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.
Authors
- Mike Machaba Sathekge (ORCID: https://orcid.org/0000-0002-2806-0625)
- Marwah Abdulrahman (ORCID: https://orcid.org/0000-0001-9863-9053)
- Akram Al‐Ibraheem (ORCID: https://orcid.org/0000-0002-0978-4716)
- Michael Christoph Kreissl (ORCID: https://orcid.org/0000-0001-5905-6015)
- Ahmed Saad Abdlkadir (ORCID: https://orcid.org/0000-0002-2009-5110)
- Saad Ruzzeh (ORCID: https://orcid.org/0009-0003-2916-0905)
- Serin Moghrabi (ORCID: https://orcid.org/0000-0001-9065-3715)
- Hongcheng Shi
Institutions
- 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)
Publication Details
- Journal
- Pharmaceuticals
- Published
- 2026-11-02
- DOI
- https://doi.org/10.3390/ph19111738
- Primary Topic
- Radiopharmaceutical Chemistry and Applications
- Type
- article
- Field-Weighted Citation Impact
- 0.00