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<p>In this study, a novel theranostic radiopharmaceutical, [<sup>13x</sup>La]La-FAP-2286, for targeting Fibroblast Activation Protein (FAP)-positive tumors. The theranostic pair of <sup>132</sup>La (half-life: 4.59&#xa0;h, 42.1% β⁺) and <sup>135</sup>La (half-life: 18.91&#xa0;h, 100% EC) was produced via proton bombardment of natural barium in a 30&#xa0;MeV cyclotron, achieving high radionuclidic purity (99.9%) and radiochemical purity (RCP &gt; 99%). Stability tests revealed the RCP greater than 91% over 24&#xa0;h in human serum and PBS buffer. Cellular studies confirmed high binding affinity (K<sub>D</sub> = 0.51 ± 0.12 nM) and effective internalization of [<sup>13x</sup>La]La-FAP-2286 in FAP + tumor cells. Distribution coefficient (log <i>D</i>) measurements demonstrated high hydrophilicity of the complex with a value of − 3.21 ± 0.14. Imaging and biodistribution studies in tumor-bearing mice further confirmed tumor targeting, with significant uptake observed up to 48&#xa0;h post-injection. These results suggest [<sup>13x</sup>La]La-FAP-2286 can be considered a candidate for theranostic applications, offering both practical PET imaging and targeted Auger-electron therapy for cancer treatment.</p>

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Preclinical evaluation of [13xLa]La-FAP-2286 as a novel theranostic agent for tumors expressing fibroblast activation protein

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年3月3日

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  • Ali Shirpour,
  • Asghar Hadadi,
  • Samaneh Zolghadri,
  • Sara Vosoughi,
  • Saeed Rajabifar

摘要

In this study, a novel theranostic radiopharmaceutical, [13xLa]La-FAP-2286, for targeting Fibroblast Activation Protein (FAP)-positive tumors. The theranostic pair of 132La (half-life: 4.59 h, 42.1% β⁺) and 135La (half-life: 18.91 h, 100% EC) was produced via proton bombardment of natural barium in a 30 MeV cyclotron, achieving high radionuclidic purity (99.9%) and radiochemical purity (RCP > 99%). Stability tests revealed the RCP greater than 91% over 24 h in human serum and PBS buffer. Cellular studies confirmed high binding affinity (KD = 0.51 ± 0.12 nM) and effective internalization of [13xLa]La-FAP-2286 in FAP + tumor cells. Distribution coefficient (log D) measurements demonstrated high hydrophilicity of the complex with a value of − 3.21 ± 0.14. Imaging and biodistribution studies in tumor-bearing mice further confirmed tumor targeting, with significant uptake observed up to 48 h post-injection. These results suggest [13xLa]La-FAP-2286 can be considered a candidate for theranostic applications, offering both practical PET imaging and targeted Auger-electron therapy for cancer treatment.