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<p>Overexpression of indoleamine 2, 3-dioxygenase (IDO) in tumors leads to excessive consumption of tryptophan and accumulation of kynurenine. In this study, a novel radiotracer 1-methyl-D-tryptophan-[<sup>18</sup>F]BF<sub>3</sub> was developed for monitoring the metabolism of IDO inhibitors. Through organic synthesis, the precursor was successfully synthesized and subsequently radiolabeled, achieving a radiochemical yield of over 20% and a radiochemical purity of over 99%. Rapid clearance via renal and enterohepatic systems was observed, with strong uptake in the thyroid gland and stomach. Tumor uptake peaked at 10&#xa0;min post-injection in A431 and SW480 xenograft models (0.86&#xa0;%ID/g and 1.10&#xa0;%ID/g, respectively).</p>

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Synthesis and evaluation of 1-methyl-D-Trp-[18F]BF3: a novel tryptophan derivative radiotracer for PET imaging

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年4月28日

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  • Guolin Wang,
  • Jiawei Zhang,
  • Xinhui Su,
  • Qianhe Xu,
  • Donghe Chen,
  • Qian Zhang,
  • Zhenfeng Liu

摘要

Overexpression of indoleamine 2, 3-dioxygenase (IDO) in tumors leads to excessive consumption of tryptophan and accumulation of kynurenine. In this study, a novel radiotracer 1-methyl-D-tryptophan-[18F]BF3 was developed for monitoring the metabolism of IDO inhibitors. Through organic synthesis, the precursor was successfully synthesized and subsequently radiolabeled, achieving a radiochemical yield of over 20% and a radiochemical purity of over 99%. Rapid clearance via renal and enterohepatic systems was observed, with strong uptake in the thyroid gland and stomach. Tumor uptake peaked at 10 min post-injection in A431 and SW480 xenograft models (0.86 %ID/g and 1.10 %ID/g, respectively).