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<p>This study reports the use of domestically produced <sup>177</sup>Lu for radiosynthesis and the characterization of [<sup>177</sup>Lu]Lu-PEG-modified DOTA as a stable and hydrophilic precursor for targeted radiopharmaceuticals. The conjugate was synthesized by coupling DOTA-NHS ester and SH-PEG-NH₂ to form an amide, followed by radiolabeling with [<sup>177</sup>Lu]LuCl₃ produced in the G.A. Siwabessy multipurpose reactor, Indonesia. Optimal labeling conditions (pH 5.0, 80°C, 1:2 molar ratio, 10&#xa0;min) resulted in &gt; 99% radiochemical purity and excellent in vitro stability in PBS (pH 7.4) for up to 168&#xa0;h at 4°C and 25°C. PEGylation significantly increased the hydrophilicity, as indicated by the lower log D value (− 1.996 ± 0.028) compared to [<sup>177</sup>Lu]Lu-DOTA without PEGylation (− 1.933 ± 0.057). These results indicate that DOTA modified with [<sup>177</sup>Lu]Lu-PEG is a promising, stable, and highly hydrophilic platform suitable for bioconjugation with tumor-targeting biomolecules in theranostic applications. This study highlights the feasibility of utilizing locally produced <sup>177</sup>Lu for the development of advanced radiopharmaceuticals, supporting national self-reliance in nuclear medicine.</p>

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[177Lu]Lu-PEG-DOTA platform for theranostics: optimized radiosynthesis using domestically sourced 177Lu in GA Siwabessy multipurpose reactor

  • 期刊论文

  • 发表日期：

    2026年1月12日

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  • Maskur,
  • Ligwina Dita Pertiwi,
  • Yono Sugiharto,
  • Sumandi Juliyanto,
  • Fransiska Christydira Sekaringtyas,
  • Miftakul Munir,
  • Ahsanal Fikri,
  • Herlan Setiawan,
  • Ilma Darojatin,
  • Muhammad Ridwan,
  • Rien Ritawidya

摘要

This study reports the use of domestically produced 177Lu for radiosynthesis and the characterization of [177Lu]Lu-PEG-modified DOTA as a stable and hydrophilic precursor for targeted radiopharmaceuticals. The conjugate was synthesized by coupling DOTA-NHS ester and SH-PEG-NH₂ to form an amide, followed by radiolabeling with [177Lu]LuCl₃ produced in the G.A. Siwabessy multipurpose reactor, Indonesia. Optimal labeling conditions (pH 5.0, 80°C, 1:2 molar ratio, 10 min) resulted in > 99% radiochemical purity and excellent in vitro stability in PBS (pH 7.4) for up to 168 h at 4°C and 25°C. PEGylation significantly increased the hydrophilicity, as indicated by the lower log D value (− 1.996 ± 0.028) compared to [177Lu]Lu-DOTA without PEGylation (− 1.933 ± 0.057). These results indicate that DOTA modified with [177Lu]Lu-PEG is a promising, stable, and highly hydrophilic platform suitable for bioconjugation with tumor-targeting biomolecules in theranostic applications. This study highlights the feasibility of utilizing locally produced 177Lu for the development of advanced radiopharmaceuticals, supporting national self-reliance in nuclear medicine.