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Life sciences · Journal article
Pharmaceuticals · November 2, 2026
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Background/Objectives: αvβ6-integrin is an emerging target for molecular imaging and radioligand therapy in epithelial malignancies. We mapped human oncologic evidence for αvβ6-targeted radiopharmaceuticals. Methods: PubMed/MEDLINE, Scopus, and Embase were searched through 1 September 2026. Human clinical studies and informative case-based reports of αvβ6-targeted imaging or therapy in oncologic and cancer-related settings were included. Study characteristics, tracers, comparators, validation methods, and clinical applications were charted and synthesized descriptively in accordance with PRISMA-ScR. Results: Thirty-nine publications included an estimated 223 unique participants after accounting for probable cohort overlap. Thirty-seven addressed imaging and two described [177Lu]Therahexin-503 therapy in single patients. [68Ga]Ga-Trivehexin was the most frequently reported diagnostic tracer. Evidence was concentrated in pancreatic, lung, and head-and-neck cancers; other malignancies were sparsely represented. Tumor visualization was feasible across several tracer platforms, and selected reports suggest a potentially complementary role alongside [18F]FDG PET/CT, particularly for equivocal nodal or inflammatory findings. Imaging protocols and reference standards varied, and most publications were small or case-based. Conclusions: αvβ6-targeted PET is promising but investigational. Prospective disease-specific studies with standardized acquisition, histopathological validation, and clinically relevant outcomes are needed; neither objective response nor progression-free survival was reported in the two therapeutic cases, and efficacy and long-term safety remain unestablished.