ArticleEuropean journal of nuclear medicine and molecular imaging2026
A LAT1-selective PET tracer, 5-[¹⁸F]F-αMe-3BPA, as a companion to its structurally matched ¹⁰B analog in boron neutron capture therapy.
Article in European journal of nuclear medicine and molecular imaging, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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3 citing papers in PubMed.
- SLC Transporter-Mediated Functional Imaging in Cancer Diagnosis.Biomolecules · 2026Review
- Optimization of [EJNMMI radiopharmacy and chemistry · 2026Article
- Preclinical Evaluation of 5F-αMe-3BPA for Improving Pharmacokinetics in Boron Neutron Capture Therapy.Pharmaceutics · 2026Article
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6 authors.
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Abstract
purposeThis study aimed to develop and evaluate 5-[¹⁸F]F-αMe-3BPA, a novel PET probe designed as a theranostic partner for 5F-αMe-3[¹⁰B]BPA in Boron Neutron Capture Therapy (BNCT). The goal was to address limitations of the clinically used BPA/[¹⁸F]FBPA pair, including poor water solubility, limited LAT1 specificity, and suboptimal diagnostic performance, thereby improving tumor-selective drug delivery and enabling accurate prediction of therapeutic biodistribution through structure-matched PET/BNCT.
methodsLAT1 dependency was tested in vitro using cancer cell lines with differential LAT1 expression. In vivo biodistribution of both therapeutic agents and their ¹⁸F-labeled analogs were assessed in xenograft mouse models. Radiosynthesis of 5-[¹⁸F]F-αMe-3BPA was achieved via copper-catalyzed nucleophilic radiofluorination. PET/CT imaging compared tumor visualization with [¹⁸F]FBPA. Co-injection studies (5-[¹⁸F]F-αMe-3BPA/5F-αMe-3BPA and [¹⁸F]FBPA/BPA) quantitatively evaluated concordance between ¹⁸F radioactivity and boron concentrations across tissues.
results5F-αMe-3BPA uptake in cancer cells was strictly LAT1-dependent. In LAT1-high T3M-4 xenografts, its tumor-to-muscle boron ratio (22) far exceeded BPA (3.4). 5-[¹⁸F]F-αMe-3BPA was synthesized successfully and achieved a tumor-to-muscle ratio of 29 versus 5.3 for [¹⁸F]FBPA. PET imaging showed clear, high-contrast visualization of T3M-4 tumors, with co-injection confirming strong concordance between PET probe and therapeutic agent biodistribution.
conclusionThe 5-[¹⁸F]F-αMe-3BPA/5F-αMe-3[¹⁰B]BPA theranostic pair demonstrates high LAT1 specificity, low normal tissue uptake, and strong pharmacokinetic alignment, enabling accurate prediction of therapeutic boron delivery for BNCT. Furthermore, 5-[¹⁸F]F-αMe-3BPA shows promise as a dedicated LAT1 imaging probe for advancing LAT1-targeted therapies.
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