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Preclinical and First-in-Human Study of a Compact Radionuclide Labeled Self-Assembly Nanomedicine for Chemo-Radio-Theranostics of Cancer.
ACS Nano
January 2025
Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, 119074, Singapore.
The emerging combination of chemotherapy and radionuclide therapy has been actively investigated to overcome the limitations of monotherapy and augment therapeutic efficacy. However, it remains a challenge to design a single delivery vehicle that can incorporate chemotherapeutics and radionuclides into a compact structure. Here, a chelator DOTA- or NOTA-modified Evans blue conjugated camptothecin molecule (EB-CPT) nanoprodrug was synthesized, which could self-assemble into nanoparticles due to its inherent amphiphilicity.
View Article and Find Full Text PDFSynthesis and characterisation of DOTA-kisspeptin-10 as a potential gallium-68/lutetium-177 pan-tumour radiopharmaceutical.
J Neuroendocrinol
January 2025
Centre for Neuroendocrinology, University of Pretoria, Pretoria, South Africa.
Kisspeptin (KISS1) and its cognate receptor (KISS1R) are implicated in the progression of various cancers. A gallium-68 labelled kisspeptin-10 (KP10), the minimal biologically active structure, has potential as a pan-tumour radiopharmaceutical for the detection of cancers. Furthermore, a lutetium-177 labelled KP10 could find therapeutic application in treating oncological diseases.
View Article and Find Full Text PDFImprovement of End-of-Synthesis Radiochemical Purity of Lu-DOTA-PSMA-Ligands with Alternative Synthesis Approaches: Conversion Upswing and Side-Products Minimization.
Pharmaceutics
November 2024
State Research Center-Burnasyan Federal Medical Biophysical Center of Federal Medical Biological Agency, Zhivopisnaya Str., Bld. 46, 123098 Moscow, Russia.
Background: Radiochemical purity is a key criterion for the quality of radiopharmaceuticals used in clinical practice. The joint improvement of analytical methods capable of identifying related radiochemical impurities and determining the actual radiochemical purity, as well as the improvement of synthesis methods to minimize the formation of possible radiochemical impurities, is integral to the implementation of high-tech nuclear medicine procedures. PSMA-targeted radionuclide therapy with lutetium-177 has emerged as an effective treatment option for prostate cancer, and [Lu]Lu-PSMA-617 and [Lu]Lu-PSMA have achieved global recognition as viable radiopharmaceuticals.
View Article and Find Full Text PDFTc-99m labeled PSMA-617 as a potential SPECT radiotracer for prostate cancer diagnostics: Complexation optimization and its in vitro/vivo evaluation.
Bioorg Med Chem
February 2025
Division of Nuclear Medicine, Department of Radiology, Faculty of Medicine, Chulalongkorn University, Bangkok 10330, Thailand. Electronic address:
Technetium-99m (Tc-99m) is the most employed radionuclide in nuclear imaging diagnostics worldwide for many diseases. The ideal physiochemical properties of Tc-99m (such as half-life and pure gamma energy) make it favorable for Single Photon Emission Computed Tomography (SPECT). In this study, we aim to expand the utilization of Tc-99m radiopharmaceutical toward prostate cancer diagnostics which is currently no FDA approved products and has been intensively examined for a potential candidate.
View Article and Find Full Text PDFComparative Study of Dimeric Fibroblast Activation Protein-Targeting Radioligands Labeled with Fluorine-18, Copper-64, and Gallium-68.
Mol Pharm
December 2024
Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul 06351, Republic of Korea.
Fibroblast activation protein inhibitors (FAPIs) labeled with gallium-68 and lutetium-177 show potential for use in the diagnosis and treatment of various cancers expressing FAP. However, Lu-labeled FAPIs often exhibit short tumor retention time, limiting their therapeutic applications. To improve tumor retention, we synthesized three radiolabeled dimeric FAPIs, [F], [Cu], and [Ga].
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