Development and evaluation of 177Lu-imatinib: radiolabeling and cell culture studies
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Emre Ozgenc
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Merve Karpuz
Abstract
Targeted radiopharmaceuticals offer promising approaches for cancer diagnosis and therapy. This study developed freeze-dried kit formulations of 177Lu-Imatinib (IMT) and evaluated their potential efficacy through in vitro studies. Four formulations (F1–F4) containing IMT and chelating agents were prepared and characterized via Fourier transform infrared (FTIR), ultraviolet spectrum (UV), and thermogravimetric analysis (TGA) to confirm complex formation. Biocompatibility was assessed in NIH-3T3 cells using the MTT assay. Radiolabeling with 177Lu was optimized by varying pH, incubation time, and reactant ratios. Radiochemical purity and stability were analyzed over 7 days using HPLC. Binding affinity and cytotoxicity were evaluated in MCF-7 and NIH-3T3 cells. Spectroscopic analyses confirm successful complex formation. All formulations exhibited >90 % viability in NIH-3T3 cells. Optimal radiolabeling conditions (45 mg IMT-chelator, pH 5, 60 min incubation) yielded >90 % efficiency, with stable radiolabeling for 7 days. The 177Lu-IMT-DOTA (F3) formulation showed significantly higher binding and cytotoxic effects in MCF-7 cells compared to controls. The 177Lu-IMT-DOTA (F3) kit demonstrates high radiolabeling efficiency, stability, and selective in vitro cytotoxicity toward breast cancer cells, supporting its potential as a targeted radiopharmaceutical.
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Research ethics: Not applicable.
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Informed consent: Not applicable.
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Author contributions: All authors have accepted responsibility for the entire content of this manuscript and approved its submission.
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Use of Large Language Models, AI and Machine Learning Tools: None declared.
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Conflict of interest: The authors state no conflict of interest.
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Research funding: None declared.
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Data availability: Not applicable.
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