision imaging and theranostic applications.