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Bioorganic & Medicinal Chemistry

Bioorganic & Medicinal Chemistry

IF: 3.3
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Tc-99m labeled PSMA-617 as a potential SPECT radiotracer for prostate cancer diagnostics: Complexation optimization and its in vitro/vivo evaluation

Published:1 February 2025 DOI: 10.1016/j.bmc.2024.118058 PMID: 39754852
Kalapaphuk Tachatumvitoon , Charasphat Preuksarattanawut , Thititip Tippayamontri , Piyachai Khomein

Abstract

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. The new formulation for Tc-99m complexation with PSMA-617, a current ligand for radionuclide therapy of prostate cancer with lutetium-177 (Lu-177), has been investigated. Co-complexation with citrate was utilized to improve the labeling efficiency by over 97?%. The stability of the new radiopharmaceutical was in vitro evaluated confirming that the Tc-99m labeled PSMA-617 remained stable for over a single half-life of Tc-99m in normal saline solution and in human serum. The in vivo study in the LNCaP xenografted mouse model confirmed a high selectivity of the new tracer toward prostate cancer.

Substances (4)

Materials
Procduct Name CAS Molecular Formula Supplier Price
PSMA-617 1702967-37-0 C49H71N9O16 49 suppliers Inquiry
PSMA-617 1702967-37-0 C49H71N9O16 49 suppliers Inquiry
PSMA-617 1702967-37-0 C49H71N9O16 49 suppliers Inquiry
PSMA-617 1702967-37-0 C49H71N9O16 49 suppliers Inquiry

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