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Purpose: [(18)F]VM4-037 was recently developed as a positron emission tomography (PET) tracer for the detection of carbonic anhydrase IX (CAIX), a tumor-specific protein upregulated under hypoxic conditions. In this study, the accumulation of [(18)F]VM4-037 was determined in two CAIX-expressing preclinical human tumor models.
Procedures: U373 and HT29 tumor-bearing animals were injected with [(18)F]VM4-037 and underwent microPET imaging up to 4 h post-injection (p.i.). Biodistribution throughout the different organs was assessed at 2 and 4 h p.i. using gamma counting.
Results: MicroPET imaging showed high [(18)F]VM4-037 uptake in the abdominal region, and biodistribution revealed high radioactivity in the kidney, ileum, colon, liver, stomach, and bladder. Although high CAIX expression was confirmed in both tumor models, tumor uptake assessed with microPET and biodistribution experiments was comparable to background tissues.
Conclusions: In this study, [(18)F]VM4-037 does not specifically accumulate in CAIX-expressing tumors, indicating that the tracer is not suitable for the detection of CAIX.
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http://dx.doi.org/10.1007/s11307-015-0831-y | DOI Listing |
Mol Imaging Biol
September 2025
Biomedical Engineering, Case Western Reserve University, Cleveland, OH, USA.
Purpose: While PSMA-targeted radioligand therapy (RLT) has shown remarkable efficacy for treating end-stage prostate cancer, the α-emitting RLT often results in severe salivary gland toxicity, limiting its use. Various strategies to mitigate this side effect have been attempted with limited success. Accordingly, this study introduced a new PSMA-targeting ligand with more favorable binding characteristics than the existing ligands.
View Article and Find Full Text PDFAcad Radiol
August 2025
Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (Y.Z., R.H.M.). Electronic address:
Rationale And Objectives: Prolonged oxidative stress, driven by aggregation of misfolded proteins such as amyloid beta (Aβ), alpha-synuclein (aSyn), and tau, plays a key role in neurodegenerative disease (ND) progression. Yet, the lack of noninvasive tools to monitor oxidative stress in vivo limits clinical tracking of disease. To address this, we evaluated [18 F]ROStrace, a novel superoxide (O₂·⁻)-sensitive PET tracer, in three proteinopathy-associated ND mouse models.
View Article and Find Full Text PDFBioconjug Chem
August 2025
Key Laboratory of Radiation Physics and Technology of the Ministry of Education, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064, P. R. China.
Fibroblast activation protein (FAP)-targeted radioligands have recently emerged as attractive tumor imaging agents. However, the therapeutic applicability of most FAP ligands has been impeded by their short tumor retention. In this study, a tetrazine (Tz)-modified FAPI derivant DOTA-FAPI-Tz was synthesized and radiolabeled with Lu and Zr to produce Zr-FAPI-Tz and Lu-FAPI-Tz with high radiochemical purity.
View Article and Find Full Text PDFNucl Med Biol
August 2025
Department of Medical Neuroscience, Donders Institute for Brain, Cognition, and Behavior, Radboud University Medical Center, Nijmegen, the Netherlands.
Rationale: [C]DASB is widely used for PET imaging of brain serotonin transporters (SERT) and the tropane ligand [F]FE-PE2I is used for PET imaging of dopamine transporters (DAT). However, their in vivo selectivity has not been confirmed using knockout (KO) models. This study aimed to provide direct in vivo evidence for the selectivity of these tracers using SERT and DAT KO rats.
View Article and Find Full Text PDFMol Pharm
August 2025
Department of Nuclear Medicine, Xijing Hospital, The Fourth Military Medical University, Xi'an 710000, China.
Myeloperoxidase (MPO), a well-established biomarker of neutrophil activation, plays a crucial role in early acute inflammation. In the study, we developed an MPO-specific PET ligand, Ga-NOTA-3G-bis-5HT, for noninvasive imaging of early acute inflammation. Ga-NOTA-3G-bis-5HT was achieved with a radiochemical yield of >70%, radiochemical purity of >95%, and molar activity of 6.
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