αvβ6-Integrin-Targeted Radiopharmaceuticals in Oncology: A Scoping Review of Diagnostic Imaging and Emerging Theranostic Applications

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.

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Publication Details

Journal
Pharmaceuticals
Published
2026-11-02
DOI
https://doi.org/10.3390/ph19111738
Primary Topic
Radiopharmaceutical Chemistry and Applications
Type
article
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article

αvβ6-Integrin-Targeted Radiopharmaceuticals in Oncology: A Scoping Review of Diagnostic Imaging and Emerging Theranostic Applications

Mike Machaba Sathekge, Marwah Abdulrahman, Akram Al‐Ibraheem, Michael Christoph Kreissl et al.
2 links
Pharmaceuticals
Radiopharmaceutical Chemistry and Applications
article

αvβ6-Integrin-Targeted Radiopharmaceuticals in Oncology: A Scoping Review of Diagnostic Imaging and Emerging Theranostic Applications

Mike Machaba Sathekge, Marwah Abdulrahman, Akram Al‐Ibraheem, Michael Christoph Kreissl, Ahmed Saad Abdlkadir, Saad Ruzzeh, Serin Moghrabi, Hongcheng Shi
article en

Abstract

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.

PharmaceuticalsVol. 19(11)
University of Jordan (JO), Fudan University (CN), King Hussein Cancer Center (JO), Steve Biko Hospital (ZA), Zhongshan Hospital (CN), University Hospital Magdeburg (DE), University of Pretoria (ZA)
Good health and well-being
Openalex Percentile: Top 15%
Radiopharmaceutical Chemistry and Applications
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